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AbstractThe aim of study was to prepared and evaluated rutin-loaded solid-lipid-nanoparticles (Ru-SLNs) gel for treatment of melanoma cells. SLNs were prepared by ultrasonication method through optimisation and evaluated their mean-diameter, PDI, zeta-potential, morphology, entrapment-efficiency, drug-loading, interaction by FTIR, in vitro skin permeation, stability, antioxidant/MTT assay and fluorescence microscopic. Further developed Ru-SLNs was incorporated into gel and characterised their physicochemical properties, drug contents, in vitro diffusion, ex vivo permeation and retention studies in human cadaver skin. Optimised Ru-SLNs batch showed 556.4 ± 2.6 nm mean-diameter, −21.9 mV zeta-potential, 94.8 ± 04% entrapment-efficiency, 62.3 ± 29% loading, and 86.63% release after 6 hrs. MTT assay showed, Ru-SLNs have 15.37 times more effectiveness against melanoma cells, while fluorescence microscopy confirmed the cellular uptake over time. Gel based Ru-SLNs, have reduction in flux across skin, indicating a sustained release of rutin and higher retention within the deeper epidermis layer. Finally, Ru-SLNs based gel exhibited promising potential and effectively targeting to skin’s epidermal layer for melanoma cells. [ABSTRACT FROM AUTHOR]

Study was to develop a nanostructured-lipid-careers (NLCs) of paliperidone (PLP) for nose-to-brain targeting. NLCs was prepared by sonication, high-shear homogenisation method, and characterised their mean diameter, PDI, zeta-potential, morphology (by SEM, TEM and AFM), entrapment efficiency, drug loading, in vitro release, interaction study (by FTIR), and stability. Further, ex vivo permeation and ciliotoxicity performed in sheep nasal mucosa, and in vivo biodistribution/pharmacokinetic was performed in rats for schizophernia. Developed NLCs showed spherical and clearly 3-dimentinal structure with 129 ± 2.7 nm mean diameter, 0.304 ± 0.003 PDI, −7.61 ± 0.56 mV zeta-potential, 58.16 ± 0.17% entrapment efficiency, 65.8 ± 2% drug loading and 74.32 ± 0.003% release in 12 h, followed by Higuchi model. Ex vivo study showed NLCs have three times higher permeation, compare to pure drug (around 71.50.32% in 6 h) and 3.98 g/cm2/h steady sate flux. The blood/brain ratio given by intranasally have higher compare to IV route, and 94.53 ± 21.45% drug targeting efficiency in brain. In conclusion, NLCs have easily crossed BBB, higher drug delivery and effective for schizophrenia in given by intranasal. [ABSTRACT FROM AUTHOR]

Background: Voriconazole is an antifungal drug, which is classified under Bio-Classification System-II and has low water solubility (0.71 mg/mL) and high permeability. Hardly any endeavors have been made to increase the bioavailability of voriconazole. Objective: To develop and evaluate a solid SMEDDS (self-microemulsifying drug delivery system) for antifungal activity. Methods: Based on solubility studies of Labrafil-M 1994 CS (oil), Cremophor-RH 40 (a surfactant) and Transcutol-HP (a co-surfactant) were selected as components of the SMEDDS and a pseudo-ternary phase diagram was prepared. Thereafter, the oil, surfactant, and co-surfactant were mixed with altered weight ratios (1:1/1:2/2:1) and evaluated through various in vitro, in vivo analyses. Results: The particle size of the optimized formulation was observed to be 19.04 nm and the polydispersity index (PDI) value was found to be 0.162 with steady-state zeta potential. The optimized liquid SMEDDS was converted into a solid SMEDDS. Various adsorbents, such as Aerosil-200, Avicel-PH101, Neusilin-US2, and Neusilin UFL2 were screened to better detect the oil-absorbing capacity and flow properties of the powder. Neusilin UFL2 was selected as an adsorbent due to its better oil-absorbing capacity. DSC, X-ray diffraction, and dissolution studies were carried out to characterize the formulation. Further, the Pharmacokinetic profile was also studied in Wistar rats and the Cmax, tmax, and AUC0→t were calculated. The Cmax and AUC0→t plasma concentration is considerably better for the SMEDDS than for the pure drug and marketed formulation. Conclusions: This investigation clearly reveals the potential of developing a solid SMEDDS for candidiasis and invasive aspergillosis treatment, with better efficacy as compared to the commercially available marketed formulation. [ABSTRACT FROM AUTHOR]

AbstractPrimaquine (PQ) is a widely used antimalarial drug, but its high dosage requirements can lead to significant tissue damage and adverse gastrointestinal and hematological effects. Recent studies have shown that nanoformulations can enhance the bioavailability of pharmaceuticals, thereby increasing efficacy, reducing dosing frequency, and minimizing toxicity. In this study, PQ-loaded PLGA nanoparticles (PQ-NPs) were prepared using a modified double emulsion solvent evaporation technique (w/o/w). The PQ-NPs exhibited a mean particle size of 228 ± 2.6 nm, a zeta potential of +27.4 mV, and an encapsulation efficiency of 81.3 ± 3.5%. Scanning electron microscopy (SEM) confirmed their spherical morphology, and the in vitro release profile demonstrated continuous drug release over 72 h. Differential scanning calorimetry (DSC) thermograms indicated that the drug was present in the nanoparticles, with improved physical stability. Fourier-transform infrared spectroscopy (FTIR) analysis showed no interactions between the various substances in the NPs. In vivo studies in Swiss albino mice infected with Plasmodium berghei revealed that the nanoformulated PQ was 20% more effective than the standard oral dose. Biodistribution studies indicated that 80% of the NPs accumulated in the liver, highlighting their potential for targeted drug delivery. This research demonstrates the successful development of a nanomedicine delivery system for antimalarial drugs, offering a promising strategy to enhance treatment efficacy while reducing adverse effects. [ABSTRACT FROM AUTHOR]

