Preparation and Evaluation of Chitosan Submicroparticles Containing Pilocarpine for Glaucoma Therapy

Title:Preparation and Evaluation of Chitosan Submicroparticles Containing Pilocarpine for Glaucoma Therapy

Volume: 12 Issue: 5

Author(s): Cleonice Marques Costa, Leticia Coli Louvisse de Abreu, Elisabete Pereira dos Santos, Octavio Augusto Franca Presgrave, Anna Paola Trindade Rocha Pierucci, Carlos Rangel Rodrigues, Valeria Pereira de Sousa, Sara Nicoli, Eduardo Ricci Junior and Lucio Mendes Cabral

Affiliation:

Keywords: Chitosan, Glaucoma, Ocular delivery, Pilocarpine, Spray drying, Submicroparticles.

Abstract: The objective of the present study was to optimize the preparation of chitosan submicroparticles and to assess whether they enhanced ocular permeation of pilocarpine. Submicroparticles were produced by spray drying and characterized to determine process yield, encapsulation efficiency, morphology, size distribution, drug-polymeric matrix interaction, porcine sclera permeation as well as ocular irritancy and drug retention. Quantification of pilocarpine using High Performance Liquid Chromatography was found to be selective, linear, precise, accurate and robust. The spray drying method proved to be simple and reproducibly produced particles with satisfactory yields, thus showing potential for industrial scale applications. The pilocarpine-loaded chitosan particles exhibited adequate morphological characteristics as well as high encapsulation efficiency. The particles produced were on a submicrometric scale and compatible with intraocular administration. In pilocarpine-loaded particles, the interaction between pilocarpine and chitosan polymeric matrix resulted in delayed release of the drug, attributed to formation of a reservoir system. The best fit for drug release was obtained using the Higuchi equation. The chitosan submicroparticles enhanced the permeation effect and increased the passage of pilocarpine through porcine sclera and also demonstrated low irritancy potential. Therefore, the particles produced can be considered a promising system for the ocular delivery of pilocarpine.

Cite this article as:

Costa Marques Cleonice, Louvisse de Abreu Coli Leticia, dos Santos Pereira Elisabete, Franca Presgrave Augusto Octavio, Rocha Pierucci Trindade Anna Paola, Rodrigues Rangel Carlos, de Sousa Pereira Valeria, Nicoli Sara, Junior Ricci Eduardo and Cabral Mendes Lucio, Preparation and Evaluation of Chitosan Submicroparticles Containing Pilocarpine for Glaucoma Therapy, Current Drug Delivery 2015; 12 (5) . https://dx.doi.org/10.2174/1567201812666150901113240