Carbopol-Incorporated Thermoreversible Gel for Intranasal Drug Delivery

• Published in: Molecules (Basel, Switzerland) Vol. 20; no. 3; pp. 4124 - 4135
• Main Authors: Balakrishnan, Prabagar, Park, Eun-Kyoung, Song, Chung-Kil, Ko, Hyun-Jeong, Hahn, Tae-Wook, Song, Ki-Won, Cho, Hyun-Jong
• Format: Journal Article
• Language: English
• Published: Switzerland MDPI AG 04.03.2015; MDPI
• Subjects: 2-Hydroxypropyl-beta-cyclodextrin; Acrylates - administration & dosage; Acrylates - chemistry; Adhesiveness; Administration, Intranasal; Animals; Aqueous solutions; beta-Cyclodextrins - administration & dosage; beta-Cyclodextrins - chemistry; Bioavailability; Biological Availability; carbopol; Drug Delivery Systems; Drug dosages; Electronic mail systems; fexofenadine hydrochloride; Gels - chemistry; Histamine H1 Antagonists, Non-Sedating - administration & dosage; Histamine H1 Antagonists, Non-Sedating - pharmacokinetics; nasal delivery; Pharmacokinetics; Pharmacy; poloxamer; Poloxamer - administration & dosage; Poloxamer - chemistry; Polymers; Rabbits; Rheology; Terfenadine - administration & dosage; Terfenadine - analogs & derivatives; Terfenadine - pharmacokinetics; thermoreversibility; Tissue Distribution; Veterinary medicine; Viscoelasticity; Viscosity
• ISSN: 1420-3049; 1420-3049
• DOI: 10.3390/molecules20034124

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.