The present work is focus on development of anti-psoriasis activity of Karanjin (isolated from Pongamia pinnata seed oil) loaded liposome based lotion for enhancement of skin permeation and retention. Karanjin was isolated using liquid-liquid extraction method and characterised by HPLC analysis and partition coefficient. Further, isolated Karanjin was loaded into liposomes using thin-film hydration technique and optimised by Box-Behnken design. Selected optimised batch was characterised their mean diameter, PDI, zeta potential, and entrapment efficiency, morphology (by TEM), FTIR and ex-vivo skin retention. Additionally, Karanjin loaded liposomes were formulated into lotion and characterise their rheological, spreadability, texture, ex-vivo skin permeation & retention, stability and anti-psoriatic activity in mouse tail model. The yield of Karanjin from seed oil was 0.1% w/v and have lipophilic nature. The optimised liposomal formulation showed 195 ± 1.8 nm mean diameter, 0.271 ± 0.02 PDI, −27.0 ± 2.1 mV zeta potential and 61.97 ± 2.5% EE. TEM image revel the spherical shap of liposome surrounded by single phospholipid bilayer and no interection between drug and excipients. Further, lotion was prepared by 0.1% w/v carbopol and found to 615 mPa.sec viscosity, good thixotropic behaviour, spreadability and texture. There was 22.44% increase in drug permeation for Karanjin loaded liposomal lotion compared to pure Karanjin lotion, confirm by ex-vivo permeation and retention. While, in-vivo study revel the liposomal lotion of Karanjin was found to have 16.09% higher drug activity then 5% w/w conventional Karanjin lotion. Karanjin loaded liposomal lotion have an effective anti-psoriatic agent and showed better skin permeation and retention than the conventional Karanjin lotion. [ABSTRACT FROM AUTHOR]

The knowledge base in the field of vaccination research and development has greatly improved. In the present era, utilizing a novel vaccine design and optimization strategy improves the vaccination efficiency and activity. In this regard, a novel drug delivery system produces nanosized, vaccine-loaded carrier molecules, which is called Nanovaccine. The advancement in nanovaccine and improved technology comes under preclinical and clinical trials, whereas different routes of administration strategy are applied against infectious diseases. The nanovaccine has high efficiency and immunogenicity compared to the traditional vaccine. Its long-lasting effect reduces the booster dose as well. One of the factors like routes of administration affects the efficiency of nanovaccine. The parenteral and mucosal vaccination is a traditional administration approach. In order to increase the safety and effectiveness of vaccines, innovative administration methods such as needless injection and polymeric formulations are now being developed. The presented paper shows a mechanism involved in nanovaccine delivery, and a method of administration via a different route, to learn more about their possible effects on immunogenicity, effectiveness, safety, sustained release and dose frequency reduction. The various advanced vaccine delivery methods, with special emphasis on its industrial and regulatory requirements for the higher production of nanovaccine, are also discussed. Illustrations of nanovaccine delivery systems overcoming barriers such as mucus layer and enzymatic degradation. Diagrams demonstrating the potential benefits of nanovaccines in enhancing immune response and providing targeted protection against pathogens. [ABSTRACT FROM AUTHOR]

Several therapeutic agents are used for controlling brain diseases, but they are not successfully reaching target sites due to the complex nature of the brain. Nasal administration as an alternate administration route has been proposed for brain targeting. To solve the above limitation linked to brain targeting through the transmission of nasal products, encourage the production of novel drug delivery by the combination of nanotechnology. The present review focuses on the latest understanding of pathways underlying central nervous system intranasal transmission. Novel Drug delivery systems as important methods for targeting the brain without toxicity in the nasal mucosa and central nervous system, they have acquired the capacity of CNS. [ABSTRACT FROM AUTHOR]

Aim: The goal of this study is to optimisation and evaluation of dopamine-loaded NLC (NLCDOPA) for achieve dopamine concentrations into brain for treatment of Parkinson's disease which causes progressive neuronal death. Method: NLC-DOPA prepared by homogenisation method using solid lipids (Cholesterol and Soya lecithin), liquid lipid (Oleic acid) and surfactant (Poloxamer-188) as major excipients, optimised by central composite design using design expert-13 software. The optimised formulations were characterised by particle size, zeta potential, entrapment efficiency, SEM, TEM, FTIR, DSC, XRD, stability study and in-vitro drug release. The histopathology of rat brain tissues and goat nasal tissues were performed. The ex-vivo (permeability and nasal ciliotoxicity study) and in vivo pharmacodynamics study were also accomplished to determine its efficacy and potency of NLC. Result: The NLC-DOPA formulations were optimised in particle size and (EE)% with range from 85.53 ± 0.703 to 106.11 ± 0.822 nm and 82.17 ± 0.794 to 95.45 ± 0.891%, respectively. The optimised formulation F11 showing best goodness-fitted model kinetic, followed by Korsmeyer- Peppas equation and zero order kinetic. The SEM and TEM confirmed the spherical and smooth morphology of formulation. FTIR and DSC spectra were given compatibility of compound and XRD diffractograms confirmed the amorphous nature. An ex-vivo study was showed the high permeability coefficient (6.67*1 0-4 cm/min, which is twice, compare to pure drug) and there was no damage in nasal mucosa, confirmed by the ciliotoxicity study. In-vivo study was shown significant effects of optimised NLC-DOPA on locomotor activity, force-swimming test and neurochemical assessment using rotenone induced Parkinson's model on Albino Wistar rats. Conclusion: NLC-DOPA was prepared and optimised successfully with increased bioavailability of drug from the NLC into brain with reduce toxicity in effective treatment of Parkinson's disease. [ABSTRACT FROM AUTHOR]

