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Abstract: Several factors exist that limit the efficacy of lung cancer treatment. These may be tumor-specific delivery of therapeutics, airway geometry, humidity, clearance mechanisms, presence of lung diseases, and therapy against tumor cell resistance. Advancements in drug delivery using nanotechnology based multifunctional nanocarriers, have emerged as a viable method for treating lung cancer with more efficacy and fewer adverse effects. This review does a thorough and critical examination of effective nano-enabled approaches for lung cancer treatment, such as nano-assisted drug delivery systems. In addition, to therapeutic effectiveness, researchers have been working to determine several strategies to produce nanotherapeutics by adjusting the size, drug loading, transport, and retention. Personalized lung tumor therapies using sophisticated nano modalities have the potential to provide great therapeutic advantages based on individual unique genetic markers and disease profiles. Overall, this review provides comprehensive information on newer nanotechnological prospects for improving the management of apoptosis in lung cancer.

Cancer is one of the major health-related issues affecting the population worldwide and subsequently accounts for the second-largest death. Genetic and epigenetic modifications in oncogenes or tumor suppressor genes affect the regulatory systems that lead to the initiation and progression of cancer. Conventional methods, including chemotherapy/radiotherapy/appropriate combinational therapy and surgery, are being widely used for theranostics of cancer patients. Surgery is useful in treating localized tumors, but it is ineffective in treating metastatic tumors, which spread to other organs and result in a high recurrence rate and death. Also, the therapeutic application of free drugs is related to substantial issues such as poor absorption, solubility, bioavailability, high degradation rate, short shelf-life, and low therapeutic index. Therefore, these issues can be sorted out using nano lipid-based carriers (NLBCs) as promising drug delivery carriers. Still, at most, they fail to achieve site-targeted drug delivery and detection. This can be achieved by selecting a specific ligand/antibody for its cognate receptor molecule expressed on the surface of the cancer cells. In this review, we have mainly discussed the various types of ligands used to decorate NLBCs. A list of the ligands used to design nanocarriers to target malignant cells has been extensively undertaken. The approved ligand-decorated lipid-based nanomedicines with their clinical status have been explained in tabulated form to provide a wider scope to the readers regarding ligand-coupled NLBCs.

On the basis of the boron neutron capture therapy (BNCT) modality, we have designed and synthesized a zinc gallate (ZnGa

