Formulation, optimization, hemocompatibility and pharmacokinetic evaluation of PLGA nanoparticles containing paclitaxel.

OBJECTIVE: Paclitaxel (PTX)-loaded polymer (Poly(lactic-co-glycolic acid), PLGA)-based nanoformulation was developed with the objective of formulating cremophor EL-free nanoformulation intended for intravenous use. SIGNIFICANCE: The polymeric PTX nanoparticles free from the cremophor EL will help in eliminating the shortcomings of the existing delivery system as cremophor EL causes serious allergic reactions to the subjects after intravenous use. METHODS AND RESULTS: Paclitaxel-loaded nanoparticles were formulated by nanoprecipitation method. The diminutive nanoparticles (143.2 nm) with uniform size throughout (polydispersity index, 0.115) and high entrapment efficiency (95.34%) were obtained by employing the Box-Behnken design for the optimization of the formulation with the aid of desirability approach-based numerical optimization technique. Optimized levels for each factor viz. polymer concentration (X1), amount of organic solvent (X2), and surfactant concentration (X3) were 0.23%, 5 ml %, and 1.13%, respectively. The results of the hemocompatibility studies confirmed the safety of PLGA-based nanoparticles for intravenous administration. Pharmacokinetic evaluations confirmed the longer retention of PTX in systemic circulation. CONCLUSION: In a nutshell, the developed polymeric nanoparticle formulation of PTX precludes the inadequacy of existing PTX formulation and can be considered as superior alternative carrier system of the same.

Natural Products-based Drugs: Potential Drug Targets Against Neurological Degeneration.

Phytochemicals or natural products have been studied extensively for their potential in the treatment of neurodegenerative diseases (NDs) like Parkinson's disease, Alzheimer's disease, etc. The neuronal structure loss and progressive dysfunction are the main characteristics of these diseases. In spite of impressive and thorough knowledge of neurodegenerative molecular pathways, little advancement has been found in the treatment of the same. Moreover, it was proved that natural products can be used efficiently in the treatment of NDs while certain issues regarding the patient's safety and clinical data are still existing. As ND is a bunch of diseases and it will start the myriad of pathological processes, active targeting of the molecular pathway behind ND will be the most efficient strategy to treat all ND-related diseases. The targeting pathway must prevent cell death and should restore the damaged neurons. In the treatment of ND and related diseases, natural products are playing the role of neuroprotective agents. This review will target the therapeutic potential of various phytochemicals which shows neuroprotective action.

Formulation and Characterization of Genistein-loaded Nanostructured Lipid Carriers: Pharmacokinetic, Biodistribution and In vitro Cytotoxicity Studies.

BACKGROUND: Genistein (Gen) is a naturally occurring soy isoflavonoid, possessing anticancer, antiproliferation & antioxidant-like properties. The disadvantage of poor solubility and less oral bioavailability restrict its use as a potential anticancer agent. OBJECTIVES: The current work was focused on the formulation and characterization of the genistein loaded nanostructured lipid carriers that can entrap enough quantity of the drug which will provide sustained release of the drug for the treatment of ovarian cancer. METHODS: The nanostructure lipid carriers of genistein were developed with the aid of solvent emulsification and evaporation technique by employing TPGS as a surfactant. The resultant formulation was characterized by various physicochemical properties. Pharmacokinetics and biodistribution studies were carried out to estimate the mean plasma concentrations of the drug. Percentage cytotoxicity was evaluated by using PA-1 ovarian cancer cell lines. RESULTS: The resultant formulation exhibited a particle size of 130.23 nm, and entrapment efficiency of 94.27 %, & zeta potential of -20.21 mV with unimodal size distribution. Pharmacokinetics and biodistribution studies revealed that the formulation was able to provide sufficient plasma drug concentration for the longer period of time and the drug was more distributed in ovarian cancer tissues. Results of MTT assay concluded that GenNLC were more effective in comparison to pristine Gen. CONCLUSION: In a nutshell, GenNLC seems to be a superior alternative carrier system for the formulation industry to obtain the higher entrapment with excellent stability of the formulation.