Berberine is an anticancer medication that generates side effects due to its hydrophobicity and low cellular promiscuity as well as high dose requirement. Thus, have to prepare PEGylated dendrimer conjugates which increases the targeting and release of chemotherapeutic drugs at the tumor site although falling the adverse side effects. The circulation time of drug is enhanced by PEGylation. It is the covalent attachment of PEG to therapeutic protein or any molecule. PEGylated berberine dendrimer was prepared by biotinylation cross linking method and characterized by particle size, zeta potential, entrapment efficiency, in vitro release and stability study. The Structure validation of berberine before and after grafting was confirmed by FTIR and NMR spectroscopy. Further prepared PEGylated complex were proceeded for the cellular uptake study in AMJ-13, and BT-20 cells line by fluorescent microscopy study and MTT assay cytotoxicity study in MCF-7 cell line. The prepared PEGylated formulation showed nanometric size, desired zeta potential, and 69.56 ± 23% entrapment efficiency. The prepared PEGylated particle showed 70.23% release at 72 h with good stability at 90 days. The cellular uptake of formulation was highly appreciable which is clearly observed in AMJ-13 and BT-20 cells line. In comparison to pure drug, developed formulation has 10.8 M high efficiency for breast cancer cell line. PEGylation is easy and reasonable way, as it requires lesser time and is proved to be superior technique for treatment of cancer. [ABSTRACT FROM AUTHOR]

Background: Trigonella foenum-graecum L (Fenugreek) is an annual herb, mainly cultivated for its seed as well as for its sprouts. Pharmacological investigations reported anti-bacterial, anti-diabetic, anti-cancer, anti-diarrheal, anti-hypercholesteremic, and antiinflammatory activities of Trigonella foenum-graecum L. Aim: The purpose of this study was to accentuate on formulation of granules and investigate the effect of germinated Trigonella foenum-graecum L. (TFG) granules in Diabetes mellitus (DM) rats induced by streptozotocin as fenugreek retains hypoglycemic property. Materials and Methods: Granules of germinated TFG powder were arranged by means of several excipients comprising diverse amounts of super disintegrants by (wet) granulation method and proceed for the solid dosage form evaluation. Further, in-vivo study was performed in STZ induced DM Wister rats for four weeks. TFG granules 1600mg/kg and Glibenclamide 0.45 mg/kg (as a positive control for comparison) were orally administrated and evaluate the diabetics in rats. Results: All evaluation parameter are correct: as in standard tablet. The STZ (Streptozotocin) induced rats the treatment with the Drug (Glibenclamide) and TFG granules significantly lowered the blood plasma glucose levels by 36% (mean ± SD glucose 120 ± 0.6 mg/dL ( p < 0.001)) and 38% (mean ± SD glucose 114 ± 0.4 mg/dL; p < 0.001) respectively after 4 weeks of treatment when compared to T2DM (Type 2 Diabetes mellitus) rats. Conclusion: Experimental studies had shown that bioactive compounds found in Trigonella Foenum graceum herb have potential to cure diabetes especially due to the presence of unique chemical constituent including trigonelline, galactomannan and amino acid 4-hydroxy isoleucine. These findings suggested that TFG granules may be an alternative medicine for the management of DM. [ABSTRACT FROM AUTHOR]

The study was to extend systemic circulation and biological half-life (t1/2) of trans-resveratrol (RSV) using solid lipid nanoparticles (RSV-SLN) to improve its anti-cancer potential. RSV-SLN was prepared by solvent emulsification evaporation technique and proceeded for evaluation like particle size, PDI, zeta potential, in vitro release, in vitro cytotoxicity, cellular internalisation, haemolysis and erythrocyte membrane integrity, platelet aggregation and pharmacokinetic studies in rats. Moreover, cancer cells accumulation of RSV-SLN also needs to be evaluated for proving their targeting ability. Prepared SLN showed 126.85 ± 12.09 nm particle size, −24.23 ± 3.27 mV Zeta potential and 74.67 ± 4.76%. release at 48 h and haemocompatible. The cellular internalisation image showed the SLN reach in a cytoplasm and nucleus of PC3 prostate cells. RSV-SLN exhibited high t1/2 (8.22 ± 1.36 h) and 7.19 ± 0.69 h MRT (Mean residence time) and lower clearance i.e. 286.42 ± 13.64 mL/min/kg. The bio-distribution of RSV-SLN was found to be extremely high in prostate cells and accumulate 7.56 times greater than that of RSV solution. The developed RSV-SLN can be applied as potential carrier for delivery of drug of chemotherapeutics at an extend systemic circulation and targeting efficiency at tumour site. [ABSTRACT FROM AUTHOR]

The research focussed on development and evaluation of ethosome as an effective delivery of antigen that eliminates need for frequent dose of antigen while improving patient compliance for Hepatitis B. Prepared a single dose HBsAg ethosomal vaccine using a cold method and applied a central composite design optimisation using particles size, zeta potential and entrapment efficiency as dependent variables. Further, selected batch was assessed for their morphology, in vitro release, interaction, haemocompatibility, histological (ex vivo skin permeation) and stability studies. Further, proceeded for in-vivo study, administered in BALB/c mice via nasal route to check the immunological activity and compared with single and multiple doses of ethosome to booster doses of alum-HBsAg vaccine. Immunological marker like immunoglobulin (IgG and IgA) and cytokines (interleukin-2 and interferon-Y) were measured by ELISA techniques. The prepared ethosome showed minimum particle size (93.98 ± 4.6), 15.0 ± 2.83 mV zeta potential, with maximum entrapment efficiency (66.25 ± 8.6%). Physicochemical characterisation reveal the sustained release, haemocampatibile, and stable nature of ethosome. Further, ex-vivo skin permeation showed safely administration of drug by nasal route without toxicity. The in vivo study, found the higher immunological response observed in BALB/c mice, compare to alum-HBsAg vaccine. The single dose of ethosome showed sufficient effective and measurable immunoglobulin and cytokines levels. A single dose of ethosome is sufficient for the complete immunological response not require booster administration. The potency of ethosomes have to produce a protective immune response, as well as their ability to explore and target the immunological environment through nasal route. [ABSTRACT FROM AUTHOR]

