A novel vaginal drug delivery system: anti-HIV bioadhesive film containing abacavir

  • Kajal Ghosal
  • Alok Ranjan
  • Benoy Brata Bhowmik


Women are very much susceptible for acquired immunodeficiency syndrome (AIDS) and other sexually transmitted diseases (STDs), mainly due to unprotected heterosexual vaginal intercourse and for some other social and economical disadvantages. Our aim was to formulate and optimize vaginal film of abacavir, a potent nucleoside reverse transcriptase inhibitor, for the treatment of AIDS and HIV. Abacavir films were prepared by solvent evaporation method using sodium alginate (Na-alginate) as the main polymer, Hydroxypropyl Methylcellulose E 15 (HPMC E 15) as the copolymer and glycerol as a humectant. Abacavir sulphate (ABC) was used here as a drug. Films were optimized for various physicochemical parameters such as tensile strength, % elongation at break, swelling capacity, drug content (mg/cm2), thickness, folding endurance, bioadhesion, pH, moisture content and SEM. Drug polymer interaction was studied by FTIR Spectra. The drug release study was accomplished in dissolution apparatus. In vivo study was also carried out. This newly formed film was one kind of sustain release type and can be considered as a novel drug carrier system for the treatment of AIDS and other STDs. It was suitable for local as well as systemic effect. The films showed good physicochemical property with good aesthetic appeal.


Human Immunodeficiency Virus High Performance Liquid Chromatography Alginate Drug Release Acquire Immune Deficiency Syndrome 
These keywords were added by machine and not by the authors. This process is experimental and the keywords may be updated as the learning algorithm improves.


