Formulation, Development, In Vitro Characterization, and Application of a Drug-Loaded Microporous Drug Delivery System

Microsponges are an excellent choice of drug delivery system because they are porous, spherical, polymeric, and have a very high internal surface area, which facilitates efficient entrapment and controlled release of drugs. This study aims at formulation and systematic optimization of a microsponge-based drug delivery system for a poorly water-soluble BCS Class II drug, which suffers from the drawbacks of low bioavailability, burst release, frequent dosage and poor stability. The microsponges will be prepared by the quasi-emulsion solvent diffusion (QESD) method and optimized by employing a 2³ factorial design. The amount of ethyl cellulose, dichloromethane volume, and stirring speed will be used as independent variables, and the responses of dependent variables will be particle size, entrapment efficiency, and cumulative drug release. The formulation will be optimized in terms of particle size, zeta potential, surface morphology, drug entrapment, crystallinity, thermal behavior, elemental composition, and in vitro drug release, utilizing the appropriate analytical methods such as P-XRD, DSC, FESEM-EDS, and dissolution studies. Accelerated stability testing will be conducted in line with the ICH guidelines. The study is projected to develop a quality-by-design (QbD) based platform of microsponge formulation that will be used to increase the drug solubility and release profile, enhance the formulation stability, and potentially increase the therapeutic efficacy of the drugs.