Preparation of polymeric nanocapsules containing octyl methoxycinnamate by the emulsification–diffusion technique: Penetration across the stratum corneum

Abstract

Polymeric nanocapsules (NCs) containing octyl methoxycinnamate (OMC) as lipophilic molecule were prepared, and their in vivo distribution profile through the stratum corneum (SC) was determined by the tape-stripping technique. Penetration degree of OMC formulated in NCs was compared with that obtained for a nanoemulsion (NE), and a conventional oil-in-water (o/w) emulsion (EM). To produce stable cellulose acetate phthalate (CAP) nanocapsules containing the lipophilic sunscreen, a study was conducted to optimize the process of NC preparation based on the emulsification–diffusion technique. NC formation was verified by measuring their density using differential centrifugation. NC density revealed that an OMC (µL)/CAP (mg) ratio of 2.5:1 is optimal for encapsulation. High encapsulation entrapment (>96%) and excellent process efficiency (recovered quantity of NCs in relation with the initial amount of OMC and CAP >99%) were always achieved with this ratio or a higher one. The capsular structure of the NCs was evidenced with a direct SEM technique. NE was prepared by the emulsification–diffusion technique, dissolving a specific quantity of OMC in water-saturated 2-butanone and then, emulsifying with an aqueous solution of PVAL. In vivo percutaneous penetration, evaluated by the tape-stripping technique, demonstrated that NE increased the extent of OMC penetration relative to the penetration achieved by NCs or EM, with relative penetration depths through the SC of 0.86±0.1, 0.64±0.11, and 0.57±0.08, respectively. In the same manner, the accumulation in the skin of OMC was significantly greater with NE than with EM or NCs. OMC penetration depth was strongly dependent upon the size of the colloidal particles and their flexibility. © 2005 Wiley-Liss, Inc. and the American Pharmacists Association.