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The aim of present work is to formulate and characterize the Vildagliptin (VLD) loaded polymeric nanoparticles for the treatment of type II diabetes mellitus. Polymeric nanoparticles were prepared by ionotropic gelation method with sodium tripolyphosphate (STPP) as a cross linkers. The obtained sample of VLD was evaluated by UV and FT-IR studies. Prepared polymeric nanoparticles were characterized in term of drug-polymer intraction, particle size and polydispersity index (PDI), zeta potential, % drug content (DC), % drug entrapment efficiency (DEE) and scanning electron microscopy (SEM). In vitro and in vivo drug release studies were also performed. FT-IR study showed that drug and polymers are compatible with each other and cross-linking was observed between chitosan and STPP. Particle size was range from 238.2 nm to 708.8nm for all the formulations. Zeta potential was range from-8.49mV to 11.1mV. %DC range from68.12% to 84.37%, and % DEE was range from 78.76% to 93.91%. SEM images showed that the prepared formulations were smooth and spherical. In vitro drug release evaluation in phosphate buffer pH 7.4 showed sustained release pattern, i.e. 55.17% to 62.89% within 12hours. The data were fitted to Korsmeyer-Peppas model which showed fickian diffusion as a predominant release mechanism. In vivo drug release evalutionshowed significant decrease in the blood glucose level. Thus, conclude that prepared polymeric nanoparticles by ionotropic gelation method have a sustain release pattern and incresesstabilty of drug. [ABSTRACT FROM AUTHOR]

Nasrul Wathoni,1,* Yedi Herdiana,1,* Cecep Suhandi,1,* Ahmed Fouad Abdelwahab Mohammed,2,* Ali El-Rayyes,3,* Angga Cipta Narsa4,* 1Department of Pharmaceutics and Pharmaceutical Technology, Faculty of Pharmacy, Universitas Padjadjaran, Jatinangor, 45363, Indonesia; 2Department of Pharmaceutics, Faculty of Pharmacy, Minia University, Minia, 61519, Egypt; 3Department of Chemistry, College of Science, Northern Border University, Arar, Saudi Arabia; 4Department of Pharmaceutics and Pharmaceutical Technology, Faculty of Pharmacy, Mulawarman University, Samarinda, 71157, Indonesia*These authors contributed equally to this workCorrespondence: Nasrul Wathoni, Department of Pharmaceutics and Pharmaceutical Technology, Faculty of Pharmacy, Universitas Padjadjaran, Jatinangor, 45363, Indonesia, Tel +62-22-842-888-888, Email nasrul@unpad.ac.idAbstract: Nanoparticle systems integrating alginate and chitosan emerge as a promising avenue to tackle challenges in leveraging the potency of pharmacological active agents. Owing to their intrinsic properties as polysaccharides, alginate and chitosan, exhibit remarkable biocompatibility, rendering them conducive to bodily integration. By downsizing drug particles to the nano-scale, the system enhances drug solubility in aqueous environments by augmenting surface area. Additionally, the system orchestrates extended drug release kinetics, aligning well with the exigencies of chronic drug release requisite for antibacterial therapeutics. A thorough scrutiny of existing literature underscores a wealth of evidence supporting the utilization of the alginate-chitosan nanoparticle system for antibacterial agent delivery. Literature reviews present abundant evidence of the utilization of nanoparticle systems based on a combination of alginate and chitosan for antibacterial agent delivery. Various experiments demonstrate enhanced antibacterial efficacy, including an increase in the inhibitory zone diameter, improvement in the minimum inhibitory concentration, and an enhancement in the bacterial reduction rate. This enhancement in efficacy occurs due to mechanisms involving increased solubility resulting from particle size reduction, prolonged release effects, and enhanced selectivity towards bacterial cell walls, stemming from ionic interactions between positively charged particles and teichoic acid on bacterial cell walls. However, clinical studies remain limited, and there are currently no marketed antibacterial drugs utilizing this system. Hence, expediting clinical efficacy validation is crucial to maximize its benefits promptly.Keywords: alginate, chitosan, polymeric nanoparticle, antibacterial agents, drug delivery, controlled release, nano-delivery systems

Artificial intelligence has revolutionized many sectors with unparalleled predictive capabilities supported by machine learning (ML). So far, this tool has not been able to provide the same level of development in pharmaceutical nanotechnology. This review discusses the current data science methodologies related to polymeric drug-loaded nanoparticle production from an innovative multidisciplinary perspective while considering the strictest data science practices. Several methodological and data interpretation flaws were identified by analyzing the few qualified ML studies. Most issues lie in following appropriate analysis steps, such as cross-validation, balancing data, or testing alternative models. Thus, better-planned studies following the recommended data science analysis steps along with adequate numbers of experiments would change the current landscape, allowing the exploration of the full potential of ML. Executive summary Data science The main methodologies in data science are presented, including the knowledge discovery in databases (KDDs). Extracting new knowledge from datasets requires the realization of critical steps. The model should be validated outside the laboratory to assess its compliance. State-of-the-art polymeric nanoparticles assisted by data science Only a few qualified studies used machine learning to obtain polymeric nanoparticles. Several methodological flaws were identified, considering modern practices in data science. Databases commonly showed an inappropriate number of experiments. All the studies were performed using commercial software without personalized computer programming. Several studies exhibited models with apparent problems of overfitting or selection bias. Opportunities for improvements Data science analysis steps should be scrupulously followed with the assistance of an expert in the field. Performing an appropriate data balancing and the proper number of experiments is crucial. Better-planned studies using machine learning could lead to reliable and helpful real-life models. [ABSTRACT FROM AUTHOR]

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Gout is an inflammatory arthropathy resulting from the deposition of monosodium urate crystals in and around joints, triggering the release of pro-inflammatory cytokines. Some of the key principles for managing gout are encompassing comorbidity screening, gout flare treatment, urate-lowering therapy, and anti-inflammatory prophylaxis. One of the major concerns with gout treatment is the side effects of drug due to uncontrolled biodistribution. Nanocarrier systems are utilized to surmount the limitations of current drugs, including not only biodistribution issues but also the stability and bioavailability of the drugs. Nanocarriers as promising drug delivery systems can effectively deliver drugs by specifically targeting inflamed tissues through enhanced permeability and retention effect mediated delivery. Notable examples include liposomes, niosomes, ethosomes, transfersomes, solid lipid nanoparticles, polymeric nanoparticles, nanoemulsions, and liquid crystalline nanoparticles, namely, cubosomes, hexosomes, and spongosomes. These nanocarriers hold great promise as vehicles for transporting poorly therapeutic agents to precise target sites, associated with controlled release capabilities to bolster bioavailability. Preclinical studies have demonstrated the efficacy of nanocarrier-based therapies in reducing inflammation by specifically targeting inflamed tissues, inhibiting urate crystal formation, and improving joint function in animal models of gout. In this review, we explore the main nanocarrier systems, including their respective advantages and drawbacks, and emphasize their role in nanoformulations for advancing gout treatment. The encapsulation of active agents within nanocarriers for gout therapy represents a significant advancement in the pharmaceutical area and nanomedicine application to succeed in the overall context of gout treatment in the near future. [ABSTRACT FROM AUTHOR]

