Carbopol-incorporated thermoreversible gel for intranasal drug delivery.
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.
College of Pharmacy, Hanyang University, Ansan 426-791, Korea. prabagarb@gmail.com.
Prabagar
P
Balakrishnan
Department of Organic Material Science & Engineering, Pusan National University, Busan 609-735, Korea. ek31004@hanmail.net.
Eun-Kyoung
EK
Park
College of Pharmacy and Research Institute of Pharmaceutical Sciences, Seoul National University, Seoul 151-742, Korea. saintck@naver.com.
Chung-Kil
CK
Song
College of Pharmacy, Kangwon National University, Chuncheon 200-701, Korea. hjko@kangwon.ac.kr.
Hyun-Jeong
HJ
Ko
College of Veterinary Medicine and Institute of Veterinary Science, Kangwon National University, Chuncheon 200-701, Korea. twhahn@kangwon.ac.kr.
Tae-Wook
TW
Hahn
Department of Organic Material Science & Engineering, Pusan National University, Busan 609-735, Korea. kwsong@pusan.ac.kr.
Ki-Won
KW
Song
College of Pharmacy, Kangwon National University, Chuncheon 200-701, Korea. hjcho@kangwon.ac.kr.
Hyun-Jong
HJ
Cho
D000073738:2-Hydroxypropyl-beta-cyclodextrin; D000179:Acrylates / Q000008:administration & dosage / Q000737:chemistry*; D000268:Adhesiveness; D000281:Administration, Intranasal; D000818:Animals; D001682:Biological Availability; D016503:Drug Delivery Systems; D005782:Gels / Q000737:chemistry*; D039563:Histamine H1 Antagonists, Non-Sedating / Q000008:administration & dosage* / Q000493:pharmacokinetics; D020442:Poloxamer / Q000008:administration & dosage / Q000737:chemistry; D011817:Rabbits; D012212:Rheology; D016593:Terfenadine / Q000008:administration & dosage / Q000031:analogs & derivatives* / Q000493:pharmacokinetics; D014018:Tissue Distribution; D014783:Viscosity; D047392:beta-Cyclodextrins / Q000008:administration & dosage / Q000737:chemistry
D000179:Acrylates; D005782:Gels; D039563:Histamine H1 Antagonists, Non-Sedating; D047392:beta-Cyclodextrins; D020442:Poloxamer; D000073738:2-Hydroxypropyl-beta-cyclodextrin; D016593:Terfenadine; C093230:fexofenadine; C453622:carbopol 934P