The current study focussed on the development and evaluation of aqueous core nanocapsules (ACNs) as an effective carrier to deliver an optimal synergistic combination of a highly water-soluble Vinorelbine bitartrate (VRL) and a poorly water-soluble Resveratrol (RES) for treatment of breast cancer. Various molar ratios of VRL to RES were screened against MCF-7 cell lines to determine the synergistic effects using the Chou-Talalay method. The synergistic ratio of therapeutic agents was then incorporated into aqueous core nanocapsules utilising a double emulsion solvent evaporation technique to yield dual drug-loaded nanocapsules (dd-ACNs). The dd-ACNs were optimised using Box-Behnken design and characterised for physicochemical parameters such as particle size, zeta potential, polydispersity index, total drug content and encapsulation efficiency, surface morphology, drug excipient compatibility by FTIR and DSC, release kinetics, toxicity studies and anticancer efficacy (in-vitro and in-vivo). Results demonstrated that the combination exhibited maximum synergy when higher doses of VRL were combined with smaller doses of RES (1:1, 5:1, and 10:1). The dual drug-loaded ACNs were found to be stable and depicted a core-shell structure, narrow size range (150.2 ± 3.2 nm) with enhanced encapsulation (80% for VRL and 99% for RES). Moreover, the dd-ACNs were 5 times more efficacious in-vitro than a combination of free drugs, while reducing systemic toxicity. Also, pre-clinical evaluation of dd-ACNs also depicted a drastic reduction of tumour volume as compared tp pristine VRL and a physical combination of drugs. The developed dd-ACNs can be applied as a potential carrier for delivery of a combination of chemotherapeutics at a synergistic ratio at the tumour site. [ABSTRACT FROM AUTHOR]

This work studies the development and evaluation of Gymnema sylvestre (GYM) extract loaded sustained release polymeric nanoparticles (PNPs) for enhanced bioavailability and reduced nephrotoxicity. The current therapy is associated with the drawbacks of addiction and repeated administration. The sustained release PNPs were developed and evaluated for toxicity. PNPs of GYM were prepared by double emulsion solvent evaporation technique utilising Taguchi model and evaluated for physicochemical properties (particle size, zeta potential, entrapment efficiency), in vitro drug release, compatibility, and stability. Further, the bioavailability and in vivo nephrotoxicity studies in diabetic rat model were also carried out. The developed optimised nanoparticles were 205.7 ± 1.20 nm in size, −40.68 mV zeta potential, compatible, and stable in nature with improved entrapment efficiency (67.1 ± 0.2%) and sustained release. Moreover, nanoparticles were found to lower the blood glucose level in single as well as multiple doses. Results of in vivo study indicated that GYM-NPs increased the phosphorylase activity and thus enhanced insulin secretion. Furthermore, the nanoparticles were free from toxicity, which was confirmed by the estimation of kidney biomarker. The nanoparticles increased the bioavailability of GYM extract and have a great potential for the treatment of diabetes in reduced dose, and so these can be potential candidates for treating diabetes. [ABSTRACT FROM AUTHOR]

Migraine is a frequent neurological condition characterized by throbbing headaches, nausea, photophobia, and phonophobia, among other symptoms. Sumatriptan belongs to a BCS class III, which exhibits poor oral bioavailability and several side-effects. The objective of the present study was to develop solid lipid nanoparticles (SLNPs) of sumatriptan succinate for brain targeting by nasal route. Solvent injection method was used to increase the entrapment efficiency of hydrophilic drug. Thus, formulation was optimized by central composite design with minimum particle size, optimized zeta potential, and maximum entrapment efficiency, which was found to be 133.4 nm, −17.7 mV, and 75.5%, respectively. Optimized batch was further evaluated for surface morphology, Fourier-transform infrared spectroscopy, in vitro release, permeation across nasal mucosa, and histopathology. It was seen that most of the particles were spherical in shape as confirmed by scanning electron microscopy and transmission electron microscopy. The release of drug through the lipid showed initial burst release followed by sustained release up to 12 h. The ex vivo diffusion study using goat nasal mucosa at pH 6.8 revealed that SLNPs permeation across nasal mucosa was quick, which was sufficient for brain targeting. Histopathology studies further revealed integrity of nasal mucosa after treatment with SLNPs. The investigation indicated that hydrophilic drug, sumatriptan succinate can be successfully entrapped in SLNPs to target brain via nasal delivery, and thus it could be an effective approach for nose-to-brain delivery. [ABSTRACT FROM AUTHOR]

Background: Atorvastatin Calcium (ATC) used for lowering the cholesterol levels in body. It is competitive inhibitor of hydroxyl methylglutaryl-coenzyme A (HMG-CoA) reductase, followed mevalonate pathway, which have low bioavailability and poor solubility. Present work focus on development of mucoadhesive microspheres of atorvastatin calcium, for improve the delayed transit, continuous longer period release and preclinical pharmacokinetic estimation in rabbit. Materials and Methods: Microsphere was prepared by emulsification method in which the independent variables (like polymer amount) were studied on critical quality attributes like entrapment efficiency, percentage yield and in-vitro release. Microspheres were characterized in terms of physicochemical parameters, micromeritic properties, FT-IR, DSC and mucoadhesive wash-off test and further, evaluated for their pharmacokinetics study in rabbits. Results: The designed microsphere exhibited an average size with smooth surface, negative zeta potential, maximum entrapment efficiency and sustained release. Microspheres fulfil the micromeritic properties and showed no any interaction between drug and polymer, confirmed by FT-IR and DSC. The in-vivo study demonstrated that the prepared microspheres are effective for colon targeted drug delivery system at longer duration. In pharmacokinetics study, relatively steady plasma drug concentrations were observed within after oral administration of drug. The AUC0-24h for formulation were significantly higher than that of pure drug (p<0.05). Conclusion: The pre-clinical oral bioavailability study of drug was increased as the relative availability values were high compared with pure drug and it showed delayed transit for longer period of time. [ABSTRACT FROM AUTHOR]