Developing combination chemotherapy systems with high drug loading efficiency at predetermined drug ratios to achieve a synergistic effect is important for cancer therapy. Herein, a polymeric dual‐drug nanoparticle composed of a Pt(IV) prodrug derived from oxaliplatin and a mitochondria‐targeting cytotoxic peptide is constructed through emulsion interfacial polymerization, which processes high drug loading efficiency and high biocompatibility. The depolymerization of polymeric dual‐drug nanoparticle and the activation of Pt prodrug can be effectively triggered by the acidic tumor environment extracellularly and the high levels of glutathione intracellularly in cancer cells, respectively. The utilization of mitochondria‐targeting peptide can inhibit ATP‐dependent processes including drug efflux and DNA damage repair. This leads to increased accumulation of Pt‐drugs within cancer cells. Eventually, the polymeric dual‐drug nanoparticle demonstrates appreciable antitumor effects on both cell line derived and patient derived xenograft lung cancer model. It is highly anticipated that the polymeric dual‐or multi‐drug systems can be applied for combination chemotherapy to achieve enhanced anticancer activity and reduced side effects. [ABSTRACT FROM AUTHOR]

Multilayered polymeric particles work as carriers of compounds with controlled release triggered by the layer's disassembly, allowing chemical stability along with transport through the bloodstream and tissues. Here, we present versatile multilayered polymeric particles as a vaccine approach against COVID-19 based on coupling a recombinant form of the receptor binding domain (RBD) antigen of the SARS-CoV-2 Spike proteins. The particle core comprises poly-(d,l-lactide) coated with Triton X-100 and polyethylenimine, prepared by nanoemulsion/solvent evaporation method and functionalized with heparin by layer-by-layer (PLTP-H). The recombinant RBD is anchored to the nanoparticles by the negative outer layer (PLTP-H-RBD). The nanoparticles reached a complexation efficiency of 95% for the RBD and a final hydrodynamic diameter of 140 nm with a zeta potential of −46 mV. No toxicity was recorded with the nanoparticles using cultured mammalian cells or after inoculation into mice. The immunization of mice with antigen-loaded nanoparticles induced strong adjuvant effects on the serum levels of RBD-specific IgG antibodies, which were capable of neutralizing the virus under in vitro conditions. Furthermore, PLTP-H-RBD conferred enhanced protective immunity to mice challenged with the SARS-CoV-2 virus. These findings represent a proof of concept for the use of PLTP-H as a delivery and adjuvant strategy for recombinant vaccine antigens aiming at the induction of neutralizing antibodies. [ABSTRACT FROM AUTHOR]

Breast cancer is associated with high morbidity and mortality in women since conventional treatment methods are limited due to toxicity problems and inadequate targeting of cancer cells. The aim of this study is to develop caffeic acid phenethyl ester (CAPE) loaded polymeric nanoparticles to provide treatment for breast cancer and investigate their anti-tumor activity on MCF-7 and MDA-MB-231 breast cancer cells. CAPE was encapsulated into poly lactic-co-glycolic acid (PLGA) polymer using single-emulsion (o/w) solvent evaporation method and characterization of CAPE loaded PLGA nanoparticles (CAPE-NPs) were performed by particle size, zeta potential, polydispersity index , in vitro release profile, and surface morphology. CAPE-NPs were tested for cytotoxicity, anti-migration, anti-proliferation and apoptotic activities on breast cancer cells. The mean nanoparticle size was found as 196,1 ± 8982 nm and polydispersity index (PDI) was 0186 ± 0069. The results of the in vitro cell culture studies indicated that treatment of breast cancer cells with CAPE and CAPE-NPs inhibited cell viability and proliferation. IC 50 values for 48 h were determined as 28.35 μg/ml,19.57 μg/ml for CAPE and CAPE-NP, respectively. Additionally, CAPE-NPs induced intrinsic pathway of apoptosis in MCF-7 and MDA-MB-231 cell lines. Overall, CAPE-NPs showed more efficient anti-tumour activity on breast cancer cells by small size and enhanced bioavability. [Display omitted] • The aim of this study is to develop CAPE-NPs to provide treatment for breast cancer. • CAPE loaded PLGA nanoparticles were produced (CAPE-NPs). • CAPE-NPs anti-tumour activity was evaluated on breast cancer cell lines. • CAPE-NPs exhibited higher cytotoxicity than CAPE due to their small size and controlled release. • CAPE-NPs demonstrated a decrease in cell proliferation and induced the intrinsic pathway of apoptosis. [ABSTRACT FROM AUTHOR]

Poly-hydroxyethyl methacrylate [p(HEMA)] is one of the most widely used polymers in different biomedical applications because it is a biocompatible and a biodegradable material. Tryptophan (Trp) is a biocompatible, antioxidant, and anti-inflammatory amino acid. Trp modification contributes to the more effective use of nanoparticles in cancer therapy. The aim of this study was to synthesize polymeric nanoparticles tryptophan-graft-poly(HEMA) [Trp-g-p(HEMA)] and assess characterization and toxicity/biocompatibility potential of it in terms of using a drug carrier. The nanoparticles were synthesized with surfactant-free emulsion polymerization and grafting technique and the grafting efficiency was found as 78.65 ± 2.48%. The characterization of the nanoparticles was performed by FT-IR spectroscopy, zeta analysis, scanning electron microscopy, atomic force microscopy, and swelling test. The nanopolymers had the spectra from 750 to 4000 cm−1 and characteristic peaks of stretching bands, 164.1 ± 29.2 nm average size, − 10.2 ± 8.7 mV surface charge, smooth surface, and nearly spherical shape. The swelling ratios of them were estimated as 79.52 ± 0.86% in d.w. and 93.33 ± 2.32% in PBS at 25 °C, 35.71 ± 0.62% in d.w., and 42.86 ± 0.64% in PBS at 37 °C. The nanoparticles did not induce cytotoxicity, oxidative stress generation, and genotoxicity on human healthy lymphocyte cells. Trp-g-p(HEMA) had hemocompatible properties. We found no irritant effect in the HET-CAM test. The acute oral LD50 value of the nanopolymers was > 2000 mg/kg body weight on BALB/c mice. We announce that the polymeric nanoparticles Trp-g-p(HEMA) is a biocompatible material and has potential to use as a drug carrier for oral, intravenous, and ocular administrations. [ABSTRACT FROM AUTHOR]

