Carbopol-Incorporated Thermoreversible Gel for Intranasal Drug Delivery

Abstract

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.

In Situ Hydrogel-Forming/Nitric Oxide-Releasing Wound Dressing for Enhanced Antibacterial Activity and Healing in Mice with Infected Wounds

“…The rheological properties of the hydrogel-form of NO/GP were evaluated as previously reported, with some modification [27,28,29]. The steady shear and dynamic viscoelastic properties of the hydrogel-form of NO/GP were measured using a strain-controlled rheometer (Advanced Rheometric Expansion System [ARES], Rheometric Scientific, Piscataway, NJ, USA) equipped with a parallel-plate fixture with a radius of 12.5 mm and a gap size of 1.0 mm.…”

Bimatoprost loaded nanovesicular long-acting sub-conjunctival in-situ gelling implant: In vitro and in vivo evaluation

“…The sol-gel transition of combination of P407 with various viscolysing polymers was determined by inverting the test tube at 180 o at increasing temperatures of 1 o C step size [30]. The vials with 0.5 ml formulation were immersed for 1 min, in a water bath at each temperature, and observations were made.…”

“…Though widely employed as gelling agents poloxamers are limited by their weak mechanical strength, which can result in rapid erosion [43]. Hence, we presently used a blend of poloxamer [40] and other polymers like carbopol 934 P [30,44], HPMC [45], CMC [42], poloxamer 188 and chitosan [46] (Table 1). P407 showed a suitable in-situ gelling behavior between 37.5-39 o C when used alone at 20% w/v concentration [42].…”

“…However when mixed with vesicles the gelling temperature increased to ≥38 o C. Latter was probably due to the traces of ethanol present in the NV dispersion [39]. A blend of P407 with carbopol 934P (F12-F16; Table 1) showed a good insitu gelling behavior at 37±0.5 o C. Carbopol, a mucoadhesive polymer not only increases the mechanical strength of the formulation but also shows improved surface contact with the ocular tissues [30]. The formulation F 16 was selected as the best suitable option.…”

Formulation and Evaluation of Eudragit RL-100 Nanoparticles Loaded In-Situ Forming Gel for Intranasal Delivery of Rivastigmine

“…However, a thermoreversible hydrogel formulation of drug is more feasible and convenient for the intranasal medication, as it is a liquid at room temperature and turns into a gel at body temperature. 13 PF-127 can be applied to prepare the in-situ hydrogel forming systems. 14 PF-127 aqueous solution within a certain range of concentration forms a liquid at room or lower temperatures, but spontaneously forms a non-flowing gel at body temperature.…”