PEGylation is the covalent addition of PEG to one more molecule. PEGylation can improve the maintenance time of the therapeutics similar to proteins, liposomes, and nanoparticle through shielding them beside different debasing mechanisms dynamic in a body that improve beneficial properties. This skill is used to get better half-life and other pharmaceutical properties of a protein, peptide, or non-peptide molecule. Polyethylene glycol is harmless, non-immunogenic, non-antigenic, and extremely soluble in water and FDA accepted polymer. It shows a significant role in drug delivery. A variety of PEG-based formulations are available in the market. This paper represents the benefits of PEGylation over non-PEGylated products. Now a day, PEGylation plays an important role in the drug delivery system. PEGylation increases the therapeutic potential of drugs. [ABSTRACT FROM AUTHOR]

Background: Irbesartan is hypertensive drugs approved for high blood pressure and protect the kidneys damage due to diabetes. It is an angiotensin receptor blockers, belongs to BCS class II, exhibit low and variable oral bioavailability due to its poor aqueous solubility. Therefore, it is need to enhancement of dissolution rate and bioavailability. The objective of this study was to develop a transdermal patches system of Irbesartan to reduce the above drawback. Methods: Various batch of Irbesartan loaded transdermal patches were prepared by the solvent extraction method employing HPMC and ethyl cellulose as polymer in presence or absence of eudragit. Physicochemical characterization of patches was done by thickness, weight variation, folding endurance, drug content, moisture uptake and loss. The drug interaction was carried out by FTIR spectroscopy. Further, patches were evaluated their in-vitro drug release, ex-vivo permeation study in Franz diffusion cell. While in-vivo skin irritation and toxicity study performed in Wistar rats. Results: The final batch was selected on the basis of physicochemical characteristics and proceeds for further studies FTIR result indicates that there is no interaction between drug and polymer. The in-vitro release study showed that 93.54% of drugs released at 48 hr and steady-state flux was found to be 0.35±3.23 µg/cm2/h. the developed patch were free from edema and hypersensitivity reaction which is confirm by in-vivo study. Conclusion: Patches were successfully prepared and their evaluation of excellent quality and uniformity. This can be the potential for therapeutic application due to reduced dosing frequency, improve patient compliance and bioavailability. [ABSTRACT FROM AUTHOR]

Chronic Hepatitis B Virus (HBV) infections are severe with weak antiviral immune responses. The lack of an appropriate small animal model for chronic hepatitis, a major hurdle for studying the immunotolerance and immunopathogenesis induced by hepatitis B viral (HBV) infection. In this study, for enhancing the antibody production efficiency the prepared polymeric HBsAg-loaded nanoparticles (nanovaccine) will be tested in immune-deficit mice, which suffer from chronic Hepatitis B virus. Vaccination of Balb/c mice by this prepared nanoparticles that were engrafted with peripheral blood mononuclear cells (PBMCs), which was already lethally irradiated and transplanted by the bone marrow of NOD (knockout mice) mice. In the present study, after the vaccination detected the high frequencies of immunoglobulin G (IgG)-secreting B cells and mitogen-responsive interferon-Y (IFN-Y) secreting T cells in serum, determined by specific ELISA technique. During the entire observation period, unvaccinated animals showed lower concentration of specific IgG secreting B cells and IFN-Y secreting T cells found in comparison to vaccinated mice group. Chronic HBV carrier PBMCs transplanted into the chimera failed to produce antigen and increased the antibodies production due to vaccination. Furthermore, another advantage was that the viral gene expression and viral DNA replication was no longer observed in vaccinated group. This prepared nanovaccine formulations is better for the cure of Hepatitis B viral infection carrier. Therefore, specific memory responses were elicited by vaccination with Hepatitis B virus surface (HBsAg) antigen of chimeric mice transplanted with PBMCs derived from HBV donors. [ABSTRACT FROM AUTHOR]

Research on thiazole derivatives has been a popular topic in medicine and one of the most active fields in heterocyclic chemistry. Pharmacological and industrial researchers have been studying thiazole-containing derivatives in great detail because they have a lot of biological uses. These compounds are one of the best examples of a five-membered heterocyclic compound that has a lot of potential and has had a lot of success in recent decades. Investigating viable hybrid designs utilizing thiazole is critical for the development of new anti-tuberculosis medications. This article offers a thorough overview of the latest advancements in thiazole-containing hybrids, offering potential therapeutic applications as anti-TB drugs. We also discussed the structure-activity correlations (SAR) of the powerful thiazole moiety and its several functional groups, along with a few potential molecular targets., Competing Interests: Declaration of competing interest The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper., (Copyright © 2024 Elsevier Inc. All rights reserved.)

