FORMULATION AND EVALUATION OF WOUND HEALING ACTIVITY OF LINEZOLID TOPICAL PREPARATIONS ON DIABETIC RATS
Objective: The aim of the study is to formulate and evaluate the topical preparations of antibacterial formulation for the treatment of diabetic wound infection.
Methods: Different types of topical formulations were prepared and evaluated for in vitro release. The prepared formulations were also tested for its antibacterial activity against the pathogens existing in diabetic wound infection. Based on in vitro drug release and antimicrobial activity, two formulations were selected as optimized formulations. Optimized formulations were tested for wound healing activity in diabetic rats.
Results: Based on in vitro drug release and antimicrobial activity two formulations (F8, F10) were selected as optimized formulations. FTIR studies of pure drug and optimized formulation shown absence of any incompatibility between drug and excipients. Optimized formulation shown good physicochemical properties and passed short-term stability study. F8 and F10 formulations were applied to untreated diabetic rats for diabetic wound infection, the rate of wound healing was quite faster. These results indicate that the linezolid semisolid dosage form could provide an adjunctive antimicrobial formulation for the management of diabetic wounds.
Conclusion: Further studies are required on chronic diabetic wounds with and without diabetic medications to confirm its effectiveness.
Keywords: Staphylococcus aureus, Linezolid, Semisolid dosage forms, Wound healing activity
2. Bengalorkar GM, Kumar Tayur Nagendra. Diabetic foot infectionsâ€“a review. Int J Biol Med Res 2011;2:453-60.
3. Snir N, Meron-Sudai S, Deshmukh A, Dekel S, Ofek I. Antimicrobial properties and elution kinetics of linezolid from polymethylmethacrylate. Orthopedics 2013;36:1412-7.
4. Indian Pharmacopoeia. Indian Pharmacopoeia Commission; 2007.
5. Manikandan M, Kannan K, Manavalan R. Compatibility studies of camptothecin with various pharmaceutical excipients used in the development of nanoparticle formulation. Int J Pharm Pharm Sci 2013;5:315-21.
6. Jadhav Ravindra, Patil Pratibha R, Payal Hasmukhlal Patil. Formulation and evaluation of semisolid preparation (Ointment, Gel and Cream) of thiocolchicoside. J Pharm Biomed Sci 2011;8:1-6.
7. Prabhjotkaur, Loveleenpreetkaur, Khan MU. Topical formulations and Hydrogel: an overview. Int J Adv Pharm Biol Chem 2013;2:201-6.
8. Bazigha K Abdul Rasool, Eman F Abu-Gharbieh, Sahar A Fahmy, Heyam S Saad, Saeed A Khan. Development and evaluation of ibuprofen transdermal gel formulations. Trop J Pharm Res 2010;9:355-63.
9. Dheeraj T Baviskar, Yogeshkumar A Biranwar, Kapil R Bare, Venkatesh B Parik, Mangesh K Sapate, Dinesh K Jain. In vitro and in vivo evaluation of diclofenac sodium gel prepared with cellulose ether and carbopol 934P. Trop J Pharm Res 2013;12:489-94.
10. Jennifer M. Andrews, BSAC standardized disc susceptibility testing method. The British Society for Antimicrobial Chemotherapy; 2001.
11. AL Barry, MB Coyle, C Thornsberry, EH Gerlach, RW Hawkinson. Methods of measuring zones of inhibition with the bauer-kirby disk susceptibility test. J Clin Microbiol 1979;10:885â€“9.
12. Qiuxi Fan, Mark Mitchnick, Andrew Loxley. The issues and challenges involved in in vitro release testing for semi-solid formulations. Drug Delivery Technol 2007;7:62-6.
13. Akbarzadeh A, Norouzian D, Mehrabi M, Jamshidi S, Farhangi A, Verdi A, et al. Induction of diabetes by streptozotocin in rats. Indian J Clin Biochem 2007;22:60-4.
14. Mahmoud Abu Abeeleh, Zuhair Bani Ismail, Khaled R Alzaben, Sami A Abu-Halaweh, Mohamed K Al-Essa, Jaafar Abuabeeleh, et al. Induction of diabetes mellitus in rats using intraperitoneal streptozotocin: a comparison between 2 strains of rats. Eur J Sci Res 2009;32:398-402.
15. Murthy S, Gautam M, Goel S, Purohit V, Sharma H, Goel R. Evaluation of in vivo wound healing activity of bacopa monniera on different wound model in rats. BioMed Res Int 2013;1-9. Doi.org/10.1155/2013/972028.
16. ICH. Stability testing of new drug substances and products. Available from http://www.ich.org/fileadmin/Public_Web_ Site/ICH_Products/Guidelines/Quality/Q1A_R2/Step4/Q1A_R2__Guideline.pdf. [Last accessed on 02 Aug 2015].