title: Microemulsion for topical application of pentoxifylline: In vitro release and in vivo evaluation.
abstract: Microemulsion containing pentoxifylline was developed and characterized for use as a topical alternative to treat skin disorders. The transparent formulation was developed and optimized based on a pseudoternary phase diagram. Pentoxifylline-loaded microemulsion (PTX-ME) was composed of 44% Tween 80™/Brij 52™ mix as surfactants (S), 51% of caprylic/capric triglycerides as the oil phase (O) and 5% of water as aqueous phase (A). It was classified as an isotropic water-in-oil (W/O) system with droplets that had a heterogeneous spherical shape within the nanosized range (67.36±8.90nm) confirmed by polarized light microscopy, differential scanning calorimetry (DSC), transmission electron microscopy (TEM) and dynamic light scattering (DLS) analysis. In vitro studies using static diffusion Franz cells revealed that the release of PTX from ME followed the Higuchi kinetic model. Topical PTX-ME application developed superior anti-inflammatory activity when compared to the PTX solution, reducing the paw edema up to 88.83%. Our results suggested that this colloidal nanosystem is a promising agent for the delivery of pentoxifylline, increasing its ability to modulate the inflammatory aspects of skin disorders.
authors.affiliation: Graduation Program in Pharmaceutical Sciences, Center for Biological and Health Sciences, State University of Paraíba (UEPB), Campina Grande, Brazil; Laboratory of Development and Characterization of Pharmaceutical Products, Department of Pharmacy, Center for Biological and Health Sciences, State University of Paraíba (UEPB), Campina Grande, Brazil.
authors.forename: Airlla L M
authors.initials: AL
authors.lastname: Cavalcanti
authors.affiliation: Graduation Program in Pharmaceutical Sciences, Center for Biological and Health Sciences, State University of Paraíba (UEPB), Campina Grande, Brazil; Laboratory of Development and Characterization of Pharmaceutical Products, Department of Pharmacy, Center for Biological and Health Sciences, State University of Paraíba (UEPB), Campina Grande, Brazil.
authors.forename: Mysrayn Y F A
authors.initials: MY
authors.lastname: Reis
authors.affiliation: Laboratory of Development and Characterization of Pharmaceutical Products, Department of Pharmacy, Center for Biological and Health Sciences, State University of Paraíba (UEPB), Campina Grande, Brazil.
authors.forename: Geilza C L
authors.initials: GC
authors.lastname: Silva
authors.affiliation: Laboratory of Development and Characterization of Pharmaceutical Products, Department of Pharmacy, Center for Biological and Health Sciences, State University of Paraíba (UEPB), Campina Grande, Brazil.
authors.forename: Ízola M M
authors.initials: ÍM
authors.lastname: Ramalho
authors.affiliation: Laboratory of Development and Characterization of Pharmaceutical Products, Department of Pharmacy, Center for Biological and Health Sciences, State University of Paraíba (UEPB), Campina Grande, Brazil.
authors.forename: Geovani P
authors.initials: GP
authors.lastname: Guimarães
authors.affiliation: Graduation Program in Pharmaceutical Sciences, Center for Biological and Health Sciences, State University of Paraíba (UEPB), Campina Grande, Brazil; Laboratory of Development and Characterization of Pharmaceutical Products, Department of Pharmacy, Center for Biological and Health Sciences, State University of Paraíba (UEPB), Campina Grande, Brazil.
authors.forename: José A
authors.initials: JA
authors.lastname: Silva
authors.affiliation: Graduation Program in Pharmaceutical Sciences, Center for Biological and Health Sciences, State University of Paraíba (UEPB), Campina Grande, Brazil; Nucleus of Technology Platforms, Aggeu Magalhães Research Center, Fiocruz, Recife, Brazil.
authors.forename: Karina L A
authors.initials: KL
authors.lastname: Saraiva
authors.affiliation: Graduation Program in Pharmaceutical Sciences, Center for Biological and Health Sciences, State University of Paraíba (UEPB), Campina Grande, Brazil; Laboratory of Development and Characterization of Pharmaceutical Products, Department of Pharmacy, Center for Biological and Health Sciences, State University of Paraíba (UEPB), Campina Grande, Brazil. Electronic address: bolivarpgld@pq.cnpq.br.
authors.forename: Bolívar P G L
authors.initials: BP
authors.lastname: Damasceno
mesh_terms: D000279:Administration, Cutaneous; D000818:Animals; D002626:Chemistry, Pharmaceutical / Q000379:methods; D004195:Disease Models, Animal; D065546:Drug Liberation; D004487:Edema / Q000188:drug therapy; D004655:Emulsions; D005079:Excipients / Q000737:chemistry*; D007249:Inflammation / Q000188:drug therapy; D008297:Male; D053758:Nanoparticles; D010316:Particle Size; D010431:Pentoxifylline / Q000008:administration & dosage* / Q000737:chemistry / Q000493:pharmacokinetics; D044367:Phase Transition; D010726:Phosphodiesterase Inhibitors / Q000008:administration & dosage* / Q000737:chemistry / Q000493:pharmacokinetics; D051381:Rats; D017208:Rats, Wistar; D012869:Skin Absorption; D013501:Surface-Active Agents / Q000737:chemistry
chemical_list: D004655:Emulsions; D005079:Excipients; D010726:Phosphodiesterase Inhibitors; D013501:Surface-Active Agents; D010431:Pentoxifylline
keywords: Anti-inflammatory activity; Caprylic/capric triglycerides PubChem CID: 93356; Drug release; Pentoxifylline PubChem CID: 4740; Phosphodiesterase inhibitor; Polyoxyethylene sorbitan monooleate PubChem CID: 86289060; Skin diseases