Despite the global administration of approved COVID-19 vaccines (e.g., ChAdOx1 nCoV-19®, mRNA-1273®, BNT162b2®), the number of infections and fatalities continue to rise at an alarming rate because of the new variants such as Omicron and its subvariants. Including COVID-19 vaccines that are licensed for human use, most of the vaccines that are currently in clinical trials are administered via parenteral route. However, it has been proven that the parenteral vaccines do not induce localized immunity in the upper respiratory mucosal surface, and administration of the currently approved vaccines does not necessarily lead to sterilizing immunity. This further supports the necessity of a mucosal vaccine that blocks the main entrance route of COVID-19: nasal and oral mucosal surfaces. Understanding the mechanism of immune regulation of M cells and dendritic cells and targeting them can be another promising approach for the successful stimulation of the mucosal immune system. This paper reviews the basic mechanisms of the mucosal immunity elicited by mucosal vaccines and summarizes the practical aspects and challenges of nanotechnology-based vaccine platform development, as well as ligand hybrid nanoparticles as potentially effective target delivery agents for mucosal vaccines. This review shows the induction of mucosal immunity efficiently induces secretory IgA and IgG in the upper respiratory tract and systemic immunity via intranasal administration of nanovaccine. [Display omitted] [ABSTRACT FROM AUTHOR]

In spinal cord injuries, axonal regeneration decreases with the activation of astrocytes followed by glial scar formation. Targeting reactive astrocytes has been recently performed by unsafe viral vectors to inhibit gliosis. In the current study, biocompatible polymeric nanoparticles were selected as an alternative for viruses to target reactive astrocytes for further drug/gene delivery applications. Lipopolysaccharide-bonded chitosan-quantum dots/poly acrylic acid nanoparticles were prepared by ionic gelation method to target reactive astrocytes both in vitro and in spinal cord-injured rats. Owing to their biocompatibility and pH-responsive behavior, chitosan and poly acrylic acid were the main components of nanoparticles. Nanoparticles were then chemically labeled with quantum dots to track the cell uptake and electrostatically interacted with lipopolysaccharide as a targeting ligand. In vitro and in vivo studies were performed in triplicate and all data were expressed as the mean ± the standard error of the mean. Smart nanoparticles with optimum size (61.9 nm) and surface charge (+ 12.5 mV) successfully targeted primary reactive astrocytes extracted from the rat cerebral cortex. In vitro studies represented high cell viability (96%) in the exposure of biocompatible nanoparticles. The pH-responsive behavior of nanoparticles was proved by their internalization into the cell's nuclei due to the swelling and endosomal escape of nanoparticles in acidic pH. In vivo studies demonstrated higher transfection of nanoparticles into reactive astrocytes compared to the neurons. pH-responsive ligand-bonded chitosan-based nanoparticles are good alternatives for viral vectors in targeted delivery applications for the treatment of spinal cord injuries. [ABSTRACT FROM AUTHOR]

In this study, green self-assembled two-dimensional (2D) bio-preservatives were prepared for the sonosynthesis of sandalose gum-supported bio-polymeric nanoparticles (PNPs) with excellent biological activities. Polyvinyl alcohol (PVA), alginate (Alg), and sandalose gum (SG) were used to fabricate the green and low-cost bio-preservative. The prepared PVA/Alg/SG PNPs were confirmed using various characterization techniques such as SEM, HRTEM, XRD, FTIR, DLS, zeta potential, TGA, and DSC. According to the surface characterization results, the green self-assembled 2D PVA/Alg/SG PNPs had a spherical shape and particle diameters ranging from 10–50 nm. The thermal results showed that PVA/Alg/SG PNPs had good thermal stability. Furthermore, we investigated the antibacterial and antifungal activities of the self-assembled 2D PVA/Alg/SG PNPs as a safe bio-preservative against pathogenic microorganisms for use in biomedical applications. Consequently, our experimental results indicated a strong synergistic interaction between pathogenic microorganisms and the surface of the 2D nanostructure, resulting in the preservative efficacy of PNPs with a high performance. [ABSTRACT FROM AUTHOR]

The identification of novel biomarkers and therapeutic targets in advanced cancer is critical for improving cancer diagnosis and therapeutics. Survivin (SV) is highly expressed predominantly in most cancer cells and tissues but is absent or undetectable in terminally differentiated normal adult tissues. Therefore, it functions as an almost universal tumor antigen. Peptides are short chains of amino acids linked by peptide bonds. To obtain novel SV decamers that are able to induce SV-specific cytotoxic T lymphocytes (CTLs) with a higher cytotoxic efficiency against cancer cells, major histocompatibility complex (MHC) peptide binding algorithms were conducted to predict nine modified SV95 decamers (from SV95-2 to SV95-10) based on the natural SV95-104 peptide sequence of ELTLGEFLKL (here defined as SV95-1). The fluorescent density of each SV95 peptide was determined by a MHC stability assay, followed by the generation of SV95-specific CTLs with each SV95 peptide (from SV95-1 to SV95-10) and human dendritic cells (DCs) loaded with Poly(lactic-co-glycolic) acid (PLGA) nanoparticles encapsulated with SV95 peptide. Finally, IFN-γ ELISpot and CytoTox 96® Non-Radioactive Cytotoxicity Assays were employed to verify their cytotoxic efficiency of the SV95-specific CTLs generated with the corresponding artificial antigen presenting cells (aAPCs) containing SV95 (SV95-1 to SV95-10) peptide. Furthermore, the cytotoxicity of the SV95 specific CTLs generated with nine mutated SV95 peptides was compared to the one generated with natural SV95-1 peptide and TIL2080 cells. The results indicated that the HLA-A2-restricted mutated SV95 epitope decamers (SV95-6 and SV95-7) showed significant higher binding ability compared to natural peptide SV95-1 in MHC stability assay. More importantly, SV95-specific CTLs with higher cytotoxicity were successfully induced with both SV95-6 and SV95-7 peptides, which significantly eliminated target cells (not only SV95-1 peptide pulsed T2 cells, but also both HLA-A2 and SV positive cancer cells) when compared to those generated with natural SV95-1 peptide and TIL2080 cells. These findings suggest that the SV95-6 and SV95-7 peptides are two novel HLA-A2-restricted CTL epitopes and may be useful for the immunotherapy for patients with survivin expressing cancer.