In 2023, the world is facing problems such as global warming, hazardous chemicals, non-destructible plasticizers, similar to viruses. All of these issues are major concerns for our environment. To address these issues, there is a strong need for a multifunctional material that serves as a catalyst, which is stable, efficient, selective, and reusable. The conventional catalyst based on photoinduced charge carriers is insufficient. The intrinsic properties of a material, such as ferroelectricity, piezoelectricity, and magnetism, can play a role in the catalysis process and enhance the catalyst's activity by driving forces such as spontaneous polarization, piezoelectric coefficient, and ferromagnetism at room temperature. These qualities are found and cherished in the classic ceramic semiconductor Bismuth Ferrite (BiFeO3; BFO), commonly known as the "The drosophila of multiferroics." BFO exhibits ferroic orderings at room temperature. For catalytic purposes, a large surface area is required to have a high number of active sites. Therefore, nanosized BFO particles are chosen. Although BFO nanoparticles (NPs) absorb visible light, they have smaller ferroelectric polarization than bulk BFO due to reduced crystal asymmetry, and they also possess weak ferromagnetic properties. To achieve a larger surface area while maintaining increased ferroelectric and magnetic properties, ionic engineering at Bi and Fe sites is utilized. The dopants not only further reduce the particle size of BFO NPs but also influence the shape of NPs, resulting in different morphologies. The macroscopic and local crystal structure of doped BFO NPs is examined using several techniques. The alteration in Bi-O and Fe-O bond parameters and the increase in microstrain of the BFO crystal structure due to doping are major factors responsible for altered ferroic properties. Doping magnetic ions at the Fe site of BFO NPs leads to an increase in total magnetization mainly through superexchange interaction, disrupting the spin cycloid. Further co-doping at the Bi site results in even higher magnetization due to changes in the Fe-O-Fe bond angle and the presence of uncompensated spins on the surface of small-sized NPs. Doping also influences the coercive field and anisotropy of the NPs, making them suitable for magnetic hyperthermia. Doped BFO NPs exhibit efficiency in converting magnetic energy into heat when exposed to an alternating magnetic field, showing promise for applications in magnetic hyperthermia for cancer treatment. The local ferroelectricity and piezoelectric response in doped BFO NPs are found to be higher than in pristine BFO NPs due to crystal structure distortion caused by asymmetrical Bi-O bonds in the BiO12 cuboctahedron and resulting alterations in the FeO6 octahedron. Doping Mn at the Fe site does not significantly influence the ferroelectricity of BFO NPs. However, further doping of divalent cations (Ca2+ or Ba2+) at the Bi site in BiFe0.95Mn0.05O3 (BFM) NPs reduces the local ferroelectricity, while doping of trivalent (Dy3+) and monovalent (Ag+) cations into BFM NPs increases the ferroelectric properties of BFM NPs approximately three times. This study finds that single doping at the Fe site has a substantial influence on the band gap compared to doping at the Bi site, primarily due to the indirect effect on the electronic structure of BFO NPs. The band gap of BFO, which is 2.2 eV, can be reduced to 1.6 eV with the appropriate ratio of Ba and Mn co-doping. This provides the maximum utilization of the solar spectrum to generate photoinduced charge carriers for catalytic purposes. Dopants at the Bi site have a slight impact on the light absorption properties of the BFO NPs, creating oxygen vacancies or defect states in the band gap. The catalytic activity of the doped BFO NPs for the degradation of organic pollutants under visible and UV light illumination is compared. Ba-doped BFM NPs exhibit enhanced photocatalytic efficiency compared to pristine BFM and BFO NPs. 1 mol% Ba-doped BFM NPs degrade rhodamine B and methyl orange dyes within 60 and 25 minutes under UV and visible illumination, respectively. The increased photocatalytic efficiency in Ba-doped BFM NPs is attributed to a cooperative effect of factors such as increased light absorption ability, large surface area, active surface, reduced recombination of charge carriers, and spontaneous polarization to mitigate photoinduced charge carrier recombination. In piezo-photocatalysis, Dy-BFM and Ag-BFM NPs show the best photocatalytic activity under ultrasonication conditions. The increase in spontaneous polarization by mono- and trivalent doping is one of the major factors in enhancing the photocatalytic performance, along with stronger light absorption in the visible range, low recombination rate of charge carriers, and larger surface area of NPs. Dibutyl phthalate (DBP) is notorious as an endocrine disruptor, making it a significant threat to both human health and the environment. Successful photodegradation of DBP is achieved under UV light irradiation within 2.5 hours using Ag-doped BFM NPs supported on graphene oxide (GO) nanosheets. Gas chromatography and mass spectrometry (GCMS) show that Ag-BFM NPs supported on GO have a higher photodegradation efficiency than the pristine free-standing BFO NPs alone. The photodegradation process of DBP generates various intermediate products, such as phthalic acid, benzoic acid, benzaldehyde, and 3-methyl butyric acid, before achieving complete mineralization into carbon dioxide and water. The investigation delves into the functionality exhibited by doped BFM NPs concerning the hydrogen evolution reaction (HER). The electrocatalytic activity of BFM NPs undergoes a transformative shift as a consequence of mono-, di-, and trivalent cation substitutions. Notably, strategic engineering of doping at the Bi site within BFM NPs yields a remarkable outcome, namely the reduction of the kinetic overpotential prerequisite for HER. This diminished overpotential in doped BFM NPs arises from the confluence of multifarious factors: diminished charge transfer resistance, augmented specific surface area, a discernible distribution of pore sizes ranging from narrow to broad, particles endowed with a shape boasting abundant active facets, and the integration of dopants as novel active sites upon the surface. Furthermore, the presence of surface defects, oxygen vacancies, and amplified microstrain within doped BFM NPs contributes to the reduced overpotential. This study underscores the successful synthesis of phase-pure doped and undoped BFO NPs with diverse morphologies using different methods and the profound impact of doping on their magnetic, electrical, optical, and catalytic properties. The findings highlight the tremendous multifunctional potential of doped BFO NPs in a wide range of applications. These doped BFM NPs encapsulate immense potential to revolutionize the realm of HER in the photoelectrochemical domain, owing to their profound light absorption capabilities and aptitude for catalysis. Dissertation, Universität Duisburg-Essen, 2023

