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Objective: The study aimed at designing a pH sensitive Lipid polymeric Hybrid nanoparticle (LPHNP) for targeted release of Paclitaxel (PTX) and Curcumin (CUR) in breast cancer. Significance: Such systems shall result in controlled triggered release in acidic microenvironment of tumor cells with improved pharmacokinetic profile. Methods: Chitosan-coated CUR and PTX coloaded pH-sensitive LPHNPs were synthesized employing nanoprecipitation technique. The synthesized NPs were characterized in terms of particle size, polydispersity index (PDI), zeta potential, and morphology. Results: LPHNPs co-loaded with curcumin (CUR) and paclitaxel (PTX) were successfully formulated, achieving a size of 146 nm, a PDI of 0.18, and an entrapment efficiency exceeding 90%. In vitro release studies demonstrated controlled release of CUR and PTX under tumor pH conditions showing 1.6 fold and 1.7 fold higher release in ABS pH 5 in comparison to PBS 7.4 for PTX and CUR respectively. MTT-assay studies revealed enhanced cytotoxicity of CUR and PTX as LPHNPs showing IC50 value of free CUR & PTX 480.06 µg/mL decreasing to 282.97 µg/mL for CS-CUR-PTX-LPHNPs. In vivo pharmacokinetic evaluations in rats confirmed significantly improved bioavailability, with a 3.8-fold increase in AUC for CUR and a 6.6-fold increase for PTX. Additionally, the LPHNPs demonstrated controlled release and prolonged retention, evidenced by a 2.2-fold increase in the half-life (t1/2) of CUR and a 1.3-fold increase in the half-life of PTX. Conclusions: The results underscores potential of chitosan-coated LPHNP as a promising delivery platform, offering high drug loading, optimal size for cellular penetration, and prolonged blood circulation for cancer. [ABSTRACT FROM AUTHOR]

Objective: To obtain controlled release of captopril in the stomach, coated, mucoadhesive donut-shaped tablets were designed. Materials and methods: Donut-shaped tablet were made of different ratios of diluents to polymer or combination of polymers by direct compression method. Top and bottom portions of the tablet were coated with water-insoluble polymer followed by mucoadhesive coating. Time of water penetration, measurement of tensile strength, mucoadhesion studies (static ex vivo and ex vivo wash-off) were taken into account for characterization of respective films. In vitro study has been performed at different dissolution mediums. Optimized batches were also prepared by wet granulation. Stability studies of optimized batches have been performed. Results: The results of time of water penetration and tensile strength indicated positive response against water impermeation. Mucoadhesive studies showed that film thickness of 0.12 mm was good for retention of tablet at stomach. At pH 1.2, optimized batch of tablet made with hydroxypropyl methyl cellulose (HPMC) E15 as binder showed 80% w/w drug release within 4-5 h with maximum average release of 97.49% w/w. Similarly, maximum average releases of 96.36% w/w and 95.47% w/w were obtained with nearly same dissolution patterns using combination of HPMC E5 and HPMC E50 and sodium salt of carboxy methyl cellulose (NaCMC) 500-600 cPs instead of HPMC E15. The release profiles in the distilled water and pH 4.5 followed the above pattern except deviation at pH 6.8. Stability studies were not positive for all combinations. Conclusion: Coated, mucoadhesive donut-shaped tablet is good for controlled release of drug in the stomach. [ABSTRACT FROM AUTHOR]

AbstractResveratrol (Res), a potent nutraceutical, holds promise in ameliorating cancer and catalyzing breakthroughs in cancer therapy. Despite numerous preclinical studies on its anticancer activity, translational research progress remains limited. Poor pharmacokinetics and low potency are primary bottlenecks of Res therapy. In this study, we aimed to enhance the pharmacokinetic profile of Res in a rat model and assess its cytotoxicity against human ovarian cancer cells by developing Res loaded Nanostructured Lipid Carriers (Res-NLCs). The Res-NLCs were synthesized using the solvent injection method, featuring a size of 177 nm, a PDI of 0.25, and an entrapment efficiency exceeding 80%. The formulation exhibited stability for three months at 4 °C and 40 °C. Cytotoxicity assessments using the MTT assay and cellular uptake studies on human ovarian cancer cells (PA1 and SKOV3 luc) revealed significantly superior time-dependent cytotoxic effects and cellular accumulation of Res-NLCs compared to free Res. Pharmacokinetic studies of intravenously administered Res in NLCs demonstrated prolonged plasma levels of Res for at least 48 h. Remarkably, Res-NLCs exhibited approximately 15- and 5-fold improvements in AUC and elimination half-life (t1/2), respectively, compared to Res in solution in rats. Moreover, Res tissue distribution from Res-NLCs in rats showed significantly higher accumulation in the liver, lungs, and ovaries over 48 h, underscoring the potential for targeted therapy. In conclusion, NLCs effectively mitigated premature reduction of Res in the bloodstream, prolonged circulation period, and enhanced tissue accumulation. These findings suggest promising prospects for improving therapeutic outcomes in ovarian cancer therapy using Res-NLCs. [ABSTRACT FROM AUTHOR]

Over the past several years, treatment of infectious diseases and immunisation has undergone a revolutionary shift. With the advancement of biotechnology and genetic engineering, not only a large number of disease-specific biological have been developed, but also emphasis has been made to effectively deliver these biologicals. Niosomes are vesicles composed of non-ionic surfactants, which are biodegradable, relatively nontoxic, more stable and inexpensive, an alternative to liposomes. This article reviews the current deepening and widening of interest of niosomes in many scientific disciplines and, particularly its application in medicine. This article also presents an overview of the techniques of preparation of niosome, types of niosomes, characterisation and their applications.