PREPARATION AND CHARACTERIZATION OF THERMOSENSITIVE MUCOADHESIVE IN_SITU GELS FOR NASAL DELIVERY OF ONDANSETRON HYDROCHLORIDE | ||||
| Al-Azhar Journal of Pharmaceutical Sciences | ||||
| Article 14, Volume 50, Issue 2 - Serial Number 50, September 2014, Page 191-207 PDF (1.17 MB) | ||||
| Document Type: Original Article | ||||
| DOI: 10.21608/ajps.2014.6953 | ||||
 View on SCiNiTO | ||||
| Author | ||||
| Ghada Abdel Bary | ||||
| Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Cairo University, Cairo, Egypt | ||||
| Abstract | ||||
| A nasal mucoadhesive thermo reversible in-situ gel appears very attractive since it is fluid-like prior to nasal administration and can thus easily be installed as a drop allowing accurate drug dosing. The feasibility of developing an efficacious intranasal formulation of the potent antiemetic drug Ondansetron HCL has been undertaken in this work. The ultimate goal is to circumvent the first-pass elimination of the drug when taken orally. Poloxamers P407 and P188 (20/5% w/v) were used using cold method to prepare thermo reversible gels as they have excellent thermo-sensitive gelling properties, water solubility , good drug release, low toxicity and irritation. Mucoadhesive polymers like chitosan high molecular weight (HMW), sodium carboxymethyl cellulose low molecular weight (LMW) and polyvinylpyrrolidone K30 (PVP) were used at concentration of 0.5 % (w/v) to form thermo reversible gels. Three nasal in-situ gels with desirable Tsol-gel in the range of 30-35ºC were developed. pH, mucoadhesion, rheological measurements, in vitro release and ex-vivo permeation studies were performed to evaluate the prepared gels. The incorporation of chitosan to poloxamer polymers showed significant increase in the mucoadhesion ability. The prepared gels exhibited non-Newtonian shear thinning behavior at 35ºC. Drug contents were in the range of 97.8-100.1%. The release pattern was enhanced by the PVP polymer, in opposition; chitosan and NaCMC retarded it. Concerning permeation through sheep nasal mucosa, the steady state flux (Jss) of the three formulae was found to be 3.57, 5.64 and 3.81 µg/cm2.min., respectively. No marked alteration in the histological structure of the nose epithelial cell membrane of male Wister rats after application of the formed gels was observed to confirm their safety. The bioavailability for the optimized formulation was 86.98% providing that intranasal route could be promising for Ondansetron HCL delivery. | ||||
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