Introduction: The amalgamation of novel drug delivery techniques and potential drugs is considered the most promising tool for the treatment of diseases. In our study, we have employed N-isopropyl acrylamide, N-vinyl pyrrolidone, and acrylic acid (NIPAAM-VP-AA) copolymeric nanoparticles for delivering Ipomoea turpethum root extract. I. turpethum is a perennial herb (Convolvulaceae family) and has been used as medicine for ages. The present study was conducted to evaluate the safety of I. turpethum root extract-loaded NIPAAMVP-AA polymeric nanoparticles (NVA-IT) in Wistar rats. Methods: An acute oral toxicity study was conducted in accordance with OECD guidelines 423 for the testing of chemicals. Different doses of NVA-IT i.e., 5 mg/kg, 50 mg/kg, 300 mg/kg, and 2000 mg/kg were administered to female Wistar rats in a stepwise manner using oral gavage. The toxicity signs were thoroughly observed for the next 14 days. At the end of the study, the blood and vital organs were harvested for hematological, biochemical, and histopathological studies. Result: No mortality or pathological anomalies were observed even at the highest dose which exemplifies that the lethal dose would be more than 2000 mg/kg body weight (GSH category 5). Behavioral changes, biochemical parameters, and histopathology of vital organs were normal after NVA-IT administration. Conclusion: This study demonstrated that NVA-IT nanoparticles are non-toxic and can be considered for therapeutic use in different diseases, such as inflammation, CNS diseases, Cancer, etc. [ABSTRACT FROM AUTHOR]

Cancer develops with unexpected mutations and causes death in many patients. Among the different cancer treatment strategies, immunotherapy is promising with the benefits of high specificity and accuracy, as well as modulating immune responses. Nanomaterials can be used to formulate drug delivery carriers for targeted cancer therapy. Polymeric nanoparticles used in the clinic are biocompatible and have excellent stability. They have the potential to improve therapeutic effects while significantly reducing off-target toxicity. This review classifies smart drug delivery systems based on their components. Synthetic smart polymers used in the pharmaceutical industry, including enzyme-responsive, pH-responsive, and redox-responsive polymers, are discussed. Natural polymers derived from plants, animals, microbes, and marine organisms can also be used to construct stimuli-responsive delivery systems with excellent biocompatibility, low toxicity, and biodegradability. The applications of smart or stimuli-responsive polymers in cancer immunotherapies are discussed in this systemic review. We summarize different delivery strategies and mechanisms that can be used in cancer immunotherapy and give examples of each case. [ABSTRACT FROM AUTHOR]

Alpha mangostin (AM) has potential anticancer properties for breast cancer. This study aims to assess the potential of chitosan nanoparticles coated with hyaluronic acid for the targeted delivery of AM (AM-CS/HA) against MCF-7 breast cancer cells. AM-CS/HA showed a spherical shape with an average diameter of 304 nm, a polydispersity index of 0.3, and a negative charge of 24.43 mV. High encapsulation efficiency (90%) and drug loading (8.5%) were achieved. AM released from AM-CS/HA at an acidic pH of 5.5 was higher than the physiological pH of 7.4 and showed sustained release. The cytotoxic effect of AM-CS/HA (IC50 4.37 µg/mL) on MCF-7 was significantly higher than AM nanoparticles without HA coating (AM-CS) (IC50 4.48 µg/mL) and AM (IC50 5.27 µg/mL). These findings suggest that AM-CS/HA enhances AM cytotoxicity and has potential applications for breast cancer therapy. [ABSTRACT FROM AUTHOR]

Black pepper, a commonly utilized culinary condiment, holds significant importance in Ayurvedic and Chinese medicinal practices due to its various biological benefits, including antioxidant, antimicrobial, and anti-inflammatory properties. To amplify these attributes and enhance their efficacy in formulations, the utilization of nanocarriers presents a promising approach. Thus, the objective of this study was to obtain a pepper extract, evaluate its constituents, and encapsulate it in polymeric nanoparticles. The ethanol extract of the grains powder had a higher concentration of piperine and better antioxidant activity when compared to whole grains. Pepper extract encapsulation efficiency in terms of piperine concentration was 84.8 ± 3.5%, and a sustained and prolonged release profile was observed, as well as other studies in the literature using polycaprolactone (PCL). The presence of the extract did not change the instability index and the sedimentation velocity of the nanoparticles, as well as the polydispersity index and the zeta potential of nanoparticles. However, there was a difference in the mean size and concentration of particles. This study highlights the potential of PCL nanoparticles as a promising delivery system for black pepper extract, which could have various applications in the cosmetic and pharmaceutical industries, maximizing the benefits of black pepper extract.

Introduction: The amalgamation of novel drug delivery techniques and potential drugs is considered the most promising tool for the treatment of diseases. In our study, we have employed N-isopropyl acrylamide, N-vinyl pyrrolidone, and acrylic acid (NIPAAM-VP-AA) copolymeric nanoparticles for delivering Ipomoea turpethum root extract. I. turpethum is a perennial herb (Convolvulaceae family) and has been used as medicine for ages. The present study was conducted to evaluate the safety of I. turpethum root extract-loaded NIPAAM-VP-AA polymeric nanoparticles (NVA-IT) in Wistar rats.Methods: An acute oral toxicity study was conducted in accordance with OECD guidelines 423 for the testing of chemicals. Different doses of NVA-IT i.e., 5 mg/kg, 50 mg/kg, 300 mg/kg, and 2000 mg/kg were administered to female Wistar rats in a stepwise manner using oral gavage. The toxicity signs were thoroughly observed for the next 14 days. At the end of the study, the blood and vital organs were harvested for hematological, biochemical, and histopathological studies.Result: No mortality or pathological anomalies were observed even at the highest dose which exemplifies that the lethal dose would be more than 2000 mg/kg body weight (GSH category 5). Behavioral changes, biochemical parameters, and histopathology of vital organs were normal after NVA-IT administration.Conclusion: This study demonstrated that NVA-IT nanoparticles are non-toxic and can be considered for therapeutic use in different diseases, such as inflammation, CNS diseases, Cancer, etc.

Purpose: Hepatitis B virus (HBV) infection is such a global health problem that hundreds of millions of people are HBV carriers. Current anti-viral agents can inhibit HBV replication, but can hardly eradicate HBV. Cytosine-phosphate-guanosine (CpG) oligodeoxynucleotides (ODNs) are an adjuvant that can activate plasmacytoid dendritic cells (pDCs) and conventional dendritic cells (cDCs) to induce therapeutic immunity for HBV eradication. However, efficient delivery of CpG ODNs into pDCs and cDCs remains a challenge. In this study, we constructed a series of cationic lipid-assisted nanoparticles (CLANs) using different cationic lipids to screen an optimal nanoparticle for delivering CpG ODNs into pDCs and cDCs. Methods: We constructed different CLANCpG using six cationic lipids and analyzed the cellular uptake of different CLANCpG by pDCs and cDCs in vitro and in vivo, and further analyzed the efficiency of different CLANCpG for activating pDCs and cDCs in both wild type mice and HBV-carrier mice. Results: We found that CLAN fabricated with 1,2-Dioleoyl-3-trimethylammonium propane (DOTAP) showed the highest efficiency for delivering CpG ODNs into pDCs and cDCs, resulting in strong therapeutic immunity in HBV-carrier mice. By using CLANCpG as an immune adjuvant in combination with the injection of recombinant hepatitis B surface antigen (rHBsAg), HBV was successfully eradicated and the chronic liver inflammation in HBV-carrier mice was reduced. Conclusion: We screened an optimized CLAN fabricated with DOTAP for efficient delivery of CpG ODNs to pDCs and cDCs, which can act as a therapeutic vaccine adjuvant for treating HBV infection. [ABSTRACT FROM AUTHOR]

