Contri, Renata Vidor

Guterres, Silvia Stanisçuaski

Katzer, Tatiele

Pohlmann, Adriana Raffin

English

Lume 5.8

caderno d•farmácla ISSN 0102-6593 Órgão Oficial da Faculdade de Farmácia da Universidade Federal do Rio Grande do Sul volume 26, Suplemento, 201 O TECNOLOGIA FARMACÊUTICA E BIOFARMÁCIA 224 ~~~~~~~~·:}~i-~~cb~~l{~O~~~~~~~-Pharmaceutical technology and biopharmacy IN VITRO RELEASE ANO EX VIVO SKIN PERMEATION OF A NANOSTRUCTURED FORMULATION FOR TOPICAL DELIVERY OF CAPSAICINOIDS Contri R.V. 1·; Katzer T. 1; Pohlmann A.R. 2; Guterres S.S.1 1Laboratório de Cosmetologia, Faculdade de Farmácia, UFRGS; 2 Laboratório de Nanopartículas, Instituto de Química, UFRGS *Doutoranda -Início: 2010/1 lntroduction: Formulations based on the association of nanocarriers and hydrogels have been deeply studied in the past years 1 •2•3 . Such systems can provi de a controlled release of the active substances, due to both the hydrogel network and the reservoir property of the nanocarriers4 , besides being capable of an appropriate delivery of the substances to the active sites, such as the skin. In this work it is proposed the use of chitosan as the hydrogel-forming biopolymer5 and Eudragit RS 1 oo® as the biocompatible polymeric wall of capsaicinoids-loaded nanocapsules for developing an innovative formulation for topical delivery. The capsaicinoids (capsaicin and dihydrocapsaicin) are the substances responsible for the hot and pungent taste of chil~ peppers and have been applied as analgesic for the treatment of chronic pain in severa! diseases . Objective: The aim of this work was to characterize a chitosan hydrogel containing capsaicinoids-loaded nanocaspules by means of the determination of the in vitro release and ex vivo skin permeation, as well as to relate the results obtained in both studies. Materiais and Methods: The hydrogel containing nanocapsules (n=3) was obtained by the incorporation of a nanocapsule aqueous suspension prepared by the interfacial deposition of preformed polymer method7 in a chitosan hydrogel (chitosan 3.5% and lactic acid 1.5%). The formulation was characterized in terms of capsaicinoids content (HPLC-UV), particle size analysis (laser diffraction), morphology [transmission electron microscopy (TEM)], pH (potentiometry), in vitro release (dialyses bags method, quantification by HPLC-UV) and ex vivo skin permeation (pig skin in Franz diffusion cells, quantification by HPLC-UV). For the in vitro release and skin permeation studies, the control, representing the free drug, was a chitosan hydrogel containing a hydroalcoholic solution (30% ethanol) of capsaicinoids. Results and Discussion: The hydrogels containing capsaicinoids-loaded nanocapsules presented capsaicin and dihydrocapsaicin content close to 95%, considering O, 161 mg/g and O, 183 mg/g as 100%, and pH of 4.42 ± 0.21, which is acid, due to the presence of lactic acid, but suitable for topical application. lt was possible to detect the nanoparticles in the hydrogel network by TEM and by laser diffraction, after dilution of the hydrogel. Considering the in vitro release, it was observed a more prolonged release of the capsaicinoids due to the nanoencapsulation. The skin permeation study showed that, for the nanostructured formulation, after 8h of permeation, the capsaicinoids amount that was retained on the skin surface, without permeation through the skin layers, remained the same, probably dueto the fact that capsaicin and dihydrocapsaicin were not yet significantly released from the nanocapsules. For the chitosan hydrogel containing free capsaicinoids (control), it was observed that, after 8h, the amount retained on the skin surface was lower than after 4 and 2h, probably because the drugs were not encapsulated and they could diffuse through the hydrogel and permeate through the skin layers. Conclusions: The proposed formulation presented suitable properties for topical delivery. The nanoencapsulation of capsaicinoids promoted a controlled release from the vehicle, which was verified by the in vitro experiment and confirmed by the skin permeation test. So, it was possible to relate the data observed on the in vitro release and the ex vivo skin permeation. References: 1. E.B Souto et a/., Eur. J. Pharm. 58, 83 (2004). 2. E. Ruei-Gariépy et a/., J. Contrai. Release 82, (2002). 3. C.Y. Gong et ai. J Phys Chem, Part 8. 113, 10183 (2009). 4. A. Jãger et ai., lnt. J. Pharm. 338, 297 (2007). 5. M. Rinaudo Prog. Polym. Sei. 31, 603 (2006). 6. M. Hayman & P.C.A. Kam Curr. Anaesth. Crit. Care 19, 338 (2008). 7. H. Fessi et ai., lnt. J. Pharm. 55, R 1 ( 1989). Acknowldgements: Financiai support from CNPq/Brazil. 

In vitro release and ex vivo skin permeation of a nanostructured formulation for topical delivery of capsaicinoids

https://lume.ufrgs.br/bitstream/10183/267763/1/000770540.pdf

In vitro release and ex vivo skin permeation of a nanostructured formulation for topical delivery of capsaicinoids

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