Brain, a subtle organ of multifarious nature presents plethora of physiological, metabolic and bio-chemical convolutions that impede the delivery of biomolecules and thereby resulting in truncated therapeutic outcome in pathological conditions of central nervous system (CNS). The absolute bottleneck in the therapeutic management of such devastating CNS ailments is the BBB. Another pitfall is the lack of efficient technological platforms (due to high cost and low approval rates) as well as limited clinical trials (due to failures of neuro‑leads in late-stage pipelines) for CNS disorders which has become a literal brain drain with poorest success rates compared to other therapeutic areas, owing to time consuming processes, tremendous convolutions and conceivable adverse effects. With the advent of intranasal delivery (via direct N2B or indirect nose to blood to brain), several novel drug delivery carriers viz. unmodified or surface modified nanoparticle based carriers, lipid based colloidal nanocarriers and drysolid/liquid/semisolid nanoformulations or delivery platforms have been designed as a means to deliver therapeutic agents (small and large molecules, peptides and proteins, genes) to brain, bypassing BBB for disorders such as Alzheimer's disease (AD), Parkinson's disease (PD), epilepsy, schizophrenia and CNS malignancies primarily glioblastomas. Intranasal application offers drug delivery through both direct and indirect pathways for the peripherally administered psychopharmacological agents to CNS. This route could also be exploited for the repurposing of conventional drugs for new therapeutic uses. The limited clinical translation of intranasal formulations has been primarily due to existence of barriers of mucociliary clearance in the nasal cavity, enzyme degradation and low permeability of the nasal epithelium. The present review literature aims to decipher the new paradigms of nano therapeutic systems employed for specific N2B drug delivery of CNS drugs through in silico complexation studies using rationally chosen mucoadhesive polymers (exhibiting unique physicochemical properties of nanocarrier's i.e. surface modification, prolonging retention time in the nasal cavity, improving penetration ability, and promoting brain specific delivery with biorecognitive ligands) via molecular docking simulations. Further, the review intends to delineate the feats and fallacies associated with N2B delivery approaches by understanding the physiological/anatomical considerations via decoding the intranasal drug delivery pathways or critical factors such as rationale and mechanism of excipients, affecting the permeability of CNS drugs through nasal mucosa as well as better efficacy in terms of brain targeting, brain bioavailability and time to reach the brain. Additionally, extensive emphasis has also been laid on the innovative formulations under preclinical investigation along with their assessment by means of in vitro /ex vivo/in vivo N2B models and current characterization techniques predisposing an efficient intranasal delivery of therapeutics. A critical appraisal of novel technologies, intranasal products or medical devices available commercially has also been presented. Finally, it could be warranted that more reminiscent pharmacokinetic/pharmacodynamic relationships or validated computational models are mandated to obtain effective screening of molecular architecture of drug-polymer-mucin complexes for clinical translation of N2B therapeutic systems from bench to bedside.

For the past few years, there has been a surge in the use of nutraceuticals. The global nutraceuticals market in 2020 was USD 417.66 billion, and the market value is expected to increase by 8.9% compound annual growth rate from 2020 to 2028. This is because nutraceuticals are used to treat and prevent various diseases such as cancer, skin disorders, gastrointestinal, ophthalmic, diabetes, obesity, and central nervous system-related diseases. Nutritious food provides the required amount of nutrition to the human body through diet, whereas most of the bioactive agents present in the nutrients are highly lipophilic, with low aqueous solubility leading to poor dissolution and oral bioavailability. Also, the nutraceuticals like curcumin, carotenoids, anthocyanins, omega-3 fatty acids, vitamins C, vitamin B12, and quercetin have limitations such as poor solubility, chemical instability, bitter taste, and an unpleasant odor. Additionally, the presence of gastrointestinal (GIT) membrane barriers, varied pH, and reaction with GIT enzymes cause the degradation of some of the nutraceuticals. Nanotechnology-based nutrient delivery systems can be used to improve oral bioavailability by increasing nutraceutical stability in foods and GIT, increasing nutraceutical solubility in intestinal fluids, and decreasing first-pass metabolism in the gut and liver. This article has compiled the properties and applications of various nanocarriers such as polymeric nanoparticles, micelles, liposomes, niosomes, solid lipid nanocarriers, nanostructured lipid carrier, microemulsion, nanoemulsion, dendrimers in organic nanoparticles, and nanocomposites for effective delivery of bioactive molecules.

