Pharmaceutical Approaches and Advancements in Male Contraception

Currently available contraceptive methods offer a variety of options for women, but only very few for men which include surgical methods, condom and hormonal methods. Non-surgical and non-hormonal methods are under investigation. Among these, hormonal contraceptive approaches, including injections, oral and transdermal delivery systems of testosterone, have attracted the attention of investigators. Also non-hormonal approaches based on chemicals extracted from different plants suchas cotton seed plant, Neem tree, Trypterigium wilfordii and Momordica Charantia seed, are known to have effect on male fertility. Additionally, alkylated imino sugars, Ca++ channel blockers, indenopyridines, indazole-3-carboxylic acid analogues, reversible inhibition of sperm under guidance(RISUG) which involves injection of stericmaleic anhydride with dimethyl sulfoxide, spermicide– microbicide (including gel formulations) and vaccine approaches are intended to interfere in a certain fertilization step. Information obtained from multi-center studies in several countries on both men or women shows the necessity for additional reversible male contraceptive methods. Results from recent surveys clearly indicate that there is a market and a need for novel pharmaceutical preparations formale contraception.Keywords: Male Contraception, Contraceptive agents, Hormonal method

Poly(ethylene oxide)–Poly(propylene oxide)-Based Copolymers for Transdermal Drug Delivery: An Overview

Amphiphilic poly(ethylene oxide)–poly(propylene oxide) (PEO–PPO)-based copolymers are thermoresponsive materials having aggregation properties in aqueous medium. As hydrosolubilizers of poorly water-soluble drugs and improved stability of sensitive agents, these materials have been investigated for improvement in solubility, stability, release and bioavailability of drugs. The goal of the present review is to summarize the properties of PEO–PPO based copolymers and highlight the works that have been carried out on these materials for transdermal drug delivery.Keywords: PEO–PPO based copolymer, Poloxamer, Hydrogel, Transdermal, Drug delivery

Injectable In Situ Forming Microparticles: A Novel Drug Delivery System

Pharmaceutical formulation research has recently been focusing on delivery systems which provide long therapeutic effects and reduced side effects, and involving simplified production stages and facilitated application process. In situ forming microparticle (ISM) systems, one of the latest approach in this field, offer a new encapsulation technique and meet the objectives stated above. Factors such as the carrier used to form the multiparticles, amount and type of drug and the vehicle type can be taken as the main performance criteria for these systems. Ongoing studies have shown that this new multiparticulate drug delivery system is suitable for achieving new implant delivery system with low risk of dose-dumping, capable of being modulated to exhibit varying release patterns, reproducible, easily applicable and welltolerated compared with classically surgical implants.Keywords: Injectable, In situ forming, Microparticle system, Controlled drug delivery

Etodolac transdermal cubosomes for the treatment of rheumatoid arthritis: ex vivo permeation and in vivo pharmacokinetic studies

Journal Drug Delivery Volume 24, 2017 - Issue 1In this study, transdermal etodolac-loaded cubosomes were developed in order to relieve patient pain and joints stiffness by providing stable etodolac concentration at the targeting sites through controlled drug delivery via the noninvasive skin route with more sustaining and less frequent dosing. Different ratios and percentages of poloxamer 407 and monoolein were used to formulate the cubosomes using emulsification and homogenization processes. The etodolac-loaded cubosomes showed particle size values ranging from 135.95 to 288.35 nm and zeta potential values ranging from −18.40 to −36.10 mV. All the cubosomes offered an encapsulation efficiency value of about 100% and showed drug loading capacity ranging from 1.28 to 6.09%. The in vitro drug release studies revealed a controlled drug release profile with a drug release rate up to 15.08%/h. Increasing poloxamer concentration in etodolac-loaded cubosomes resulted in nanoparticles with less particle size and faster drug release. The particles exhibited cubic and hexagonal shapes. The DSC and X-ray analysis demonstrated that the drug was encapsulated in the cubosomes bicontinuous structures in amorphous form. In addition, investigated cubosomes exhibited fast drug penetration through excited mice skin followed by slower drug penetration for up to 24 h. The pharmacokinetic study in human volunteers showed that the selected etodolac-loaded cubosomes enhanced the bioavailability of etodolac as compared to the oral capsules (266.11%) with evidence of longer half-life and higher MRT that reached 18.86 and 29.55 h, respectively. The etodolac-loaded cubosomes propose a promising system for treatment of arthritis simply through skin application