Development and Evaluation of Terbinafine Hydrochloride Polymeric Microsponges for Topical Drug Delivery

Abstract

Mahaparale et al.: Terbinafine Hydrochloride Polymeric MicrospongesThe objective of the present study was to develop and evaluate sustained delivery of terbinafine hydrochloride from topical polymeric microsponges. Microsponges of ethyl cellulose containing terbinafine hydrochloride were prepared by quasi emulsion solvent diffusion method. Effect of drug polymer ratio on active drug content, particle size and entrapment efficiency were studied. Drug polymer ratio greatly affects properties (entrapment efficiency, active drug content, particle size) of microsponges. Terbinafine hydrochloride microsponges showed highest actual drug content, entrapment efficiency and smaller particle size, so 1.5:1 ratio of drug and polymer was selected for optimization study. Optimization study was carried out by taking internal phase volume, stirring rate, emulsifier concentration as independent variables and their effects on entrapment efficiency, particle size were studied. It was found that as stirring speed increases, the particle size decreases and entrapment efficiency increases, while as volume of dichloromethane increases, particle size decreases. Morphology of obtained microsponges was revealed by scanning electron microscope and was found to be porous and spherical. Optimized formulation of microsponge was dispersed in Carbopol gel and evaluated for drug content, pH, viscosity and in vitro drug release. Release of drug was found to be sustained through microsponge gel as compared to marketed product and pure drug gel. Ex vivo drug deposition study was carried using rat abdominal skin. Drug deposition was found to be satisfactory. Prepared polymeric microsponges could be a potential topical drug delivery system in antifungal therapy.

Development and Evaluation of Polymeric Nanosponge Hydrogel for Terbinafine Hydrochloride: Statistical Optimization, In Vitro and In Vivo Studies

“…The studies established that the sustained release mechanism was followed by the developed formulation. Satisfactory drug deposition was also deduced [15]. Amer et al showed the importance of developing TH nanosponge that exhibited 90% of drug release within 8 h. Furthermore, the highest in vivo skin deposition and antifungal activity were also demonstrated in the developed formulation [16].…”

Optimization of entrapment efficiency and release of clindamycin in microsponge based gel

“…A total of 2 mL of the sample was withdrawn from the receptor compartment at definite time intervals and replaced with an equal volume of fresh receptor fluid. The aliquots were suitably diluted with the receptor medium and analysed by HPLC method 14 – 16 . In vitro drug release kinetics To investigate the release mechanism of CLN-free base from the microsponge loaded gels, the release data was analysed using zero order, first order, Higuchi, Hixson-Crowell, and Korsmeyer-Peppas.…”

“… Stability study Optimized batches of CLN microsponge gels were monitored for up to 6 months at 40 ± 2°/75 ± 5% RH as per ICH guidelines 17 . At the interval of 1, 2, 3, 4, 5, and 6 months, samples were withdrawn and analysed to determine changes in appearance, pH, viscosity and drug content, and drug release 14 . …”

Microsponge: A Novel Tool for Topical Drug Delivery of Anti Rheumatoid Drugs

“…A condition of stability study is temperature and relative humidity (40±2 ºC/75%±5%RH) as per ICH (International Conference on Harmonization) guidelines. Upon completion of stability study, collected samples can be subjected to analysis for various parameters [54][55][56].…”