In the recent years, herbal medicines have gained worldwide attention of peoples and researchers due to their esthetic value, more patient’s compliance and prominent therapeutic effects. Novel drug delivery systems for delivery of herbal drugs possesses several advantages over conventional formulations. It includes enhancement of solubility, bioavailability, and protection from toxicity, etc. The herbal drugs can be used in a more upright course with enhanced efficacy by incorporating them into suitable dosage forms. This can be achieved by designing novel drug delivery systems for such drugs. Such systems are polymeric nanoparticles, nanocapsules, phytosomes, animations, microsphere, etc. The present article highlights the current condition of the development of novel herbal formulations and summarizes their type of active components, biological activity, and applications of novel formulations.

The ferroelectricity of multivalent codoped Bismuth ferrite (BiFeO3; BFO) nanoparticles (NPs) is revealed and utilized for photocatalysis, exploiting their narrow electronic bandgap. The photocatalytic activity of ferroelectric photocatalysts BiFe0.95Mn0.05O3 (BFM) NPs and mono‐, di‐, or tri‐valent cations (Ag+, Ca2+, Dy3+; MDT) coincorporated BFM NPs are studied under ultrasonication and in acidic conditions. It is found that such doping enhances the photocatalytic activity of the ferroelectric NPs approximately three times. The correlation of the photocatalytic activity with structural, optical, and electrical properties of the doped NPs is established. The increase of spontaneous polarization by the mono‐ and tri‐valent doping is one of the major factors in enhancing the photocatalytic performance along with other factors such as stronger light absorption in the visible range, low recombination rate of charge carriers, and larger surface area of NPs. A‐site doping of BFO NPs by divalent elements suppresses the polarization, whereas trivalent (Dy3+) and monovalent (Ag+) cations provide an increase of polarization. The depolarization field in these single domain NPs acts as a driving force to mitigate recombination of the photoinduced charge carriers., The ferroelectricity of Ag/Ca/Dy‐doped BiFe0.95Mn0.05O3 nanoparticles are utilized for photocatalysis under ultrasonic conditions. The mitigated recombination of photoinduced charge‐carriers in the nanoparticles due to the depolarization field, is one of the important factors for the photocatalytic rate. The piezoresponse becomes a crucial parameter under ultrasonic conditions for ferroelectric photocatalysts. The pink dye (rhodamine B) is photodegraded using MDT doped nanoparticles. The ease of photoinduced charge carrier separation in single domain nanoparticles using the depolarization field as a driving force is shown. image

The rapid advancement of nanomedicine presents novel alternatives that have the potential to transform health care. Targeted drug delivery as well as the synthesis of nanocarriers is a growing discipline that has been intensively researched to reduce the complexity of present medicines in a variety of diseases and to develop new treatment and diagnostic techniques. There are several designed nanomaterials used as a delivery system such as liposomes, micelles, dendrimers, polymers, carbon-based materials, and many other substances, which deliver the drug moiety directly into its targeted body area reducing toxic effect of conventional drug delivery, thus reducing the amount of drug required for therapeutic efficacy and offering many more advantages. Currently, these are used in many applications, including cancer treatment, imaging contrast agents, and biomarker detection and so on. This review provides a comprehensive update in the field of targeted nano-based drug delivery systems, by conducting a thorough examination of the drug synthesis, types, targets, and application of nanomedicines in improving the therapeutic efficiency.

