Development and evaluation of xanthan gum-facilitated ethyl cellulose microsponges for controlled percutaneous delivery of diclofenac sodium

Abstract

In this study, xanthan gum-facilitated ethyl cellulose microsponges were prepared by the double emulsification technique and subsequently dispersed in a carbopol gel base for controlled delivery of diclofenac sodium to the skin. Scanning electron microscopy revealed the porous, spherical nature of the microsponges. Increase in the drug/ polymer ratio (0.4:1, 0.6:1, 0.8:1, m/m) increased their yield (79.1-88.5 %), drug entrapment efficiency (50.0-64.1 %), and mean particle diameter (181-255 mm). Compared to the microsponges with high drug/polymer ratio (0.8:1, m/m), the flux of entrapped drug through excised rat skin decreased by 19.9 % and 17.0 %, respectively, for the microsponges prepared at low and intermediate drug/polymer ratios. When an equivalent amount of pure drug (not entrapped into microsponges) was dispersed into the gel base and the flux was compared, the microsponges (drug/polymer ratio 0.8:1, m/m) were found to reduce the flux by 33.3 %. Whether the drug was dispersed either in un-entrapped or entrapped form into the gel base, the drug permeation through rat skin followed Higuchi's diffusion kinetic model. The microsponges prepared at the lowest drug/polymer ratio exhibited a comparatively slower drug permeation profile and were hence considered most suitable for controlled drug delivery application. FTIR spectroscopy and DSC analyses indicated the chemically stable, amorphous nature of the drug in these microsponges. The gel containing these optimized microsponges was comparable to that of a commercial gel formulation and did not show serious dermal reactions. Hence, the microsponge system obtained at the lowest drug/polymer ratio could be useful for controlled release of diclofenac sodium to the skin.

Evaluation of sodium diclofenac release using natural rubber latex as carrier

“…The absence of crystallinity in the NaDic-NRL membrane indicates that NaDic is amorphous or molecularly disperse within the microparticles 25,26 . Amorphous NaDic has also been found by Li et al 27 , Manjunatha et al 28 , Lopes et al 29 and Maiti et al 30 showed barely irritant to rat skin.…”

Bioadhesive vaginal tablets containing spray dried microspheres loaded with clotrimazole for treatment of vaginal Candidiasis

“…Peaks at wavelengths corresponding to the pure drug were also observed in the microsphere formulation M4. The FTIR spectra of the pure drug and formulation indicated that the positions of characteristic peaks of CTZ were not altered after their successful entrapment in the microspheres, suggesting the absence of interactions between the drug and other components of the formulation (19).…”

Design and formulation of a topical hydrogel integrating lemongrass-loaded nanosponges with an enhanced antifungal effect: in vitro/in vivo evaluation

“…22 Ethyl cellulose has been used successfully by several researchers for the development of topically applied microsponges and nanosponges, with enhanced performance. 17,[23][24][25] This present research aimed to develop lemongrassloaded ethyl cellulose nanosponges with topical hydrogel with an enhanced antifungal effect and decreased irritation, using the emulsion solvent evaporation technique. A 3 2 full factorial design was applied to investigate the effect of formulation factors on the in vitro release of lemongrass and the particle size of the prepared nanosponges.…”