Improving Bioavailability of Gallic Acid and Quercetin by Designing Polymeric Nanoparticle Formulation

Objective The pharmacokinetic properties of encapsulated polyherbal nanoparticles (Gallic acid and quercetin nanoparticle) and polyherbal extract (Amla and pomegranate fruit peels) in normal and DMH-induced colorectal cancer in rats was examined in this work. Method Polyherbal nanoparticles such as Gallic acid isolated from amla fruit and quercetin from pomegranate peel extract formulated into polymeric nanoparticle by using probe sonicator and high pressure homogenization. Result In normal and DMH-induced rats, a pharmacokinetic study demonstrated that polyherbal nanoparticles had a typical sustained release profile with a 2-fold increase in bioavailability when compared to polyherbal extract. Based on serum–concentration profiles of polyherbal nanoparticles and polyherbal extract following oral administration, the pharmacokinetic parameters for polyherbal nanoparticles and polyherbal extract were established using a single compartmental approach. Conclusion This research suggests that encapsulating gallic acid and quercetin in polymeric nanoparticles improves oral bioavailability than polyherbal extract of amla and pomegranate peel. Polymeric nanoparticles could be a novel therapeutic possibility for carcinogenesis prevention.

Polymeric Nanoparticles: Exploring the Current Drug Development and Therapeutic Insight of Breast Cancer Treatment and Recommendations

This manuscript aims to provide the latest update on polymeric nanoparticle drug delivery system for breast cancer treatment after 2015 and how research-oriented it is based on the available research data. Therefore, the authors have chosen breast cancer which is the most frequent and common reason for mortality in women worldwide. The first-line treatment for breast cancer treatment is chemotherapy, apart from surgery, radiation and hormonal therapy. Chemotherapy is associated with lesser therapeutics and undesirable side effects and hence. In addition, drug resistance affects the therapeutic dose to the target site. Although various nano-based formulations have been developed for effective treatment, the polymeric nanoparticles effectively avoid the lacunae of conventional chemotherapy. There has been an effort made to understand the chemotherapy drugs and their conventional formulation-related problems for better targeting and effective drug delivery for breast cancer treatment. Thus, the polymeric nanoparticles as a strategy overcome the associated problems with resulting dose reduction, enhanced bioavailability, reduced side effects, etc. This present review has compiled the research reports published from 2015 to 2021 from different databases, such as PubMed, Google Scholar, ScienceDirect, which are related to breast cancer treatment in which the drug delivery of numerous chemotherapeutic agents alone or in combination, including phytoconstituents formulated into various polymer-based nanoparticles.

Development, Characterization, and Evaluation of α-Mangostin-Loaded Polymeric Nanoparticle Gel for Topical Therapy in Skin Cancer

The aim of this study was to prepare and evaluate α-mangostin-loaded polymeric nanoparticle gel (α-MNG-PLGA) formulation to enhance α-mangostin delivery in an epidermal carcinoma. The poly (D, L-lactic-co-glycolic acid) (PLGA) nanoparticles (NPs) were developed using the emulsion–diffusion–evaporation technique with a 3-level 3-factor Box–Behnken design. The NPs were characterized and evaluated for particle size distribution, zeta potential (mV), drug release, and skin permeation. The formulated PLGA NPs were converted into a preformed carbopol gel base and were further evaluated for texture analysis, the cytotoxic effect of PLGA NPs against B16-F10 melanoma cells, and in vitro radical scavenging activity. The nanoscale particles were spherical, consistent, and average in size (168.06 ± 17.02 nm), with an entrapment efficiency (EE) of 84.26 ± 8.23% and a zeta potential of −25.3 ± 7.1 mV. Their drug release percentages in phosphate-buffered solution (PBS) at pH 7.4 and pH 6.5 were 87.07 ± 6.95% and 89.50 ± 9.50%, respectively. The release of α-MNG from NPs in vitro demonstrated that the biphasic release system, namely, immediate release in the initial phase, was accompanied by sustained drug release. The texture study of the developed α-MNG-PLGA NPs gel revealed its characteristics, including viscosity, hardness, consistency, and cohesiveness. The drug flux from α-MNG-PLGA NPs gel and α-MNG gel was 79.32 ± 7.91 and 16.88 ± 7.18 µg/cm2/h in 24 h, respectively. The confocal study showed that α-MNG-PLGA NPs penetrated up to 230.02 µm deep into the skin layer compared to 15.21 µm by dye solution. MTT assay and radical scavenging potential indicated that α-MNG-PLGA NPs gel had a significant cytotoxic effect and antioxidant effect compared to α-MNG gel (p < 0.05). Thus, using the developed α-MNG-PLGA in treating skin cancer could be a promising approach.

Validation UV Spectrophotometric Method to Determine Entrapment Efficiency of Ocular Polymeric Nanoparticle Levofloxacin Hemihydrate

Simple, easy, and economical UV spectrophotometric methods have been developed using simulated tear fluid (STF) solvent to determine levofloxacin hemihydrate (LEVH) levels in ocular nanoparticles, as indicated by the % entrapment efficiency. A maximum wavelength of levofloxacin at 288nm, with a 4.0-12.0µg/mL concentration, shows linear results with a correlation coefficient (r) of 0.9997 and an average % recovery of 99.920 –100.804%. The developed method is able to use for the analysis of levofloxacin hemihydrate in nanoparticle preparations.