Skin penetration and photoprotection of topical formulations containing benzophenone-3 solid lipid microparticles prepared by the solvent-free spray-congealing technique

Author(s)

Martins, Rodrigo Molina ^[1] ; Siqueira, Silvia ^[1] ; Vieira Fonseca, Maria Jose ^[1] ; Pedro Freitas, Luis Alexandre ^[1]

Affiliation

^[1] Univ Sao Paulo, Fac Ciencias Farmaceut Ribeirao Preto, BR-14040903 Ribeirao Preto, SP - Brazil

• Document type: Journal article
• Source: Journal of Microencapsulation; v. 31, n. 7, p. 644-653, 2014.
• Web of Science Citations: 9

Abstract

Purpose: Solid-lipid microparticles loaded with high amounts of the sunscreen UV filter benzophenone-3 were prepared by spray congealing with the objective of decreasing its skin penetration and evaluate whether the sunscreen's photoprotection were impaired by the microencapsulation process. Methods: The microparticles were produced using the natural lipids carnauba wax or bees wax and three different concentrations of benzophenone-3 (30, 50 and 70%) using spray congealing technique. Results: The microparticles presented properties suitable for topical application, such as spherical morphology, high encapsulation efficiency (95.53-102.2%), average particle sizes between 28.5 and 60.0 mu m with polydispersivities from 1.2 to 2.5. In studies of in vitro skin penetration and preliminary stability, formulations of gel cream containing carnauba wax solid lipid microparticles and 70% benzophenone-3 when compared to the formulation added of bees wax solid-lipid microparticles containing 70% benzophenone-3, was stable considering the several parameters evaluated and were able to decrease the penetration of the UV filter into pig skin. Moreover, the formulations containing solid lipid microparticles with 70% benzophenone-3 increased the photoprotective capacity of benzophenone-3 under UV irradiation. Conclusion: The results show that spray-congealed microparticles are interesting solid forms to decrease the penetration solar filters in the skin without compromising their photoprotection. (AU)

• FAPESP's process: 10/11602-3 - Pharmaceutical development and photo chemopreventive evaluation of a formulation containing sunscreen and rutin
• Grantee: Rodrigo Molina Martins
• Support Opportunities: Scholarships in Brazil - Doctorate
• FAPESP's process: 08/02848-9 - Study on the Preparation of Solid Dispersions containing Low Solubility Pharmaceuticals by Spray Congealing
• Grantee: Luis Alexandre Pedro de Freitas
• Support Opportunities: Regular Research Grants