In vitro and In vivo Evaluation of Propranolol Microspheres Loaded Buccal Gel

DOI:

https://doi.org/10.37285/ijpsn.2017.10.2.4

Authors

  • Gajanan J Deshmukh
  • M. Mohan Varma
  • Bhikshapathi D. V. R. N.

Abstract

The selected propranolol microsphere formulation, S6 was employed for gel formulation with a variety of polymers like Carbopol 934, HPMC and Sodium CMC by mechanical stirring method in order to develop a sustained release propranolol microspheres containing bioadhesive gel. The prepared bioadhesive gels were evaluated for pH, viscosity, %drug content, in vitro drug release studies, bioadhesion, ex vivo permeation studies, accelerated stability and in vivo bioavailability studies. From all the above studies FG3 was found to be optimized formulation. In vitro experiments indicated a sustained release of 98.92% over 12 h and an acceptable bioadhesion quality for formulation FG3. Optimized formulation was characterized for FTIR, SEM and stability studies and found to be stable. Propranolol Optimized formulation exhibited significant increased bioavailability in vivo when compared with marketed tablet. The drug release from the optimized formulation follows zero order kinetics with anomalous Non-fickian diffusion. In vivo studies revealed that Propranolol Optimized formulation FG3 exhibited significant increased bioavailability when compared with marketed product, due to reduced first pass metabolism, when it is administered by the buccal route. Hence, it can be concluded that the formulation FG3 has potential to deliver Propranolol in a controlled and constant manner for prolong period over other formulations and can be adopted for a successful delivery of propranolol for buccal use.

Downloads

Download data is not yet available.

Metrics

Metrics Loading ...

Keywords:

Propranolol HCl, buccal gel, diffusion, bioadhesion, bioavailability

Downloads

Published

2017-03-31

How to Cite

1.
Deshmukh GJ, Varma MM, D. V. R. N. B. In vitro and In vivo Evaluation of Propranolol Microspheres Loaded Buccal Gel. Scopus Indexed [Internet]. 2017 Mar. 31 [cited 2024 Jun. 20];10(2):3661-8. Available from: https://www.ijpsnonline.com/index.php/ijpsn/article/view/834

Issue

Section

Research Articles

References

Alka G., Garg S and Khar R. K. (1992). Measurement of bioadhesive strength of mucoadhesive buccal tablet: Design of an in-vitro assembly. Indian Drugs 30(4): 152-155
Basavaraj B and Devi S (2012). Antimicrobial studies of extended release amoxicillin trihydrate dental gels. Der Pharmacia Lettre; 4(1): 275-286.
Choi HG., Oh Y and Kim CK. (1998). In situ gelling and mucoadhesive liquid suppository containing acetaminophen: enhanced bioavailability, Int J of Pharm 165: 23-32.
Gajanan J Deshmukh and Mohan Varma M. (2016). Design & evaluation of propranolol hcl microspheres by ionotropic gelation method, Der Pharmacia Lettre, 8(2): 284-293.
Karthikeyan K (2012). Formulation of bioadhesive carbomer gel incorporating drug loaded gelatin microspheres for periodontal therapy. Trop J of Pharm Res 11(3): 335-343.
Palak V Patel., Dhiren J Daslaniya., Upendra L Patel and Ragin R. Shah. (2013). Formulation and Evaluation of Bioadhesive Gel Incorporated Amoxicillin Trihydrate Loaded Microspheres for Periodontal Therapy, IJPI 3; (3) 98-109.
Shojaei AH (1998). Buccal mucosa as a route for systemic drug delivery: A review. J Pharm Pharmaceutic Sci 1: 15-30.
Sudhakar Y (2006). Buccal bioadhasive drug delivery-a promising option for orally less efficient drugs. J Contro Rel 114: 15-40.
Senel S., Ikinci G., Kas S., Yousefi-Rad A., Sargon M.F and HIncal AA (2000). Chitosan films and hydrogels of chlorhexidine gluconate for oral mucosal delivery. Int. J. Pharm 193: 197-203.
Shirsand S.B., Wadageri G.V., Raju S.A and Gopi krishna Kolli (2013). Formulation and in vivo evaluation of mucoadhesive buccal tablets of carvedilol, Int J of Pharm Sci and nanotech 6(3): 2164-2171.
Patel VM., Prajapati BG., Patel HV and Patel KM. (2007). Mucoadhesive bilayer tablets of propanolol hydrochloride. AAPS Pharm Sci Tech 8: E1-6.
Yong CS., Choi JS., Quan QZ., Rhee JD., Kim CK., Lim SJ., Kim KM and Oh PS. (2001). Effect of sodium chloride on the gelation temperature, gel strength and bioadhesive force of poloxamer gels containing diclofenac sodium. Int J of Pharm 226: 195-205.

Most read articles by the same author(s)

1 2 > >>