Formulation and In Vitro Evaluation of Acyclovir Mucoadhesive Microspheres for Intravaginal Application Acyclovir Mucoadhesive Microspheres
Iranian Journal of Pharmaceutical Sciences,
Vol. 10 No. 3 (2014),
1 Tir 2014
,
Page 35-46
https://doi.org/10.22037/ijps.v10.40813
Abstract
https://doi.org/10.22034/IJPS.2014.15252
The purpose of the research was to formulate microspheres of acyclovir (ACV) using mucoadhesive polymers, sodium alginate and chitosan. Calcium chloride was used as the ionotropic gelling agent. Sodium alginate was crosslinked by calcium chloride leading to a slower release of the drug. Chitosan which is a cationic polymer interacted with sodium alginate, an anionic polymer, to form an interpolymer complex, which also slowed the release and improved the mucoadhesion. Prior to the formulation, drug: excipient compatibility study was carried out for 12 weeks at 40 ºC ± 2 ºC /75% RH ± 5 RH. Then, FTIR was recorded to check for any chemical degradation of the drug ACV. The morphological properties, the drug encapsulation efficiency, the drug release profile and the ex vivo mucoadhesion strength were investigated. Based on these studies, P8 was found to be the best formulation. P8 had a % cumulative drug release (CDR) of 100.81% at the end of 12 h. High encapsulation efficiency of 80.92% and smaller average particle size of 596.74 μm further favored its selection as the best formulation. P8 followed Higuchi model. Further, SEM of P8 was recorded. Accelerated stability study of P8 for 6 months at 40 ºC ± 2 ºC /75% ± 5% RH indicated that it was stable.
- Acyclovir
- Chitosan
- Intravaginal
- Microsphere
- Mucoadhesive
- Topical
How to Cite
References
[2] O’Neil MJ. The Merck Index: An encyclopedia of chemicals, drugs, and biologicals, 14th ed., Merck & Co., Inc: USA (2006).
[3] Hayden FG. Antiviral agents. In: Hardman JG, Limbird LE, editors. Goodman & Gilman's The Pharmacological Basis of Therapeutics, 9th ed., McGraw-Hill, USA (1996) 1195.
[4] Celum C, et al. Effect of aciclovir on HIV-1 acquisition in herpes simplex virus 2 seropositive women and men who have sex with men: a randomised, double-blind, placebo-controlled trial. Lancet (2008) 371(9630):2109-2119.
[5] FDA Center for Drug Evaluation and Research. Microbiology review(s) [Internet]. Maryland: USFDA; 2013 [cited 2015 April 06]. Available from: http://www.accessdata.fda.gov/drugsatfda_docs/nda/2013/203791Orig1s000MicroR.pdf
[6] Mathiowitz E, Chickering D, Jacob JS, Santos C. Bioadhesive drug delivery systems. Mathiowitz E (Ed) In: Encyclopedia of Controlled Drug Delivery, Wiley, New York (1999) 9–44.
[7] Smart JD. The basics and underlying mechanisms of mucoadhesion. Adv Drug Deliv Rev (2005) 57:1556 – 1568.
[8] Shaikh R, Raj Singh TR, Garland MJ, Woolfson AD, Donnelly RF. Mucoadhesive drug delivery systems. Journal of Pharmacy and Bioallied Sciences (2011) 3(1):89-100. doi:10.4103/0975-7406.76478.
[9] Khonsari F, Zakeri-Milani P, Jelvehgari M. Formulation and Evaluation of in-vitro characterization of Gastric-mucoadhesive microparticles/discs containing metformin hydrochloride. IJPR (2014) 13(1):67-80.
[10] Aslani A, Ghannadi A, Najafi H. Design, formulation and evaluation of a mucoadhesive gel from Quercus brantii L. and coriandrum sativum L. as periodontal drug delivery. Advanced Biomedical Research (2013) 2:21.
[11] Gavini E, Vanna S , Juliano C , Bonferoni Giunchedi P. Mucoadhesive vaginal tablets as veterinary delivery system for the controlled release of an antimicrobial drug acriflavine. AAPS PharmSci (2002) 3(3):1-7
[12] Lim ST, Martin GP, Berry DJ, Brown MB. Preparation and evaluation of the in vitro drug release properties and mucoadhesion of novel microspheres of hyaluronic acid and chitosan. J Control Release (2000)66:281-292.
[13] Adrianov AK, Chen J, Payne LG. Preparation of hydrogel microspheres by coacervation of aqueous polyphosphazene solutions. Biomaterials (1998) 19:109-112.
[14] Bruschi ML, Cardoso MLC, Lucchesi MB, Gremião MPD. Gelatin microparticles containing propolis obtained by spray-drying technique: preparation and characterization. Int J Pharm (2003) 264:45-55.
[15] Avadi MR, Sadeghi AMM, Mohammadpour N, Abedin S, Atyabi F, Dinarvand R, Tehrani MR. Preparation and characterization of insulin nanoparticles using chitosan and Arabic gum with ionic gelation method. Nanomedicine NBM (2010) 6:58-63.
[16] Yan XL, Khor E, Lim LY. Chitosan-alginate films prepared with chitosans of different molecular weights. J Biomed Mater Res (2001) 58: 358–365.
- Abstract Viewed: 287 times
- IJPS_Volume 10_Issue 3_Pages 35-46 Downloaded: 244 times