Mucoadhesive in situ gel formulations of miconazole nitrate for the treatment of mucosal candidiasis

This study focused on developing in situ gel formulations of miconazole nitrate with poloxamer 188 and 407 for treatment of mucosal candidiasis. In situ gel formulations were prepared and gelation temperature, rheological, mechanical and mucoadhesive properties, syringeability and release profiles were evaluated. Based on their suitable gelation temperature properties, formulations containing the poloxamer (Plx) 407 and 188 in ratios of 15:15 (F1), 15:20 (F2) and 20:10 (F3) were chosen for further studies. F3 exhibited typical gel-type mechanical spectra at 37 °C whereas F1 and F2 behaved like weakly cross-linked gels. Texture profile analysis demonstrated that F3 showed the highest cohesiveness, adhesiveness, hardness and compressibility. According to the these results, F3 was chosen for in vivo studies and it was shown that it is effective for the treatment of the vaginal candidiasis. Histopathologic evaluation also supported the effectiveness of the formulation. As a result, in situ gel formulations prepared with Plx 407 and 188 mixture of miconazole nitrate proved to be a promising alternative dosage form for treatment of mucosal candidiasisColegio de Farmacéuticos de la Provincia de Buenos Aire

Design and Formulation of Mebeverine HCl Semisolid Formulations for Intraorally Administration

WOS: 000278921800022PubMed ID: 20101482Gel formulations of mebeverine hydrochloride (MbHCl) containing hydroxypropylmethylcellulose (HPMC), metolose (MTL), and poloxamer 407 (PLX) were prepared to be used in the treatment of different oral painful conditions. HPMC was used as a mucoadhesive gel base while MTL and PLX were used to prepare sol-gel thermosensitive gels. MTL and PLX formulations showed proper sol-gel transition temperature for intraoral application. Formulations were evaluated in terms of their viscosity, mechanical properties, mucoadhesivity, stability, and in vitro drug release. The formulation prepared with 2% of HPMC K100M provided the highest viscosity at room temperature. However, the viscosity of HPMC-PLX mixture showed a significant increase at body temperature. The greatest mucoadhesion was also noted in HPMC PLX combinations. Texture pro. le analysis exhibited the differences of the adhesion, hardness, elasticity, cohesiveness, and compressibility of the formulations. The release profiles of MbHCl were obtained, and non-Fickian release was observed from all the formulations. The formulations were stored at different temperature and relative humidity. No significant changes were observed at the end of the 3 months. HPMC-PLX formulation of MbHCl was chosen for in vivo studies, and it remained longer than dye solution on the rabbit's intraoral mucosal tissue. It was found worthy of further clinical evaluation

A COMPARISION OF MECHANICAL PROPERTIES OF BUCCAL GEL FORMULATIONS BASED ON DIFFERENT BIOADHESIVE POLYMERS

WOS: 00020934590006

Strategies to Prolong the Intravaginal Residence Time of Drug Delivery Systems

WOS: 000272231000007PubMed ID: 20067707The vagina has been studied as a suitable site for local and systemic delivery of drugs. There are a large number of vaginal medications on the market. Most of them, however, require frequent applications due to their short vaginal residence time. A prolonged vaginal residence time of formulations is therefore a key parameter for improved therapeutic efficacy. Promising approaches for prolonging the residence time base on mucoadhesion, were in- situ sol-to-gel transition and mechanical fixation. Mucoadhesive drug delivery systems can be tailored to adhere to the vaginal tissue. In-situ gelling systems offer the advantage of increased viscosity in vaginal cavity and consequently reduce outflow from the vagina. Mechanical fixation needs specially shaped drug delivery systems and reduce the frequency of administration significantly. In this review, an overview on these different strategies and systems is provided. Furthermore, the techniques to evaluate the potential of these systems for prolonged vaginal residence time are described