Background: Epilepsy is a critically deep-rooted CNS disorder affecting above 50 million people all over the world. Thus, a safe and effective treatment that proves its worth in this ailment is urgently needed. Thiazolidine-4-ones possess the molecules to be used as anticonvulsants. The thiazolidinedione is a cyclic analogue of thiosemicarbazides and thioureas as well as a (bio)isostere of hydantoin (imidazolidine-2,4-dione), which are recognized as novel anticonvulsant designs., Aim: This study aimed to develop and evaluate a novel thiazolidine-4-one derivative by three-component condensation in one pot reaction method., Methods: A novel thiazolidine-4-one derivative was formulated by three-component condensation. The selected OH (Alcohol) derivatives were found to be more potent; hence, a molecular docking study against a selected target LGI1 LRR domain was performed. Various analytical tests like FTIR and H1 NMR were accomplished. The FTIR was used to validate the existence of multiple functional moieties like C-S, O-H, C=O, C-N, N=O, C-NH, C-O in the wave region from 3075 cm-1 - 1236 cm-1 and H1 NMR was employed to ascertain if the synthesized analogues had the complete set of protons. Then, the anti-seizure activity of the selected compound was examined using PTZ models in mice at three successive doses, i.e., 25, 50, and 100mg/kg, and compared with standard ethosuximide., Results: The docking simulations were initiated using PyMOL after the binding site was determined and the receptor and ligand were suitably prepared. It showed higher binding frequency in comparison to the standard marketed drug Ethosuximide. FTIR and H1 NMR spectroscopy were used to characterize the chemical components. Numerous functional groups, including O-H (alcohol), C=O (ketones), N=O, C-NH, C-N, C-S, and C-O bending stretching, were visible in the synthesized molecule accordingly. The synthesized compound was effective in inhibiting the convulsions at the concentration of 100 mg/kg., Conclusion: The novel thiazolidine-4-one derivative showed promising activity and could be considered for further investigation and dosage form preparation., (Copyright© Bentham Science Publishers; For any queries, please email at epub@benthamscience.net.)

Breast Cancer stands on the second position in the world in being common and women happen to have it with high rate of about five-folds around the world. The causes of occurrence can matter with different humans be it external factors or the internal genetic ones. Breast cancer is primarily driven by mutations in the BRCA1 and BRCA2 susceptibility genes. These BC susceptibility genes encode proteins critical for DNA homologous recombination repair (HRR). Poly (ADP ribose) polymerases (PARP) are the essential enzymes involved in the repairing of the damaged DNA. So the inhibition of these inhibitors can be considered as the promising strategy for targeting cancers with defective damage in the deoxyribonucleic acid. Olaparib and talazoparib are PARP inhibitors (PARPi) are being employed for the monotherapies in case of the deleterious germline HER2-negative and BRCA-mutated breast cancer. The potency of PARP for trapping on DNA and causes cytotoxicity may have difference in the safety and efficacy with the PARPi. The PARPi have been found its place in the all different types of Breast Cancers and have shown potential benefits. The purpose of this review is to provide an update on the oral poly(ADP-ribose) polymerase (PARP)inhibitors for the improvement in the treatment and management of Breast Cancer., (Copyright© Bentham Science Publishers; For any queries, please email at epub@benthamscience.net.)

Parkinson's disease (PD) is a complex neurological condition caused due to inheritance, environment, and behavior among various other parameters. The onset, diagnosis, course of therapy, and future of PD are thoroughly examined in this comprehensive review. This review also insights into pathogenic mechanisms of reactive microgliosis, Lewy bodies, and their functions in the evolution of PD. It addresses interaction complexity with genetic mutations, especially in genes such as UCH-L1, parkin, and α-synuclein, which illuminates changes in the manner dopaminergic cells handle proteins and use proteases. One of the emerging therapeutic routes that are being investigated is neuroprotective medicines that aim to prevent the aggregation of α-synuclein and interventions that modify the progression of diseases. The review concludes by stressing the dynamic nature of PD research and the potential game-changing impact of precision medicines on current approaches to therapy. This raises the improved outcomes and life quality for those with PD. Potential treatments for severe PD include new surgical methods like Deep Brain Stimulation (DBS). Further, exploration of non-motor manifestations, such as cognitive impairment, autonomic dysfunction, and others, is covered in this review article. These symptoms have a significant impact on patients' quality of life. One of the emerging therapeutic routes that are being investigated is neuroprotective medicines that aim to prevent the aggregation of α-synuclein and interventions that modify the progression of diseases. The review concludes by stressing the dynamic nature of PD research and the potential game-changing impact of precision medicines on current approaches to therapy., (Copyright© Bentham Science Publishers; For any queries, please email at epub@benthamscience.net.)

More than two hundred million people around the world are infected with malaria, a blood-borne disease that poses a significant risk to human life. Single medications, such as lumefantrine, primaquine, and chloroquine, as well as combinations of these medications with artemisinin or its derivatives, are currently being used as therapies. In addition, due to rising antimalarial drug resistance, other therapeutic options are needed immediately. Furthermore, due to anti-malarial medication failures, a new drug is required. Medication discovery and development are costly and time-consuming. Many malaria treatments have been developed however, most treatments have low water solubility and bioavailability. They may also cause drug-resistant parasites, which would increase malaria cases and fatalities. Nanotechnology may offer a safer, more effective malaria therapy and control option. Nanoparticles' high loading capacity, concentrated drug delivery, biocompatibility, and low toxicity make them an attractive alternative to traditional therapy. Nanotechnology-based anti-malarial chemotherapeutic medications outperform conventional therapies in therapeutic benefits, safety, and cost. This improves patient treatment compliance. The limitations of malaria treatments and the importance of nanotechnological approaches to the treatment of malaria were also topics that were covered in this review. The most recent advancements in nanomaterials and the advantages they offer in terms of medication delivery are discussed in this article. The prospective therapy for malaria is also discussed. Additionally, the limitations of malaria therapies and the importance of nanotechnology-based approaches to the treatment of malaria were explored., (Copyright© Bentham Science Publishers; For any queries, please email at epub@benthamscience.net.)