Anomalies in brain insulin signaling have been demonstrated to be involved in the pathology of Alzheimer disease (AD). In this context, the neuroprotective efficacy of an insulin sensitizer, rosiglitazone, has been confirmed in our previous study. In the present study, we hypothesize that a combination of an epigenetic modulator, vorinostat, along with rosiglitazone can impart improved gene expression of neurotrophic factors and attenuate biochemical and cellular alteration associated with AD mainly by loading these drugs in a surface modified nanocarrier system for enhanced bioavailability and enhanced therapeutic efficacy. Hence, in this study, rosiglitazone and vorinostat were loaded onto a poloxamer stabilized polymeric nanocarrier system and administered to mice in the intracerebroventricular streptozotocin (3 mg/kg) induced model of AD. Treatment with the free drug combination (rosiglitazone 5 mg/kg, vorinostat 25 mg/kg) for 3 weeks attenuated the behavioral, biochemical, and cellular alterations as compared to either treatment alone (rosiglitazone 10 mg/kg, vorinostat 50 mg/kg). Further, the coencapsulated nanoformulation (rosiglitazone 5 mg/kg, vorinostat 25 mg/kg) exerted better neuroprotective efficacy than the free drug combination as evidenced by improved behavioral outcome, reduced oxidative stress, and elevated levels of neurotrophic factors. In conclusion, the synergistic neuroprotective efficacy of rosiglitazone and vorinostat has been increased through the poloxamer stabilized polymeric nanocarrier system.

Antimicrobial-resistant (AMR) bacterial infections remain a significant public health concern. The situation is exacerbated by the rapid development of bacterial resistance to currently available antimicrobials. Metal nanoparticles represent a new perspective in treating AMR due to their unique mechanisms, such as disrupting bacterial cell membrane potential and integrity, biofilm inhibition, reactive oxygen species (ROS) formation, enhancing host immune responses, and inhibiting RNA and protein synthesis by inducing intracellular processes. Metal nanoparticles (MNPs) properties such as size, shape, surface functionalization, surface charges, and co-encapsulated drug delivery capability all play a role in determining their potential against multidrug-resistant bacterial infections. Silver, gold, zinc oxide, selenium, copper, cobalt, and iron oxide nanoparticles have recently been studied extensively against multidrug-resistant bacterial infections. This review aims to provide insight into the size, shape, surface properties, and co-encapsulation of various MNPs in managing multidrug-resistant bacterial infections.

The present study aimed to investigate the brain targeting efficacy of Lamotrigine (LTG) loaded PLGA nanoparticles (LTG-PNPs) upon intranasal administration. LTG-PNPs were fabricated through the emulsification-solvent evaporation technique and evaluated for % Entrapment efficiency, particle size, in-vitro release, surface morphology, crystallinity, ex-vivo permeation & thermal behaviour. Biodistribution, gamma scintigraphy, and pharmacodynamic studies were performed in BALB/c mice, New Zealand rabbits, and Wistar rats respectively. LTG-PNPs exhibited % EE 71%; particle size 170.0 nm; Polydispersity index 0.191; zeta potential -16.60 mV. LTG-PNPs exhibited a biphasic release pattern. Biodistribution and gamma scintigraphy studies proved a greater amount of LTG in the brain following intranasal delivery of LTG-PNPs in comparison to LTG-SOL. Pharmacodynamic studies demonstrated delayed seizure onset time with LTG-PNPs in comparison to LTG-SOL. Intranasal administration of LTG-PNPs provided prolonged release, higher bioavailability, and better brain targeting bypassing the BBB. The developed formulation could be administered as a once-a-day formulation that would reduce the dosing frequency; dose; dose-related side effects; cost of the therapy and would be beneficial in the management of epilepsy as compared to the LTG-SOL. However, the proof of concept generated through these studies needs to be further validated in higher animals and human volunteers.

Background: Skin diseases affect all the age groups of people and have an impact on patients’ physical, mental, and emotional status. Conventional topical preparation is limited with its efficacy due to low permeation, frequent application, and poor adherence to the therapy for prolong time. Objective: The objective of this review article is to address the emerging trends of nanotechnology derived lipidic carrier systems for an effective treatment for skin disorders. Methodology: Various research and review articles from reputed international journals were referred and compiled. Results and Discussion: opical drug delivery systems were found to be more effective than oral and parenteral drug delivery systems for treating skin diseases due to targeted localized applications with reduced side effects. Lipid-based nanoparticles have been found to have the potential in treating skin diseases due to the biocompatibility and the versatility of the lipids. Nanostructured lipid carriers (NLCs) have gained much attention in treating skin diseases due to improved stability of the drugs, enhanced skin permeation, retention, and better therapeutic efficacy. The review summarizes the NLCs characteristics and their application for topical delivery of various therapeutics in skin disorders. NLCs have shown great potential in effective drug delivery for the treatment of psoriasis, dermatitis, bacterial infections, and skin cancer. Its cosmetic application has opened a new area for skincare. Furthermore, safety and clinical status revealed its future commercial acceptability. Conclusion: NLCs have been found as effective lipid nanocarriers for the delivery of topical therapeutics.