Various types of skin disorders across each age group and in each part of geographical world are very dreadful. Despite not being fatal each time they are always of social and mental concern for suffering individuals, causing complications in millions of patients every day and require comparatively longer duration of treatment. Off late, various topical/transdermal formulations have been widely explored for the treatment of various skin ailments. The efficiency of topical therapy depends on various physiochemical properties of drugs like particle size, particle size distribution, partition coefficient, viscosity of dosage form, skin permeability, skin condition and the site of application. Therefore, in plenty of examples, long-acting topical formulations have shown to be markedly excellent in comparison to conventional dosage forms. The major advantages of topical formulations accrue from their demonstrated ability: (i) Reduced serious side effects that may occur due to undesirably higher systemic absorption of drug. (ii) Enhancement of drug accumulation at the desired site. (iii) Easy incorporation of enormous range of hydrophilic and hydrophobic drugs and (iv) Reduced risk of dose dumping and comparatively easy termination of drug release. The prospective applications of topically applied formulations and the deposition of pharmaceuticals into the skin are examined. [ABSTRACT FROM AUTHOR]

Leishmaniasis is a widespread vector-borne disease in Brazil, with Leishmania (Leishmania) infantum as the primary etiological agent of visceral leishmaniasis (VL). Dogs are considered the main reservoir of this parasite, whose treatment in Brazil is restricted to the use of veterinary medicines, which do not promote a parasitological cure. Therefore, efficient vaccine development is the best approach to Canine Visceral Leishmaniasis (CVL) control. With this in mind, this study used hamsters (Mesocricetus auratus) as an experimental model in an anti-Leishmania preclinical vaccine trial to evaluate the safety, antigenicity, humoral response, and effects on tissue parasite load. Two novel formulations of nanoparticles made from poly(D, L-lactic) acid (PLA) polymer loading Leishmania braziliensis crude antigen (LB) exhibiting two different particle sizes were utilized: LBPSmG (570 nm) and LBPSmP (388 nm). The results showed that the nanoparticles were safe and harmless to hamsters and were antigenic with the induction in LBSap, LBPSmG, and LBPSmG groups of total anti-Leishmania IgG antibodies 30 days after challenge, which persists 200 days in LBSap and LBPSmP. At the same time, a less pronounced hepatosplenomegaly in LBSap, LBPSmG, and LBPSmP was found when compared to control groups, as well as a less pronounced inflammatory infiltrate and granuloma formation in the spleen. Furthermore, significant reductions of 84%, 81%, and 90% were observed in spleen parasite burden accessed by qPCR in the LBSap, LBPSmG, and LBPSmP groups, respectively. In this way, LBSap, LBPSmG, and LBPSmP formulations showed better results in vaccinated and L. infantum-challenged animals in further reducing parasitic load in the spleen and attenuating lesions in liver and splenic tissues. This results in safe, harmless nanoformulation vaccines with significant immunogenic and infection control potential. In addition, animals vaccinated with LBPSmP had an overall reduction in parasite burden in the spleen, indicating that a smaller nanoparticle could be more efficient in targeting antigen-presenting cells. [ABSTRACT FROM AUTHOR]

Polymeric nanoparticles have emerged as promising contenders for addressing the intricate challenges encountered in brain tumor therapy due to their distinctive attributes, including adjustable size, biocompatibility, and controlled drug release kinetics. This review comprehensively delves into the latest developments in synthesizing, characterizing, and applying polymeric nanoparticles explicitly tailored for brain tumor therapy. Various synthesis methodologies, such as emulsion polymerization, nanoprecipitation, and template-assisted fabrication, are scrutinized within the context of brain tumor targeting, elucidating their advantages and limitations concerning traversing the blood-brain barrier. Furthermore, strategies pertaining to surface modification and functionalization are expounded upon to augment the stability, biocompatibility, and targeting prowess of polymeric nanoparticles amidst the intricate milieu of the brain microenvironment. Characterization techniques encompassing dynamic light scattering, transmission electron microscopy, and spectroscopic methods are scrutinized to evaluate the physicochemical attributes of polymeric nanoparticles engineered for brain tumor therapy. Moreover, a comprehensive exploration of the manifold applications of polymeric nanoparticles encompassing drug delivery, gene therapy, imaging, and combination therapies for brain tumours is undertaken. Special emphasis is placed on the encapsulation of diverse therapeutics within polymeric nanoparticles, thereby shielding them from degradation and enabling precise targeting within the brain. Additionally, recent advancements in stimuli-responsive and multifunctional polymeric nanoparticles are probed for their potential in personalized medicine and theranostics tailored for brain tumours. In essence, this review furnishes an all-encompassing overview of the recent strides made in tailoring polymeric nanoparticles for brain tumor therapy, illuminating their synthesis, characterization, and multifaceted application. [Display omitted] • Polymeric nanoparticles are promising agent for brain tumor therapy. • Polymeric nanoparticles can adjust size, biocompatibility for Brain tumor therapy. • Polymeric nanoparticles can be used controlled drug release. • Characterization, applications and challenges has been highlighted. [ABSTRACT FROM AUTHOR]

Epiisopiloturine (EPI) is a compound found in jaborandi leaves with antiparasitic activity, which can be enhanced when incorporated into nanoparticles (NP). Cashew Gum (CG), modified by carboxymethylation, is used to produce polymeric nanomaterials with biological activity. In this study, we investigated the antimicrobial potential of carboxymethylated CG (CCG) NP containing EPI (NPCCGE) and without the alkaloid (NPCCG) against bacteria and parasites of the genus Leishmania. We conducted theoretical studies, carboxymethylated CG, synthesized NP by nanoprecipitation, characterized them, and tested them in vitro. Theoretical studies confirmed the stability of modified carbohydrates and showed that the EPI-4A30 complex had the best interaction energy (−8.47 kcal/mol). CCG was confirmed by FT-IR and presented DS abs of 0.23. NPCCG and NPCCGE had average sizes of 221.94 ± 144.086 nm and 247.36 ± 3.827 nm, respectively, with homogeneous distribution and uniform surfaces. No NP showed antibacterial activity or cytotoxicity to macrophages. NPCCGE demonstrated antileishmanial activity against L. amazonensis , both in promastigote forms (IC 50 = 9.52 μg/mL, SI = 42.01) and axenic amastigote forms (EC 50 = 6.6 μg/mL, SI = 60.60). The results suggest that nanostructuring EPI in CCG enhances its antileishmanial activity. [ABSTRACT FROM AUTHOR]

