Preparation and characterization of mucoadhesive gels containing pentoxifylline loaded nanoparticles for vaginal delivery of genital ulcer

Abstract

Mucoadhesive gel formulations containing pentoxifylline (PTX)-loaded nanoparticle (NP) for the treatment of genital ulcer were prepared and evaluated. In that context, formulation properties like particle size (PS), polydispersity index (PI), zeta potential (ZP), drug content and entrapment efficiency (EE), rheology, mucoadhesion, swelling index, in vitro drug release, cytotoxicity, radio-labeling, and cell binding were evaluated. The prepared NP formulation exhibited a small PS with a narrow distribution, a high ZP and a high EE. In addition, the mucoadhesive gel formulation showed a non-Newtonian plastic flow, good mucoadhesive properties, a suitable swelling index, represented as water absorption and retention abilities, a burst release within the first 1 h and release of more than 95% during the first 8 h, no cytotoxicity on PCS-480-010™ cells and a high cell binding rate of radio-labeled formulation. Mucoadhesive gel formulation containing PTX-loaded NP is beneficial for enhancing the therapeutic efficacy of PTX administered through vaginal route by increasing the retention time and the easiness for local application in the vaginal mucosa. The prepared formulation is a promising candidate for vaginal application of PTX, which could be further investigated with in vivo animal studies.