Exclusively red-emitting upconversion nanoparticles (UCNPs) with the composition NaErF

Although radiation therapy (RT) is one of the mainstays of head and neck cancer (HNC) treatment, innovative approaches are needed to further improve treatment outcomes. A significant challenge has been to design delivery strategies that focus high doses of radiation on the tumor tissue while minimizing damage to surrounding structures. In the last decade, there has been increasing interest in harnessing high atomic number materials (Z-elements) as nanoparticle radiosensitizers that can also be specifically directed to the tumor bed. Metallic nanoparticles typically display chemical inertness in cellular and subcellular systems but serve as significant radioenhancers for synergistic tumor cell killing in the presence of ionizing radiation. In this review, we discuss the current research and therapeutic efficacy of metal nanoparticle (MNP)-based radiosensitizers, specifically in the treatment of HNC with an emphasis on gold- (AuNPs), gadolinium- (AGdIX), and silver- (Ag) based nanoparticles together with the metallic oxide-based hafnium (Hf), zinc (ZnO) and iron (SPION) nanoparticles. Both in vitro and in vivo systems for different ionizing radiations including photons and protons were reviewed. Finally, the current status of preclinical and clinical studies using MNP-enhanced radiation therapy is discussed.

Theranostics has the potential to revolutionize the diagnosis, treatment, and prognosis of cancer, where novel drug delivery systems could be used to detect the disease at an early stage with instantaneous treatment. Various preclinical approaches of nanoemulsions with entrapped contrast and chemotherapeutic agents have been documented to act specifically on the tumor microenvironment (TME) for both diagnostic and therapeutic purposes. However, bringing these theranostic nanoemulsions through preclinical trials to patients requires several fundamental hurdles to be overcome, including the in vivo behavior of the delivery tool, degradation, and clearance from the system, as well as long-term toxicities. Here, we discuss recent advances in the application of nanoemulsions in molecular imaging with simultaneous therapeutic efficacy in a single delivery system.

In last two decades, the lipid nanocarriers have been extensively investigated for their drug targeting efficiency towards the critical areas of the human body like CNS, cardiac region, tumor cells, etc. Owing to the flexibility and biocompatibility, the lipid-based nanocarriers, including nanoemulsion, liposomes, SLN, NLC etc. have gained much attention among various other nanocarrier systems for brain targeting of bioactives. Across different lipid nanocarriers, NLC remains to be the safest, stable, biocompatible and cost-effective drug carrier system with high encapsulation efficiency. Drug delivery to the brain always remains a challenging issue for scientists due to the complex structure and various barrier mechanisms surrounding the brain. The application of a suitable nanocarrier system and the use of any alternative route of drug administration like nose-to-brain drug delivery could overcome the hurdle and improves the therapeutic efficiency of CNS acting drugs thereof. NLC, a second-generation lipid nanocarrier, upsurges the drug permeation across the BBB due to its unique structural properties. The biocompatible lipid matrix and nano-size make it an ideal drug carrier for brain targeting. It offers many advantages over other drug carrier systems, including ease of manufacturing and scale-up to industrial level, higher drug targeting, high drug loading, control drug release, compatibility with a wide range of drug substances, non-toxic and non-irritant behavior. This review highlights recent progresses towards the development of NLC for brain targeting of bioactives with particular reference to its surface modifications, formulations aspects, pharmacokinetic behavior and efficacy towards the treatment of various neurological disorders like AD, PD, schizophrenia, epilepsy, brain cancer, CNS infection (viral and fungal), multiple sclerosis, cerebral ischemia, and cerebral malaria. This work describes in detail the role and application of NLC, along with its different fabrication techniques and associated limitations. Specific emphasis is given to compile a summary and graphical data on the area explored by scientists and researchers worldwide towards the treatment of neurological disorders with or without NLC. The article also highlights a brief insight into two prime approaches for brain targeting, including drug delivery across BBB and direct nose-to-brain drug delivery along with the current global status of specific neurological disorders.