The surface properties of nanoparticles (NPs) affect their stability and formation of the protein corona, which influence their targeting abilities. We evaluated these properties using bone (hydroxyapatite; HAP) targeting peptide on tamoxifen (TAM)-loaded stereocomplexformed polylactide-polyethyleneglycol (SC-PLA-PEG) NPs. Octaaspartic acid-octaglycine-cysteine (D8G8C) anionic derivative (Ani. pep.) and octa-aspartic acid-octa lysine-cysteine (D8K8C), a zwitterionic derivative (Zwi. pep.) were conjugated with SC-PLA-PEG NPs as HAP-targeting peptides. The addition of hydrophobic PLA homopolymers increased the surface PEG density on the NPs. Denser PEG chains on NPs decreased their specific surface area, reducing protein adsorption on the NPs and TAM release from NPs. NPs with dense PEG chains and Zwi. pep. showed superior shelf stability and lower protein adsorption than NPs with dense PEG chains and Ani. pep. in murine serum. Furthermore, the HAP-binding ability of NPs with Zwi. pep. was significantly higher than that of NPs with Ani. pep. These results indicate that decreasing the specific surface area and zwitterionization of HAP-targeting peptides on NPs are promising approaches to improve the serum compatibility and stability of NPs. [Display omitted] [ABSTRACT FROM AUTHOR]

The aim of this study was to prepare rosuvastatin calcium (ROC)-loaded Eudragit® L100 polymeric nanoparticles (PNPs) and investigate their ability to enhance transdermal permeation. ROC is a new generation of statins which has been approved for lipid-lowering and anticancer activities. However, its poor oral bioavailability is a limiting factor for many clinical applications. Therefore, development of an efficient transdermal formulation would significantly improve its efficacy and reduce the risk of the side effects. ROC-loaded Eudragit® L100 nanoparticles were prepared by nanoprecipitation at different drug:polymer ratios. Differential light scattering (DLS) and atomic force microscopy (AFM) were used to characterize the nanoparticles. The results showed that increasing the polymer concentration will decrease the particle size from 187.4 ± 106 nm to 44.9 ± 9.3 nm at drug:polymer ratios from 1:1 to 1:9, respectively. The particle size and entrapment efficiency (EE) of the optimized formulation were 66 nm and 58%, respectively. The in vitro drug release study showed pH-dependent sustained release kinetics. Moreover, nanoparticles significantly enhanced ROC permeability by 1.6-fold through rat skin. These results suggest that nanoprecipitation can efficiently produce small, homogeneous ROC-loaded PNPs suitable for transdermal skin delivery applications. PNPs will help to develop a complex ROC PNPs formulations for various dermal and transdermal applications. [ABSTRACT FROM AUTHOR]

In this study, eugenol-loaded mPEG-PCL nanoparticles were used to improve the anti-bacterial properties of eugenol in an attempt to eliminate the resistant bacteria. The mPEG-PCL copolymer was prepared by ring-opening polymerization of ε -caprolactone monomer in the vicinity of a dry mPEG and a tin (II) octoate catalyst. Polymeric nanoparticles were prepared through the nanoprecipitation procedure. The particle size and zeta potential of mPEG-PCL/eugenol were found to be 1 5 7. 2 3 ± 3. 8 1 nm and − 6. 9 5 ± 0. 1 9 mV, respectively. The polymeric nanoparticle structure was identified by AFM, FT-IR, and DSC techniques. To evaluate and compare the antibacterial efficiency of mPEG-PCL/eugenol with that of free eugenol, a turbidity assay was used in association with gram-positive and gram-negative bacteria. SEM images were taken from the bacteria before and after exposure to the mPEG-PCL/eugenol. The colony-forming unit per milliliter (CFU/mL) method was used to evaluate the performance of mPEG-PCL/eugenol on the growth rate of bacteria in hospital wastewater. The results showed that the mPEG-PCL/eugenol nanoparticles demonstrated an enormous antibacterial effect in connection with wild gram-negative bacteria strains at 40 μ M concentration and 37∘C. In the original hospital wastewater, mPEG-PCL/eugenol at the concentration of 0.125 μ M at 25∘C showed the largest decrease in the total microbial count. Nanotechnology is very effective in eliminating bacterial infections and can be considered as a suitable alternative to antibiotics. In this research, the antibacterial effect of eugenol entrapped in polymeric nanoparticles (mPEG-PCL/eugenol) on resistant bacteria was investigated. mPEG-PCL copolymer was used as a carrier to prepare nano micelles of eugenol. Then, the antibacterial effect of eugenol-loaded mPEG-PCL on drug resistant bacteria isolated from hospital wastewater was studied. [ABSTRACT FROM AUTHOR]

Polymeric nanoparticles (NPs) play an important role in controlled cancer drug delivery. Anticancer drugs can be conjugated or encapsulated by polymeric nanocarriers, which are known as polymeric nanomedicine. Polymeric nanomedicine has shown its potential in providing sustained release of drugs with reduced cytotoxicity and modified tumor retention, but until now, few delivery systems loading drugs have been able to meet clinical demands, so more efforts are needed. This research reviews the current state of the cancer drug-loading system by exhibiting a series of published articles that highlight the novelty and functions from a variety of different architectures including micelles, liposomes, dendrimers, polymersomes, hydrogels, and metal–organic frameworks. These may contribute to the development of useful polymeric NPs to achieve different therapeutic purposes.

Nowadays antibiotic resistance is one of the most serious problems. Therefore, there is a need for sustained and controlled drug release systems for antibiotics. The aim of this study was to develop a nano-antibiotic system using biocompatible and antimicrobial polymers that are abundant in nature. Frequently used amoxicillin was chosen as the antibiotic. Before nanoparticle synthesis kappa-carrageenan was oxidized and 1.2% carboxyl, and 23.08% aldehyde groups were obtained, as confirmed by Fourier-transform infrared spectroscopy. A combination of polyelectrolyte complexation and ionic gelation was occurred in the nanoparticle synthesis. For the optimal temperature, CaCl2 concentration and polymer ratio of 37 °C, 1.5% and 6:1, respectively, the results of hydrodynamic size measurements indicated the size was 414.4 nm. Drug loading encapsulation was successful with an efficiency of 73.28%. Drug release was monitored for 95 h, and drug release was 93% and 85%, respectively, at pH 6.0 and pH 7.4. It is shown by the mathematical models that the drug release profile can be explained by the Higuchi and first-order models since R2 values were higher than for the other models. As a result, it was observed that the obtained nano-antibiotic delivery system performed a long-term drug release of approximately 4 days in a pH-sensitive manner and would be a promising drug delivery system. [ABSTRACT FROM AUTHOR]

