Innovative Mucoadhesive Precursor of Liquid Crystalline System Loading Anti-Gellatinolytic Peptide for Topical Treatment of Oral Cancer

Current researches report an actual benefit of a treatment for oral cancer via inhibition of proteolytic matrix metallopro-teinases (MPP) with a peptide drug, called CTT1. However, peptides present poor oral bioavailability. Topical administration on oral mucosa avoids its passage through the gastrointestinal tract and the first-pass liver metabolism, but the barrier function of the oral mucosa can impair the permeation and retention of CTT1. The objective of this study is to incorporate CTT1 into a mucoadhesive precursor of liquid crystalline system (PLCS) as an interesting strategy for the topical treatment of oral cancer. PLCS consisting of oleic acid, ethoxylated 20 and propoxylated cetyl alcohol 5, polyethyleneimine (P)-associated chitosan (C) dispersion and CTT1 (FPC-CTT1) was developed and characterized by polarized light microscopy (PLM) and small-angle X-ray scattering (SAXS). In vitro permeation and retention across esophageal mucosa, In vitro cytotoxicity towards tongue squamous cell carcinoma cells, and in vivo evaluation of vascular changes using the chick embryo chorioallantoic membrane (CAM) model were performed. PLM and SAXS showed that FPC-CTT1acted as PLCS, because it formed a lamellar liquid crystalline system after the addition of artificial saliva. FPC-CTT1increased approximately 2-fold the flux of permeation and 3-fold the retention of CTT1 on the porcine esophageal mucosa. CTT1 does not affect cell viability. CAM tests showed that FPC preserved the blood vessels and it can be a safe formulation. These findings encourage the use of the FPC-CTT1 for topical treatment of oral cancer.

LYOTROPIC LIQUID CRYSTALLINE SYSTEM FOR EFFECTIVE TOPICAL DELIVERY OF TOLNAFTATE

The present investigation deals with the formulation, optimization and evaluation of liquid crystalline cream of Tolnaftate. Brij-78 used as a surfactant, Cetostearyl alcohol was used as a co-surfactant and Silicon oil as a oil phase. Liquid crystalline cream system, has a potential for efficient delivery of Tolnaftate (1%), as topical dermal drug delivery system. The liquid crystalline system enhance the diffusion of water insoluble drug Tolnaftate through the skin for effective result. Liquid crystals (LC) are substances that flow like liquids but maintain some of the ordered structure characteristics of crystalline solids. Based on the ways that LCs are generated, they can be classified into two types 1) Thermotropic LCS and 2) Lyotropic LCs. Incorporation of the drug in liquid crystal increased its antimycotic activity against different antifungal microorganisms. Used surfactant enhance the penetration of drug and also improve the solubility of drug. The objective of this study was to increase the diffusion coefficient of drug through the formulation, and also to improve the availability of drug at the site of action. The prepared liquid crystalline cream exhibited the expected, viscosity, drug content, pH, spreadability, in vitro drug release and in vitro antimycotic inhibitory activity. Liquid crystalline cream for tolnaftate was found to be stable cream. It was found to have better in vitrorelease profile characteristics, and in vitro antimycotic activity, it can be concluded that the formulation F5 has better potential of antimicrobial activity and to enhance the diffusion of drug through the cream.