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

Development and characterization of self-assembling sirolimus-loaded micelles as a sublingual delivery system

The aim of this study was to develop self-assembling micelles of poorly water soluble potent immunosuppressant agent sirolimus (SRL) to enhance the solubility and mucosal permeability as stable aqueous formulations for sublingual administration. D-alpha-tocopheryl 1000 succinate (TPGS), soy phosphatidylcholine (SPC), and sodium cholate (NaC) were used to prepare the SRL-loaded micelles using the one-step self-assembly method. The mean hydrodynamic diameter of optimal micelles ranged from approximately 13 to 42 nm with low polydispersity index (PDI). The formulations possessed drug loading (DL) and drug encapsulation efficiency (EE) of around 18% and 99%, respectively. SPC caused an increase in mean hydrodynamic diameter and PDI of micelles, but no negative impact on DL and EE values was observed when used at concentrations of = 25% (w/w) of amphiphiles. However, NaC caused a detrimental effect on the characteristics of micelles in every respect. Ex vivo permeation studies revealed that TPGS-based micelles without SPC were not able to enhance the permeation of SRL compared to the SRL solution through bovine sublingual mucosa. However, the incorporation of SPC into the micelles significantly increased the mucosal permeation of SRL compared to the SRL solution. The optimal formulations maintained their characteristics at 4 degrees C for at least 90 days. These results support the feasibility of SRL-loaded micelles as a sublingual delivery system.This study was supported by Ege University Scientific Research Projects Coordination (Project Number: 17-ECZ-016)Ege University Scientific Research Projects Coordination [17-ECZ-016

Formulation and evaluation of fexofenadine hydrochloride orally disintegrating tablets for pediatric use

WOS: 000428979600026Allergic rhinitis is a common disease in children which has considerable negative effects on the quality of life. Fexofenadine hydrochloride (FFH) is a second-generation oral antihistamine which has been widely perscribed for alleviating symptoms of AR in children. The aim of this study was to take the advantage of convenient direct compression method for preparation of Orally Disintegrating Tablets (ODTs) containing 30 mg FFH per tablet. Six ready-to-use commercial tablet excipients (F-Melt (R), Pearlitol (R) Flash, Pharmaburst (R) 500, Prosolv (R) Easytab SP, Ludiflash (R), Parteck (R) ODT (R)) were used for direct compression and suitability of these excipients were evaluated. ODTs could be successfully compressed with all the investigated excipients and all of the formulations exhibited acceptable crushing stregth, low friability and remarkably short disintegration time. The ODTs which were able to possess a disintegration time below 30 s were considered eligible for further studies. In vitro dissolution studies showed a complete release of the drug from ODTs made from Pharmaburst (R) 500 within 15 min. Short term stability results exhibited no significant change of the drug in tested formulations. In conclusion, FFH containing ODTs formulated with Pharmaburst (R) 500 were determined explicitly the most promising formulation when compressed at a force of 1000 kg.Yuzuncu Yil University FoundationYuzuncu Yil University [2013-SBE YL 049]; TR Prime Ministry State Planning Organization FoundationTurkiye Cumhuriyeti Kalkinma Bakanligi [09/DPT/001]The authors would like to thank Prof. Dr. Idris Turel from Adiyaman University, Faculty of Pharmacy, Department of Pharmacology. This study was supported by Yuzuncu Yil University Foundation (Project Number: 2013-SBE YL 049). The authors would also like to thank to the TR Prime Ministry State Planning Organization Foundation (Project Number 09/DPT/001)

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

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

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

WOS: 00020934590006