Development and Evaluation of PLGA Nanoparticle-Loaded Organogel for the Transdermal Delivery of Risperidone.

A transdermal delivery approach may circumvent the limitations associated with the oral use of risperidone (RIS), an atypical antipsychotic drug. The current study focuses on the utilization of poloxamer (pluronic) lecithin organogel (PLO), a suitable transdermal vehicle, and a biodegradable nanoparticulate system of PLGA with the potential to deliver RIS in an efficient way. PLGA nanoparticles were fabricated using different ratios of the polymer and surfactant. The optimization was performed principally on the basis of particle size and entrapment efficiency (EE). The developed PLGA nanoparticles were spherical, sized around 109 nm with negative charge (−9.3 mv) and enhanced drug entrapment efficiency (58%). The in vitro drug release study of lyophilized nanoparticles showed a sustained pattern. Statistical analysis confirmed that there was a significant difference (p < 0.05) between the nanoparticle-loaded PLO gel and conventional drug formulations in terms of drug release and ex vivo permeation across rat skin (three-fold). The results confirm enhanced drug release and permeation through the skin at 72 h. Hence, the investigated formulation could be a better alternative to the conventional route for improving patient compliance.

Proniosomes derived niosomes: recent advancements in drug delivery and targeting.

Vesicular drug delivery systems have gained wide attention in the field of nanotechnology. Among them proniosomes become the superior over other vesicular carriers. Proniosomes are dry formulations of water soluble nonionic surfactant coated carrier system which immediately forms niosomes upon hydration. They have the capability to overcome the instability problems associated with niosomes and liposomes and have the potential to improve solubility, bioavailability, and absorption of various drugs. Furthermore, they offer versatile drug delivery concept for enormous number of hydrophilic and hydrophobic drugs. They have the potential to deliver drugs effectively through different routes at specific site of action to achieve controlled release action and reduce toxic effects associated with drugs. This review discusses the general preparation techniques of proniosomes and mainly focus on the applications of proniosomes in drug delivery and targeting. Moreover, this review demonstrates critical appraisal of the literature for proniosomes. Additionally, this review extensively explains the potential of proniosomes in delivering drugs via different routes, such as oral, parenteral, dermal and transdermal, ocular, oral mucosal, vaginal, pulmonary, and intranasal. Finally, the comparison of proniosomes with niosomes manifests the clear distinction between them. Moreover, proniosomes need to be explored for proteins and peptide delivery and in the field of nutraceuticals and develop pilot plant scale up studies to investigate them in industrial set up.

Thiomers and their potential applications in drug delivery.

INTRODUCTION: Thiomers are the product of the immobilization of sulfhydryl-bearing ligands onto the polymer backbone of a conventional polymer, which results in a significant improvement in mucoadhesion; in situ gelation and efflux inhibition compare with unchanged polymers. Because of thiol groups, thiomers have more reactivity and enhanced protection against oxidation. Since the late 1990s, extensive work has been conducted on these promising polymeric excipients in the pharmaceutical field. Areas covered: This review covers thiomers, their classification and their different properties. Various techniques for the synthesis, purification and characterization of thiomers are described in detail. This review also encompasses their various properties such as mucoadhesion, permeation enhancement, in situ gelation and efflux inhibition, as well as different formulations based on thiomers. In addition to the use of thiomers as multifunctional excipients, this review also encompasses their use as drugs. Expert opinion: The synthesis is realized by linkage of sulfhydryl-bearing ligands but reported methods give low yields. Higher degrees of modification are not necessary and would probably lead to extreme changes in properties. Nevertheless, an accurate characterization of the final product is important. The scale-up procedure for industrial manufacturing has been adapted to produce GMP materials; Lacrimera® eye drops have already entered the European market.