  1. 1.
    World Health Organization, AIDS epidemic update global overview, 2009:1–50. Accessed 21 Sept 2010.
  2. 2.
    Merabet J, Thompson D, Levinson SR. Advancing vaginal drug delivery. Expert Opin Drug Delivery. 2005;2:769–77.CrossRefGoogle Scholar
  3. 3.
    Alexander NJ, Baker E, Kaptein M, Karck U, Miller L. Why consider vaginal drug administration. Fertil Steril. 2004;82:1–12.CrossRefGoogle Scholar
  4. 4.
    Goh YF, Shakir I, Hussain R. Electrospun fibers for tissue engineering, drug delivery, and wound dressing. J Mater Sci. 2013;48(8):3027–54.CrossRefGoogle Scholar
  5. 5.
    Agashe H, Hu M, Rohan L. Formulation and delivery of microbicides. Curr HIV Res. 2012;10(1):88–96.CrossRefGoogle Scholar
  6. 6.
    Machado RM, Palmeira-De-Oliveira A, Martinez-De-Oliveira J, Palmeira-De-Oliveira R. Vaginal films for drug delivery. J Pharm Sci. 2013;102(7):2069–78.CrossRefGoogle Scholar
  7. 7.
    Tasoglu S, Rohan LC, Katz DF, Szeri AJ. Transient swelling, spreading, and drug delivery by a dissolved anti-HIV microbicide-bearing film. Phys Fluids. 2013;25(3):031901–90.CrossRefGoogle Scholar
  8. 8.
    Sassi AB, Cost MR, Hillier SL, Rohan LC. Permeability of tritiated water through human cervical and vaginal tissue. J Pharm Sci. 1993;10:2009–16.Google Scholar
  9. 9.
    Garg S, Tambwekar KR, Vermani K, Garg A, Waller DP. Development pharmaceutics of microbicide formulations. Part II: formulation, evaluation, and challenges. AIDS Patient Care STDS. 2003;17:377–99.CrossRefGoogle Scholar
  10. 10.
    Das MK, Ahmed AB. Formulation and ex vivo evaluation of rofecoxib gel for topical application. Acta Pol Pharm. 2007;64:461–7.Google Scholar
  11. 11.
    Ganesh S, Radhakrishnan M, Ravi M, Prasannakumar B, Kalyani J. In vitro evaluation of the effect of combination of hydrophilic and hydrophobic polymers on controlled release from Zidovudine matrix tablets. Indian J Pharm Sci. 2008;70:461–5.CrossRefGoogle Scholar
  12. 12.
    Ghosal K, Rajabalaya R, Chakraborty S, Nanda A. Formulation and characterization of both hydrophilic and hydrophobic HPMC based hydrogels containing diclofenac potassium. Latin Am J Pharm. 2010;29:1137–43.Google Scholar
  13. 13.
    McConville C, Friend DR, Clark MR, Malcolm K. Preformulation and development of an once-daily sustained-release tenofovir vaginal tablet tablet containing a single excipient. J Pharm Sci. 2013;102(6):1859–68.CrossRefGoogle Scholar
  14. 14.
    Morales JO, Ross AC, McConville JT. Protein-coated nanoparticles embedded in films as delivery platforms. J Pharm Pharmacol. 2013;65(6):827–38.CrossRefGoogle Scholar
  15. 15.
    Najafi RB, Eghbali M, Keyvanpour M, Mirzaei HR. Preparation and physicochemical evaluation of Nystatine mucoadhesive buccal film. J Rep Pharm Sci. 2013;2(1):25–31.Google Scholar
  16. 16.
    Bassi P, Kaur G. Innovations in bioadhesive vaginal drug delivery system. Expert Opin Ther Pat. 2012;22(9):1019–32.CrossRefGoogle Scholar
  17. 17.
    Guirguis, OW, Moselhey MTH. Optical study of poly(vinyl alcohol)/hydroxypropyl methylcellulose blends. J Mater Sci. 2011;46(9):5775–89.Google Scholar
  18. 18.
    Genç L, Büyüktıryakı S. Preparation and characterization of methotrexate-loaded microcapsules. Pharm Dev Technol. 2013;19(1):42–7.CrossRefGoogle Scholar
  19. 19.
    Tasdighi E, Azar ZJ, Mortazavi SA. Development and in vitro evaluation of a contraceptive vagino-adhesive propranolol hydrochloride gel. Iran J Pharm Res. 2012;11(1):13–26.Google Scholar
  20. 20.
    Swain S, Behera A, Beg S, Patra CN, Dinda SC, Sruti J, Rao ME. Modified alginate beads for mucoadhesive drug delivery system: an updated review of patents. Recent Pat Drug Deliv Formul. 2012;6(3):259–77.CrossRefGoogle Scholar
  21. 21.
    Kulkarni AR, Soppimath KS, Aminabhavi TM, Rudzinski WE. In vitro release kinetics of cefadroxil, loaded sodium alginate interpenetrating network beads. Eur J Pharm Biopharm. 2001;51:127–33.CrossRefGoogle Scholar
  22. 22.
    Sriamornsak P, Thirawong N, Putkhachorn S. Morphology and buoyancy of entrapped calcium pectinate gel beads. AAPS J. 2004;6:1–7.CrossRefGoogle Scholar
  23. 23.