The use of annatto pigments has been evaluated as a therapeutic strategy in animal models of several health disorders. Beneficial effects were generally attributed to the inhibition of oxidative stress. Bixin is the main pigment present in annatto seeds and has emerged as an important scavenger of reactive oxygen (ROS) and nitrogen species (RNS). However, this carotenoid is highly hydrophobic, affecting its therapeutic applicability. Therefore, bixin represents an attractive target for nanotechnology to improve its pharmacokinetic parameters. In this study, we prepared bixin nanoparticles (npBX) and evaluated if they could prevent pulmonary inflammation and oxidative stress induced by cigarette smoke (CS). C57BL/6 mice were exposed to CS and treated daily (by gavage) with different concentrations of npBX (6, 12 and 18%) or blank nanoparticles (npBL, 18%). The negative control group was sham smoked and received 18% npBL. On day 6, the animals were euthanized, and bronchoalveolar lavage fluid (BALF), as well as lungs, were collected for analysis. CS exposure led to an increase in ROS and nitrite production, which was absent in animals treated with npBX. In addition, npBX treatment significantly reduced leukocyte numbers and TNF-α levels in the BALF of CS-exposed mice, and it strongly inhibited CS-induced increases in MDA and PNK in lung homogenates. Interestingly, npBX protective effects against oxidative stress seemed not to act via Nrf2 activation in the CS + npBX 18% group. In conclusion, npBX prevented oxidative stress and acute lung inflammation in a murine model of CS-induced acute lung inflammation. [ABSTRACT FROM AUTHOR]

Simple Summary: Scientists have been working on the development of nanomedicine-based tumor therapy, rather than conventional treatment, to treat cancer for several years. Unfortunately, biological barriers hinder the delivery of nanomedicine to tumors. There are different strategies applied by researchers to improve the nanomedicine penetration to tumors, such as the modification of nanoparticle features and controlling the cancer micro-environment. However, complicated cancer micro-environments and delivery problems prevent these approaches from achieving optimal results. Changes in the extra-cellular matrix or blood vessels modify tumor microenvironments in a way that provides improved nanomedicine penetration and distribution but not to an optimal level. Herein, we reviewed the challenges of nanomedicine penetration to tumors along with possible approaches to deal with this concern. Nanomedicine has been under investigation for several years to improve the efficiency of chemotherapeutics, having minimal pharmacological effects clinically. Ineffective tumor penetration is mediated by tumor environments, including limited vascular system, rising cancer cells, higher interstitial pressure, and extra-cellular matrix, among other things. Thus far, numerous methods to increase nanomedicine access to tumors have been described, including the manipulation of tumor micro-environments and the improvement of nanomedicine characteristics; however, such outdated approaches still have shortcomings. Multi-functional convertible nanocarriers have recently been developed as an innovative nanomedicine generation with excellent tumor infiltration abilities, such as tumor-penetrating peptide-mediated transcellular transport. The developments and limitations of nanomedicines, as well as expectations for better outcomes of tumor penetration, are discussed in this review. [ABSTRACT FROM AUTHOR]

In this research, the antibacterial effect of curcumin entrapped in polymeric nanoparticles (mPEG-PCL/curcumin) on resistant bacteria were investigated. Ring-opening polymerization method was used for the synthesis of mPEG-PCL copolymers at 120 °C. mPEG-PCL and Sn (Oct)2 were used as initiator/catalyst respectively. Curcumin loaded polymeric nanoparticles were prepared using the nanoprecipitation method. The particle size and zeta potential of mPEG-PCL/curcumin were found to be 111.16 ± 3.26 nm and − 5.67 ± 5.26 mv, respectively. TEM, AFM, FTIR and DSC were used to determine the structure of polymeric nanoparticles. The impact of mPEG-PCL/curcumin on wild (w) and standard (s) strains in bacterial media was assessed through the procedures of turbidity assay and colony-forming based on units per milliliter (CFU/mL). The impact of mPEG-PCL/curcumin on wild (w) strains in main wastewater was assessed by colony-forming based on units per milliliter (CFU/mL). mPEG-PCL/curcumin at a concentration of 40 µM had a stronger effect on wild strains of bacteria at 37 °C. However, examination of the performance of mPEG-PCL/curcumin in wastewater showed that mPEG-PCL/curcumin can reduce the total microbial total count at a concentration of 0.125 µM and at 25 °C. [ABSTRACT FROM AUTHOR]

The effective control of an insect pest such as Drosophila suzukii (Diptera: Drosophilidae) has been challenging because its attack on red fruits can cause losses in production of up to 80% worldwide. The objective of this work was to extract and characterise the essential oil from rosemary (Rosmarinus officinalis), produce and characterise nanoparticles incorporated with this essential oil, evaluate the in vivo insecticide activity of free and nanoencapsulated essential oil against D. suzukii, and evaluate the effect of that oil on the enzyme acetylcholinesterase. The nanoparticles produced with the essential oil from rosemary had a particle size and surface charge of 236.6 nm and −11.8 mV, respectively. According to the FTIR data, the essential oil was incorporated into the polymeric matrix of poly(ε‐caprolactone). Through in vivo toxicity analysis, the free and nanoencapsulated essential oils were found to possess insecticidal activity, with an LD50 close to 9.1 g/L. The maximum anticholinesterase activity for the essential oil was 75% at a concentration of 0.10 mg/mL. The incorporation of the essential oil from R. officinalis into biodegradable nanoparticles of poly(ε‐caprolactone) potentiated and prolonged its in vivo insecticidal activity against D. suzukii. [ABSTRACT FROM AUTHOR]

To design and develop K-RAS silencing small interfering RNA (siRNA)-loaded poly (D, L-lactic-co-glycolic acid) nanoparticles and evaluate their efficacy in the treatment of K-RAS mutant lung cancer. The nanoparticles prepared by the double emulsion solvent evaporation method were characterized by TEM, FTIR and XPS analyzes and evaluated in vitro by XTT, PCR, ELISA, and Western-Blot. Metabolomic analyzes were performed to evaluate the changes in metabolic profiles of the cells after nanoparticles treatment. The nanoparticles were obtained with a particle size less than 250 nm, a polydispersity index around 0.1, a surface charge of (−12) – (+14) mV, and 80% of the siRNA encapsulation. The nanoparticles didn't affect cell viability of the cells after 72 hours. In cancer cells, KRAS expression was decreased by up to 50%, protein levels were decreased by more than 90%. The formulated siRNA delivery nanoparticles can be promising treatment in lung cancer. [ABSTRACT FROM AUTHOR]

Polymeric nanoparticles made of the copolymer Poly(L-lactide-co-caprolactone-co-glycolide) were prepared using the solvent evaporation method. Two different surfactants, polyvinyl alcohol and dextran, and a mixture of the two were employed. The three types of nanoparticles were used as hosting carriers of two chemotherapeutic drugs, the hydrophilic doxorubicin and the hydrophobic SN-38. The morphostructural characterization showed similar features for the three types of nanoparticles, while the drug encapsulation efficiency indicated that the dextran-based systems are the most effective with both drugs. Cellular studies with breast cancer cells were performed to compare the delivery capability and the cytotoxicity profile of the three nanosystems. The results show that the unloaded nanoparticles are highly biocompatible at the administered concentrations and confirmed that dextran-coated nanoparticles are the most efficient vectors to release the two drugs, exerting cytotoxic activity. PVA, on the other hand, shows limited drug release in vitro, probably due to strong interactions with both drugs. Data also show the release is more efficient for doxorubicin than for SN-38; indeed, the doxorubicin IC50 value for the dextran-coated nanoparticles was about 35% lower than the free drug. This indicates that these nanocarriers are suitable candidates to deliver hydrophilic drugs while needing further modification to host hydrophobic molecules. [ABSTRACT FROM AUTHOR]