Solid Lipid Nanocarriers (SLNs) offer a promising avenue for breast cancer treatment, a disease that accounts for 12.5% of global cancer cases. Despite strides in combined therapies (surgery, chemotherapy, radiation, and endocrine therapy), challenges like systemic toxicity, drug resistance, and adverse effects persist. The manuscript offers several novel contributions to the field of breast cancer treatment through the use of SLNs, and these are innovative drug delivery systems, multifunctionality, and biocompatibility, the potential to overcome drug resistance, integration with emerging therapies, focus on personalized medicine, ongoing and future research directions and potential for reduced side effects. SLNs present a novel strategy due to their unique physicochemical properties. They can encapsulate both hydrophilic and hydrophobic drugs, ensuring controlled release and targeted delivery, thus enhancing solubility and bioavailability and reducing side effects. The multifunctional nature of SLNs improves drug delivery while their biocompatibility supports their potential in cancer therapy. Challenges for pharmacists include maintaining stability, effective drug loading, and timed delivery. Combining SLNs with emerging therapies like gene and immunotherapy holds promise for more effective breast cancer treatments. SLNs represent a significant advancement, providing precise drug delivery and fewer side effects, with the potential for overcoming drug resistance. Ongoing research will refine SLNs for breast cancer therapy, targeting cells with minimal side effects and integrating with other treatments for comprehensive approaches. Advances in nanotechnology and personalized medicine will tailor SLNs to specific breast cancer subtypes, enhancing effectiveness. Clinical trials and new treatment developments are crucial for realizing SLNs' full potential in breast cancer care. In conclusion, SLNs offer a transformative approach to breast cancer treatment, addressing issues of drug delivery and side effects. Ongoing research aims to optimize SLNs for targeted therapy, potentially revolutionizing breast cancer care and providing hope for patients., (Copyright© Bentham Science Publishers; For any queries, please email at epub@benthamscience.net.)

Berberine is an anticancer medication that generates side effects due to its hydrophobicity and low cellular promiscuity as well as high dose requirement. Thus, have to prepare PEGylated dendrimer conjugates which increases the targeting and release of chemotherapeutic drugs at the tumor site although falling the adverse side effects. The circulation time of drug is enhanced by PEGylation. It is the covalent attachment of PEG to therapeutic protein or any molecule. PEGylated berberine dendrimer was prepared by biotinylation cross linking method and characterized by particle size, zeta potential, entrapment efficiency, in vitro release and stability study. The Structure validation of berberine before and after grafting was confirmed by FTIR and NMR spectroscopy. Further prepared PEGylated complex were proceeded for the cellular uptake study in AMJ-13, and BT-20 cells line by fluorescent microscopy study and MTT assay cytotoxicity study in MCF-7 cell line. The prepared PEGylated formulation showed nanometric size, desired zeta potential, and 69.56 ± 23% entrapment efficiency. The prepared PEGylated particle showed 70.23% release at 72 h with good stability at 90 days. The cellular uptake of formulation was highly appreciable which is clearly observed in AMJ-13 and BT-20 cells line. In comparison to pure drug, developed formulation has 10.8 M high efficiency for breast cancer cell line. PEGylation is easy and reasonable way, as it requires lesser time and is proved to be superior technique for treatment of cancer.

COVID-19, caused by the SARS-CoV-2 virus, has been expanding. SARS-CoV caused an outbreak in early 2000, while MERS-CoV had a similar expansion of illness in early 2010. Nanotechnology has been employed for nasal delivery of drugs to conquer a variety of challenges that emerge during mucosal administration. The role of nanotechnology is highly relevant to counter this "virus" nano enemy. This technique directs the safe and effective distribution of accessible therapeutic choices using tailored nanocarriers, as well as the interruption of virion assembly, by preventing the early contact of viral spike glycoprotein with host cell surface receptors. This study summarises what we know about earlier SARS-CoV and MERS-CoV illnesses, with the goal of better understanding the recently discovered SARS-CoV-2 virus. It also explains the progress made so far in creating COVID-19 vaccines/ treatments using existing methods. Furthermore, we studied nanotechnology- based vaccinations and therapeutic medications that are now undergoing clinical trials and other alternatives., (Copyright© Bentham Science Publishers; For any queries, please email at epub@benthamscience.net.)

Coronavirus disease 2019 is a global pandemic, particularly affecting individuals with pre-existing lung conditions and potentially leading to pulmonary fibrosis. Age and healthcare system limitations further amplify susceptibility to both diseases, especially in low- and middle-income countries. The intricate relationship between Coronavirus disease 2019 and lung cancer highlights their clinical implications and the potential for early detection through biosensor techniques involving hedgehog and mucin signaling. This study highlights the connection between Coronavirus disease 2019 and lung cancer, focusing on the mucosa, angiotensin- altering enzyme 2 receptors, and their impact on the immune system. It details the inflammatory mechanisms triggered by Coronavirus disease 2019, which can result in pulmonary fibrosis and influence the cancer microenvironment. Various cytokines like Interleukins-6 and Tumor Necrosis Factor-alpha are examined for their roles in both diseases. Moreover, the review delves into the Hedgehog signaling pathways and their significance in lung cancer, particularly their influence on embryonic cell proliferation and tissue integrity. Mucin signaling is another vital aspect, highlighting the diverse mucin expression patterns in respiratory epithelial tissues and their potential as biomarkers. The review concludes with insights into diagnostic imaging techniques like chest computed tomography, Positron Emission Tomography and Computed Tomography, and Magnetic Resonance Imaging for early lung cancer detection, emphasizing the crucial role of biosensors in identifying specific biomarkers for early disease detection. This review provides a comprehensive overview of the clinical impact of Coronavirus disease 2019 on lung cancer patients and the potential for biosensors utilizing hedgehog and mucin signaling for early detection. It underscores the ongoing need for research and innovation to address these critical healthcare challenges., (Copyright© Bentham Science Publishers; For any queries, please email at epub@benthamscience.net.)