    Duchene D, Touchard F, Peppas NA. Pharmaceutical and medical aspects of bioadhesive systems for drug administration. Drug Dev Ind Pharm. 1998;14:283–318.CrossRefGoogle Scholar
  24. 24.
    Ghosal K, Ray SD. Alginate/hydrophobic HPMC (60 M) particulate systems: new matrix for site-specific and controlled drug delivery. Braz J Pharm Sci. 2011;47(4):833–44.CrossRefGoogle Scholar
  25. 25.
    Ray SD, Ghosal K, Ghosal I, Ghosh D. Alginate/hydrophobic HPMC (60 L) particulate systems: new matrix for controlled release of diclofenac potassium. Lat Am J Pharm. 2011;30(5):945–51.Google Scholar
  26. 26.
    Saag MS, Sonnerborg A, Torres RA, Lancaster D, Gazzard BG, Schooley RT, Romero C, Kelleher D, Spreen W, LaFon S. Antiretroviral effect and safety of abacavir alone and in combination with zidovudine in HIV-infected adults. AIDS. 1998;12(16):F203–9.CrossRefGoogle Scholar
  27. 27.
    Gray LR, Tachedjian G, Ellett AM, Roche MJ, Cheng WJ, Guillemin GJ, Brew BJ, Turville SG, Wesselingh SL, Gorry PR, Churchill MJ. The NRTIs lamivudine, stavudine and zidovudine have reduced HIV-1 inhibitory activity in astrocytes. PLoS ONE. 2013;8(4):e62196.CrossRefGoogle Scholar
  28. 28.
    Garg S, Vermani K, Garg A, Anderson RA, Rencher WB, Zaneveld LJ. Development and characterization of bioadhesive vaginal films of sodium polystyrene sulfonate (PSS), a novel contraceptive antimicrobial agent. Pharm Res. 2005;22:584–95.CrossRefGoogle Scholar
  29. 29.
    Dobaria NB, Badhan AC, Mashru RC. A novel itraconazole bioadhesive film for vaginal delivery: design, optimization, and physicodynamic characterization. AAPS Pharm Sci Tech. 2009;10:951–9.CrossRefGoogle Scholar
  30. 30.
    Dhanikula AB, Panchagnula R. Development and characterization of biodegradable chitosan films for local delivery of Paclitaxel. AAPS J. 2004;6(3):88–99.CrossRefGoogle Scholar
  31. 31.
    Parodi B, Rasso R. Development and characterization of buccoadhesive dosage form of oxycodone hydrochloride. Drug Dev Ind Pharm. 1996;22:445–50.CrossRefGoogle Scholar
  32. 32.
    Shilpa K, Poddar S. Design of mucoadhesive vaginal metronidazole films. Acta Pharm Sci. 2010;52:181–9.Google Scholar
  33. 33.
    Subrahmanyam CV. Essentials of physical pharmacy. Vallabh Prakashan, India 1st edn. 2003; p. 315–317.Google Scholar
  34. 34.
    Shi S, Wang XH, Guo G, Fan M, Huang MJ, Qian ZY. Preparation and characterization of microporous poly (d,l-lactic acid) film for tissue engineering scaffold. Int J Nanomedicine. 2010;5:1049–55.Google Scholar
  35. 35.
    Thimmasetty J, Pandey G, Babu P. Design and in vivo evaluation of carvedilol buccal mucoadhesive patches. Pak J Pharm Sci. 2008;21(3):241–8.Google Scholar
  36. 36.
    Vyas SP, Khar RK. Controlled drug delivery. Vallabh Prakashn, India 1st edn. 2002; p. 258–292.Google Scholar
  37. 37.
    Rohan LC, Sassi AB. Vaginal drug delivery systems for HIV prevention. AAPS J. 2009;11(1):78–87.CrossRefGoogle Scholar
  38. 38.
    Li J, David B, Holly H, Sid K. In vitro drug release study of methacrylate polymer blend system: effect of polymer blend composition, drug loading and solubilizing surfactants on drug release. J Mater Sci Mater Med. 2010;21(2):583–8.CrossRefGoogle Scholar
  39. 39.
    Irwin CR, McCullough KC, Jones DS. Chlorhexidine-containing mucoadhesive polymeric compacts designed for use in the oral cavity: an examination of their physical properties, in vitro/in vivo drug release properties and clinical acceptability. J Mater Sci Mater Med. 2003;14(10):825–32.CrossRefGoogle Scholar
  40. 40.
    Chatterjee A, Kumar L, Bhowmik BB, Gupta A. Microparticulated anti-HIV vaginal gel: in vitro-in vivo drug release and vaginal irritation study. Pharm Dev Technol. 2010;16(5):466–73.CrossRefGoogle Scholar
  41. 41.
    Hedaya MA. Noncompartemental approach to pharmacokinetic data analysis. In: Basic pharmacokinetics, 2nd edn. New York: CRC Press; 2012. p. 228–231.Google Scholar

Copyright information

© Springer Science+Business Media New York 2014

Authors and Affiliations

  • Kajal Ghosal
    • 1
  • Alok Ranjan
    • 1
  • Benoy Brata Bhowmik
    • 1
  1. 1.Dr. B.C. Roy College of Pharmacy and Allied Health ScienceDurgapurIndia

Personalised recommendations