Nanoparticles are used mainly for the transmission of the therapeutic molecules (like drugs, proteins, or DNA) to the organ/tissue of human body. Polymeric nanoparticles are mostly applied for therapeutic effectiveness in cancer therapy. The micro environment of tumor tissues in vessels can assist nanoparticles in achieving their anticipated accumulation. Poly (lactic acid)(PLA) is a novel green polymer with natural sources (like sweet potato and sugar cane). PLA is a linear aliphatic which has great sustainability, renewability and compostability. PLA has popper mechanical, thermal and barrier properties. This biomaterial is thermoplastic polyester with biocompatibility, non-toxicity and biodegradability. Various forms of PLA nanoparticles are synthetized for biomedical applications like cancer treatments and wound healing process. This review article introduces the various structures of polylactic acid nanoparticles used to deliver anticancer drugs. Furthermore, the investigational approaches that are considered for using PLA nanoparticles in treatment of different types of cancers will be reported briefly.

Cancer develops with unexpected mutations and causes death in many patients. Among the different cancer treatment strategies, immunotherapy is promising with the benefits of high specificity and accuracy, as well as modulating immune responses. Nanomaterials can be used to formulate drug delivery carriers for targeted cancer therapy. Polymeric nanoparticles used in the clinic are biocompatible and have excellent stability. They have the potential to improve therapeutic effects while significantly reducing off-target toxicity. This review classifies smart drug delivery systems based on their components. Synthetic smart polymers used in the pharmaceutical industry, including enzyme-responsive, pH-responsive, and redox-responsive polymers, are discussed. Natural polymers derived from plants, animals, microbes, and marine organisms can also be used to construct stimuli-responsive delivery systems with excellent biocompatibility, low toxicity, and biodegradability. The applications of smart or stimuli-responsive polymers in cancer immunotherapies are discussed in this systemic review. We summarize different delivery strategies and mechanisms that can be used in cancer immunotherapy and give examples of each case.

Alpha mangostin (AM) has potential anticancer properties for breast cancer. This study aims to assess the potential of chitosan nanoparticles coated with hyaluronic acid for the targeted delivery of AM (AM-CS/HA) against MCF-7 breast cancer cells. AM-CS/HA showed a spherical shape with an average diameter of 304 nm, a polydispersity index of 0.3, and a negative charge of 24.43 mV. High encapsulation efficiency (90%) and drug loading (8.5%) were achieved. AM released from AM-CS/HA at an acidic pH of 5.5 was higher than the physiological pH of 7.4 and showed sustained release. The cytotoxic effect of AM-CS/HA (IC50 4.37 µg/mL) on MCF-7 was significantly higher than AM nanoparticles without HA coating (AM-CS) (IC50 4.48 µg/mL) and AM (IC50 5.27 µg/mL). These findings suggest that AM-CS/HA enhances AM cytotoxicity and has potential applications for breast cancer therapy.

[Display omitted] Coenzyme Q 10 (CoQ 10) deficiency exhibits signs of multiple organ dysfunctions, particular subtypes present isolated kidney involvement progressing to chronic kidney disease. In these patients, early administration of oral CoQ 10 has been shown to decrease proteinuria and to delay development of chronic kidney disease, which suggests that it may have a renoprotective potential in these patients. However, CoQ 10 bioavailability in mitochondria is low, therefore its efficacy is limited. We aimed to develop mitochondria-targeted CoQ 10 loaded poly(lactic-co-glycolic acid)-poly(ethylene glycol)-triphenylphosphonium nanoparticles (CoQ 10 -TPP-NPs) that would be more efficient in the treatment of CoQ 10 nephropathies. These nanoparticles were found to have a size of approximately 150 nm and a zeta potential of + 20 mV. The entrapment efficiency of the nanoparticles was determined as 40%. Cytotoxicity studies showed no effect on the viability of the human kidney proximal tubule epithelial cells exposed to the nanoparticles. The efficacy of the formulated nanoparticles on in vitro disease model, which was developed in the human kidney proximal tubule epithelial cells by siRNA based silencing of the COQ8B , was evaluated through mitochondrial functions by means of metabolomic analyses. We showed that the treatment of COQ8B-/- cells with mitochondria-targeted nanoparticles was more effective in increasing the tricarboxylic acid cycle rate compared to free-CoQ 10. Our formulation would be more effective in treatment of CoQ 10 -related nephropathies than conventional formulations. [ABSTRACT FROM AUTHOR]

The design and development of side‐chain amino‐acid‐based polymeric nanostructures have attracted a significant research interest as they bring a remarkable revolution in various territories of the biomedical field. The incorporation of amino acid moieties into the side chain of synthetic polymeric scaffolds exhibits several beneficial properties like aqueous solubility, chiral recognition, high biocompatibility, stimuli responsiveness, antifouling properties, as well as their capability to form higher ordered self‐assembled architectures. Considering the important features and widespread applications of side‐chain amino‐acid‐containing polymers, here we shed light on the self‐assembled characteristics of side‐chain amino‐acid‐containing polymers and their implications. The primary aim of this review article is to highlight the recent achievements of this bright area of research. We describe the numerous aspects of side‐chain amino‐acid‐containing polymers focusing mainly on self‐assembly properties and the biomedical applications, which include drug and gene delivery, antimicrobial activity, antifouling coating, wound healing, tissue engineering etc. © 2021 Society of Industrial Chemistry. [ABSTRACT FROM AUTHOR]

To optimize the characteristics of stereocomplex polylactide-b-polyethylene glycol nanoparticles (SC-PEG NPs) in terms of pharmacokinetics (PK), we chose continuous anti-solvent precipitation with a T-junction as a preparation method and investigated the effect of using solvents containing an ion excipient (lithium bromide, LiBr) on the characteristics of SC-PEG NPs by changing the processing temperature and total flow rate (TFR). Processing temperatures above the melting temperature (Tm) of the PEG domain produced a sharper polydispersity and denser surface PEG densities of SC-PEG NPs than those produced by processing temperatures below the Tm of the PEG domains. Response surface analysis revealed that a higher LiBr concentration and slower TFR resulted in larger and denser hydrodynamic diameters (Dh) and surface PEG densities, respectively. However, a high concentration (300 mM) of LiBr resulted in a decreased drug loading content (DLC). 14C-tamoxifen-loaded 111In-SC-PEG NPs with larger Dh and denser surface PEG densities showed a prolonged plasma retention and low tissue distribution after intravenous injection in mice. These results indicate that the novel strategy of using solvents containing LiBr at different processing temperatures and TFR can broadly control characteristics of SC-PEG NPs, such as Dh, surface PEG densities, and DLC, which alter the PK profiles and tissue distributions. [ABSTRACT FROM AUTHOR]