Contemporary medical research increasingly focuses on the blood-brain barrier (BBB) to maintain homeostasis in healthy individuals and provide solutions for neurological disorders, including brain cancer. Specialized in vitro modules replicate the BBB's complex structure and signalling using micro-engineered perfusion devices and advanced 3D cell cultures, thus advancing the understanding of neuropharmacology. This research explores nanoparticle-based biomolecular engineering for precise control, targeting, and transport of theranostic payloads across the BBB using nanorobots. The review summarizes case studies on delivering therapeutics for brain tumors and neurological disorders, such as Alzheimer's, Parkinson's, and multiple sclerosis. It also examines the advantages and disadvantages of nano-robotics. In conclusion, integrating machine learning and AI with robotics aims to develop safe nanorobots capable of interacting with the BBB without adverse effects. This comprehensive review is valuable for extensive analysis and is of great significance to healthcare professionals, engineers specializing in robotics, chemists, and bioengineers involved in pharmaceutical development and neurological research, emphasizing transdisciplinary approaches., (Copyright© Bentham Science Publishers; For any queries, please email at epub@benthamscience.net.)

The mucosal surfaces are the key site of the entrance, protection, and stability of several pathogens. Considering that >90% of pathogens gain access to the body via mucosal sites, using mucosal vaccination to generate protective immunity at mucosal sites could overcome. Some of the micro and nano carrier-based nasal delivery systems produce cellular, humoral and mucosal immunity. The nasal route vaccination may protect multiple distant mucosal sites like-rectal, vaginal, oral, and pulmonary. Also, it is a convenient and cost-effective vaccination mode with improved patient compliance. Several nasal vaccine delivery systems are currently being supplied in the form of liposomes, micro/nano particulates, which have shown immunity in animal models. Especially particulate nanovaccine has a special character related to long-term immunogenicity and high efficiency. The significance and the ability of the nasal route vaccination programs are unexplained and complications; therefore, effective delivery strategies will promote the production of nasal vaccines. The present study focuses on vaccine delivery strategies and their effects on the immune system. Also, the study discusses the benefits of mucosal-associated immune response over the conventional delivery system for vaccine via the nasal route., (Copyright© Bentham Science Publishers; For any queries, please email at epub@benthamscience.net.)

Background: The pathogenesis of hepatic diseases involves several cells, which complicates the delivery of pharmaceutical agents. Many severe liver diseases affecting the worldwide population cannot be effectively treated. Major hindrances or challenges are natural physiological barriers and non-specific targeting of drugs administered, leading to inefficient treatment. Hence, there is an earnest need to look for novel therapeutic strategies to overcome these hindrances. A kind of literature has reported that drug safety and efficacy are incredibly raised when a drug is incorporated inside or attached to a polymeric material of either hydrophilic or lipophilic nature. This has driven the dynamic investigation for developing novel biodegradable materials, drug delivery carriers, target-specific drug delivery systems, and many other novel approaches., Objective: Present review is devoted to summarizing receptor-based liver cell targeting using different modified novel synthetic drug delivery carriers. It also highlights recent progress in drug targeting to diseased liver mediated by various receptors, including asialoglycoprotein, mannose and galactose receptor, Fc receptor, low-density lipoprotein, glycyrrhetinic, and bile acid receptor. The essential consideration is given to treating liver cancer targeting using nanoparticulate systems, proteins, viral and non-viral vectors, homing peptides and gene delivery., Conclusion: Receptors based targeting approach is one such approach that was explored by researchers to develop novel formulations which can ensure site-specific drug delivery. Several receptors are on the surfaces of liver cells, which are highly overexpressed in various disease conditions. They all are helpful for the treatment of liver cancer., (Copyright© Bentham Science Publishers; For any queries, please email at epub@benthamscience.net.)

Nanotechnology provides an excellent platform for the development of a new generation of vaccines. These are based on purified subunit proteins or polysaccharides, recombinant proteins, synthetic peptides, or nucleic acids. These types of vaccines may be insufficiently immunogenic, thus requiring adjuvants that augment their immunogenicity. Nanoparticles (NPs) can act as adjuvants for vaccines, hence they are referred to as a nano-adjuvant (NA). NPs can either encapsulate or adsorb the vaccine antigen or DNA in an appropriate formulation, thus increasing stability, cellular uptake, and immunogenicity. In addition, the biodistribution and systemic release of a vaccine can also be controlled by different NA formulations. This review provides an overview of the classification of NAs and also addresses factors influencing the stability, release, and immunogenicity of the formulated vaccine. A basic understanding of these factors enables a more rational design of NA formulations. Applications of NAs and key challenges in their formulation development are also discussed.

Background: Vinorelbine bitartrate (VRL) is an antimitotic agent approved by FDA for breast cancer and non-small cell lung cancer (NSCLC) in many countries. However, high aqueous solubility and thermo degradable nature of VRL limited the availability of marketed dosage forms., Objectives: The current work is focused on the development of lipid based aqueous core nanocapsules which can encapsulate the hydrophilic VRL in the aqueous core of nanocapsules protected with a lipidic shell which will further provide a sustained release., Methods: The ACNs were prepared by double emulsification technique followed by solvent evaporation. Box Behnken Design was utilized to optimize the formulation and process variables. Thirteen batches were generated utilizing lipid concentration, surfactant concentration and homogenizer speed as dependent variables (at three levels) and particle size and encapsulation efficiency as critical quality attributes. The ACNs were characterized for particle size, zeta potential, polydispersity index (PDI), entrapment efficiency, morphology by Transmission Electron Microscopy (TEM) and in vitro release. The ACNs were further evaluated for safety against intravenous administration by haemocompatibility studies., Results: Results demonstrated that lipidic nanocapsules enhanced the entrapment efficiency of VRL up to 78%. Transmission Electron Microscopy revealed spherical shape of ACNs with core-shell structure. The GMS-VRL-ACNs showed that release followed Korsemeyer peppas kinetics suggesting Fickian diffusion. Moreover, the compliance towards haemocompatibility studies depicted the safety of prepared nanocapsules against intravenous administration., Conclusion: ACNs were found to be promising in encapsulating high aqueous soluble anticancer drugs with enhanced entrapment and safety towards intravenous administration., (Copyright© Bentham Science Publishers; For any queries, please email at epub@benthamscience.org.)