Abstract
The present study describes the preparation and evaluation of a poloxamer 407 (P407)-based thermoreversible gel using Carbopol 934P (C934P) as a mucoadhesive polymer and hydroxypropyl-β-cyclodextrin (HP-β-CD) for enhancing the aqueous solubility and intranasal absorption of fexofenadine hydrochloride (FXD HCl). The prepared gels were characterized by gelation temperature, viscoelasticity, and drug release profile. Thermoreversibility of P407/C934P gel was demonstrated by rheological studies. The incorporation of carbopol into P407 gel also reduced the amounts of drug released from the gel formulations (p < 0.05). In vivo pharmacokinetic results of the prepared gel formulations in rabbits (at 0.5 mg/kg dose) showed that the relative bioavailability of drug from P407/C934P gel was 11.3 and 2.7-fold higher than those of drug solution and P407 gel group, respectively. These findings suggested that developed thermoreversible gels could be used as promising dosage forms to improve intranasal drug absorption.
Highlights
Intranasal (IN) delivery has often considered as an alternative to the intravenous route for diverse therapeutic compounds [1]
The nasal cavity temperature is around 34 °C [25], we aimed at preparing poloxamer 407 (P407)-based thermoreversible gel that might be in a gel state in the range of 25 to 34 °C and a liquid state below
Shear-thinning behavior was observed in the profile of the developed thermoreversible gel (P407/Carbopol 934P (C934P) gel) and the fluidity was increased as the shear rate was increased
Summary
Intranasal (IN) delivery has often considered as an alternative to the intravenous route for diverse therapeutic compounds [1]. Aqueous solutions do not serve well as IN formulations because they provide low bioavailability due to fast drug clearance by ciliary movements in the nasal cavity [2]. The thermogelling phenomenon is completely reversible and can be characterized by the transition between sol and gel. This temperature, the solution becomes a semi-solid form while it remains as a liquid state below that temperature. This study investigated a thermoreversible gel formulation for IN delivery of FXD HCl, using P407 as a thermoreversible polymer, carbopol (C934P) as a mucoadhesive polymer and gelling agent, and hydroxypropyl-β-cyclodextrin (HP-β-CD) as a solubilizing agent and permeation enhancer. The developed thermoreversible gels were assessed by an in vivo pharmacokinetic study in rabbits
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