European Journal of Biomedical and Pharmaceutical Sciences

FORMULATION AND EVALUATION OF NASAL IN-SITU GEL OF ESCITALOPRAM OXALATE FOR TREATMENT OF DEPRESSION

Pallavi Chand*, G. Gnanarajan, Ganesh Kumar and Preeti Kothiyal

ABSTRACT

The purpose of present study was to deal with develop intranasal drug delivery system of Escitalopram oxalate using thermosensitive polymer ( Poloxamer -F188) and mucoadhesive polymer (Carbopol – 934P) In-situ forming polymeric formulation drug delivery system is in sol form before administration in the body, but once administered, that undergoes gelation in -situ to form a gel. Formulations were modulated so as to have gelation temperature below 34⁰C to ensure gelation at physiological temperature after intranasal administration. 30% Pluronic F68 was used and to it different concentrations of Carbopol -934P ware added (0.1 to 0.6%). The bioavailability of a drug and its therapeutic effectiveness are often influenced by route of administration. The drug delivery system through nasal mucosa is a popular novel drug delivery method because mucous membranes of nasal cavity are relatively highly permeable, allowing for the rapid uptake of a drug into the localized and systemic circulation and to avoid the first pass metabolism. Many therapeutic drugs are difficult to reach the central nervous system (CNS) from the systemic blood circulation because the blood-brain barrier (BBB) and the blood-cerebrospinal fluid barrier form a very effective barrier which prevents most molecules from passing through. The prepared Insitu gel was prepared by Cold Technique and then various evaluation were done such as desirable pH, gelation forming temperature, gel melting temperature, effect of rpm in viscosity and temperature and finally in-vitro diffusion study other tests were performed to get the desired formulation which achieves for the intranasal delivery. The results revealed that as the concentration of Carbopol increases there was a decrease in the gelation temperature. pH of all the formulations were found to be within the range between 5.1-6.4 and the nasal mucosa can tolerate the above mentioned pH of the formulations. Viscosity of all the six formulation was measured in Fungilab viscometer at different RPM (12, 10, 8, 6, 4 and 2) in table no.5.12-5.16 the effect of RPM on Escitalopram in-situ gel was observed it shows that as the RPM increase the viscosity also increased while the torque was measured against the rpm. As the rpm decreased the torque value is also decreased so, gel is converts from Newtonic to non- Newtonian behavior. The Kinetic studies of all the formulation „r‟ value of Zero order kinetic were the ranges from 0.950-0.991 to; similarly the „r‟ First order kinetic were ranges from 0.965-0.976; Huguchi matrix „r‟ range from 0.982 – 0.950; Kosmeyer peepes „n‟ 0.988 – 0.950. It is found that formulation F1 which is containing Carbopol-934P (0.1%) shows 94.05% drug releases (shows the highest release) in 4hrs.Hences formulation F1 was found to be most optimized formulation. From the kinetic models it is observed that the Huguchi model is dominant for the release of Escitalopram oxalate from in-situ gel and the mechanism of release is non-fickian. Intranasal drug delivery through nasal mucosa has been reported as an emerging tool to improve bioavailability of many CNS drugs. The biopolymers used and their compositions in the in-situ gels preparation greatly affected the drug release which allows absorption in the nasal mucosa.

Keywords: Nasal in-situ gel, Poloxamer F188, Carbopol-934P, Escitalopram oxalate.