Temozolomide is a drug approved for treating glioblastomas, which has 100% oral bioavailability but gets degraded at physiological pH thus having very short half-life and only 20-30% brain bioavailability. Due to its amphiphilic nature, reported nanoformulations exhibits poor drug loading. The objective of this work was to formulate lipid-based drug delivery systems to enhance the brain bioavailability by prolonging the drug release and circulation time of the drug to overcome the limitations of the existing therapies and possible reduction of side effects. The size of the nanocarriers obtained was less than 300 nm and the PDI obtained was less than 0.3. The designed formulation showed higher entrapment efficiency as compared to the other reported nanocarriers of temozolomide. The designed formulations showed prolonged drug release from 12 to 20 h compared to 6 h for the pure drug. About 95% of the pure drug was degraded at plasma pH at the end of 12 h, whereas only 68% and 77% was degraded when entrapped inside the lipid crystal nanoparticles and proliposomes respectively. Further, pharmacokinetic and animal studies can confirm the potential of these for improvement of brain bioavailability.

Alzheimer's disease (AD) is a progressive neurodegenerative disorder associated with memory and cognitive impairment. Donepezil is an acetylcholinesterase inhibitor used for the symptomatic treatment of AD. However, high dose of donepezil is prescribed to achieve effective concentration in the brain, which leads to significant side effects, gastrointestinal alterations, and hepatotoxicity. In the present study, ApoE3 conjugated polymeric nanoparticles derived from diblock copolymer methoxy poly(ethylene glycol)-polycaprolactone (mPEG-PCL) have been used to boost the delivery of donepezil to the brain. mPEG-PCL is an amphiphilic diblock polymer with a tendency to avoid nanoparticle uptake by phagocytic cells in the liver and can significantly reduce the gastric mucosal irritations. Moreover, ApoE3-based nanocarriers showed a promising ability to enhance brain uptake, binding to amyloid beta with high affinity and accelerating its clearance. Donepezil-loaded polymeric nanoparticles were performed by using a nanoprecipitation method and further surface modified with polysorbate 80 and ApoE3 to increase the brain bioavailability and reduce the dose. Optimization of various process parameters were performed using quality by design approach. ApoE3 polymeric nanoparticles were found to be stable in simulated gastric fluids and exhibited a sustained drug release pattern. Cellular uptake studies confirmed better neuronal uptake of the developed formulation, which is further corroborated with pharmacokinetic and biodistribution studies. Orally administered ApoE3 polymeric nanoparticles resulted in significantly higher brain donepezil levels after 24 h (84.97 ± 11.54 ng/mg tissue) as compared to the pure drug (not detected), suggesting a significant role of surface coating. Together, these findings are promising and offer preclinical evidence for better brain availability of donepezil by oral administration.

As per the WHO, every year around 2.1 million women are detected with breast cancer. It is one of the most invasive cancer in women and second most among all, contributing around 15% of death worldwide. The available anticancer therapies including chemo, radio, and hormone therapy are associated with a high load of reversible and irreversible adverse effects, limited therapeutic efficacy, and low chances of quality survival. To minimize the side effects, improving therapeutic potency and patient compliance promising targeted therapies are highly desirable. In this sequence, various nanocarriers and target modified systems have been explored by researchers throughout the world. Among these chitosan-based nanocarriers offers one of the most interesting, flexible, and biocompatible systems. The unique characteristics of chitosan like surface flexibility, biocompatibility, hydrophilicity, non-toxic and cost-effective behavior assist to overcome the inadequacy of existing therapy. The present review throws light on the successes, failures, and current status of chitosan modified novel techniques for tumor targeting of bioactives. It also emphasizes the molecular classification of breast cancer and current clinical development of novel therapies. The review compiles most relevant works of the past 10 years focusing on the application of chitosan-based nanocarrier against breast cancer.