Preparation and Evaluation of Bioadhesive Inserts Containing Verapamil Hydrochloride for Nasal Delivery

Yenil O., Kahraman E., Algin Yapar E., Cevher E., Ozkirimli S., Ozsoy Y.

LATIN AMERICAN JOURNAL OF PHARMACY, cilt.32, sa.8, ss.1170-1177, 2013 (SCI-Expanded) identifier identifier

  • Yayın Türü: Makale / Tam Makale
  • Cilt numarası: 32 Sayı: 8
  • Basım Tarihi: 2013
  • Dergi Adı: LATIN AMERICAN JOURNAL OF PHARMACY
  • Derginin Tarandığı İndeksler: Science Citation Index Expanded (SCI-EXPANDED), Scopus
  • Sayfa Sayıları: ss.1170-1177
  • İstanbul Üniversitesi Adresli: Evet

Özet

Verapamil HCl is an antihypertensive agent which have a low oral bioavailability (20-35%) due to its high first pass metabolism. The objective of the present study is to develop a verapamil HCl nasal insert of which would enable to improve the bioavailability and prolonged release of drug. As a result of textural analyses, sodium alginate gel was chosen to fabricate nasal inserts. In vitro drug release studies performed on Franz-diffusion cell showed that nasal insert gave prolonged drug release which was fitted to Higuchi kinetic model. PEG 400 was used as a penetration enhancer in formulation to increase the release of drug from insert. Ex vivo permeation studies with excised bovine nasal mucosa were carried out on inserts (with or without PEG 400). Ex vivo studies showed that PEG 400 increased the release of verapamil significantly. As a result, nasal inserts may be an alternative of oral route.

Verapamil HCl is an antihypertensive agent which have a low oral bioavailability (20-35%) due to its high first pass metabolism. The objective of the present study is to develop a verapamil HCl nasal insert of which would enable to improve the bioavailability and prolonged release of drug. As a result of textural analyses, sodium alginate gel was chosen to fabricate nasal inserts. In vitro drug release studies performed on Franz-diffusion cell showed that nasal insert gave prolonged drug release which was fitted to Higuchi kinetic model. PEG 400 was used as a penetration enhancer in formulation to increase the release of drug from insert. Ex vivo permeation studies with excised bovine nasal mucosa were carried out on inserts (with or without PEG 400). Ex vivo studies showed that PEG 400 increased the release of verapamil significantly. As a result, nasal inserts may be an alternative of oral route.