The aim of this study was to prepare and to evaluate the physicochemical and in vitro drug release characteristics of different nanostructured systems containing clobetasol propionate (CP): CP-loaded polymeric nanoparticles (nanocapsules and nanospheres) and CP-loaded nanoemulsion. Physicochemical characteristics of the formulations were monitored up to 9 months after preparation by means of drug content, encapsulation efficiency, mean size, polydispersity index, pH, and zeta potential. In vitro drug release studies were carried out using the dialysis bag method. Photostability of CP-loaded nanoparticles was evaluated by their exposition to UVA radiation. All formulations presented nanometric mean size (140-220 nm), polydispersity index below 0.25, neutral pH values, negative zeta potential and encapsulation efficiency close to 100%. All these parameters, except pH, remained unchangeable up to 9 months of storage at room temperature for CP-loaded nanocapsules. On the other hand, CP-loaded nanospheres and nanoemulsion showed an increase in their mean size, as well as in polydispersity index under storage (after 3 and 6 months, respectively). In vitro drug release studies showed a controlled release of CP from nanoparticles (nanocapsules > nanospheres > nanoemulsion) with a low burst release. Photostability of CP under UVA radiation was improved by its incorporation into nanoparticles (nanocapsules > nanoemulsions > nanospheres).
Taking all these results together, the hydrogel containing D-NC represent a promising approach to treat antiproliferative-related dermatological disorders.
The influence of the polymeric amorphous materials on the physicochemical and drug release properties of drug-loaded nanocapsules as well as their role on the protection of the entrapped drug against the degradation induced by UV radiation was evaluated. Nanocapsules were prepared by interfacial deposition of preformed polymer (PLA, PLGA 50:50, and PLGA 85:15) using clobetasol propionate as the drug model. In vitro drug release was evaluated by the dialysis bag method. Photochemical stability was studied under UVA radiation. After preparation, all formulations presented nanometric mean size (180-200 nm), polydispersity index below 0.20, acid pH, negative zeta potential, and encapsulation efficiency close to 100%. Clobetasol propionate-loaded PLGA nanocapsules presented a lower physicochemical stability, showing a high drug leakage during 3 months of storage. In vitro studies showed biphasic drug release from all nanocapsules (according to an anomalous transport) and no influence of the hydrophilic characteristics of the amorphous polymeric material on the release rate. The photostability of clobetasol propionate under UVA radiation was improved by its incorporation into PLA and PLGA nanocapsules showing that besides semicrystalline polymers, amorphous polymers could also efficiently protect nanoencapsulated drugs against UV radiation.
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