FORMULATION AND EVALUATION OF PREDNISOLONE PROLIPOSOMAL GEL FOR EFFECTIVE TOPICAL PHARMACOTHERAPY
Abstract
The present objective for the study was to prepare proliposomal gel bearing a steroidal anti-inflammatory agent, prednisolone intended for topical application. Various proliposome formulations were prepared using thin film hydration technique by varying the lipid phase composition (lecithin/cholesterol). Proliposome formulations were characterized for drug content, entrapment efficiency, surface morphology, surface charge, FTIR and stability studies. Topical proliposomal gels were prepared by incorporation of proliposome into strusctured vehicle carbopol (2%). Alternatively, hydrogels containing prednisolone were prepared and their drug release properties were investigated. Pharmacodynamic activity was also determined for optimized proliposomal gel and was compared with commercial marketed gel. A spherical shape of reconstituted prednisolone liposome with an average vesicle about 2~6μm was observed in photomicrographs. The percentage entrapment of drug was increased with increase in phospholipid composition in the range of 85-98%. FTIR studies showed no possible drug-excipient interaction. Proliposomal gel showed prolonged release of prednisolone than the hydrogels. Anti-inflammatory activity proliposomal gel showed maximum percentage of inhibition of edema 60% when compared to commercial marketed gel 55%. Stability studies indicated that product is stable and should be stored at low temperatures. Proposed prednisolone proliposomal gel showed sustains release with enhanced anti inflammatory activity implicating its potential in effective topical pharmacotherapy for the treatment of rheumatoid arthritis.
Keywords:
Prednisolone, Proliposome, Anti-inflammatory, Rheumatoid arthritis, Transdermal deliveryDOI
https://doi.org/10.25004/IJPSDR.2012.040107References
2. Grahame R. Transdermal non steroidal anti-inflammatory agent’s. J. Clinical Practice 1995; 49 (1): 33-5.
3. Vaile JH, Davis P. Topical NSAIDs for musculoskeletal conditions: a review of the literature. Drugs 1998; 56 (5):783-99.
4. Heyneman CA. Topical non steroidal anti-inflammatory drugs for acute soft tissue injuries. Ann Pharmacotherapy 1995; 29 (7):22-25.
5. American College of Rheumatology Ad Hoc Committee on Clinical Guidelines. Treatment and management of rheumatoid arthritis. Arthritis Rheum 1996; 39 (5):713-722.
6. Schumacher HR. Classification of the rheumatic diseases. In: Schumacher Jr HR, editor. Primer on the rheumatic diseases.10th ed. Atlanta (GA): Arthritis Foundation, 1993; 2(1): 2-6.
7. Paulus HE, Bulpitt KJ. Nonsteroidal anti-inflammatory agentsand corticosteroids. In: Schumacher Jr HR, editor. Primer on the rheumatic diseases. 10th ed. Atlanta (GA): Arthritis Foundation, 1993; 1(2):298-303.
8. Boh LE. Osteoarthritis. In: DiPiro JT, Talbert RL, Yee GC, et al., editors. Pharmacotherapy: a path physiological approach. 4th ed. Norwalk (CT): Appleton & Lange, 1999; 3(2):1441-59.
9. Bagge E, Brooks P. Osteoarthritis in older patients: optimum treatment. J. drugs and pharmacology 1995; 7 (3):176-83.
10. Biundo JJ. Regional rheumatic pain syndromes. In: Schumacher Jr HR, editor. Primer on the rheumatic diseases. 10th ed. Atlanta (GA): J. Arthritis Foundation, 1993; 2(1):277-87.
11. Eccles M, Freemantle N, Mason J. North of England evidence based guideline development project: summary guideline for non-steroidal anti-inflammatory drugs versus basic analgesia in treating the pain of degenerative arthritis. J. BMJ 1998; 2(1):526-30.
12. Schnitzler TJ. Osteoarthritis treatment update: minimizing pain while limiting patient risk. J. post grad Med 1993; 93(1):89-92.
13. Hochberg, Altman RD, Brandt KD, et al. Guidelines for the medical management of osteoarthritis: part II. Osteoarthritis of the knee. Arthritis Rheum 1995; 3(8):1541-6.
14. Mallesh K, Diwan PV. Estimation of Prednisolone in Proliposomal formulation using RP-HPLC method. In. J. research in Pharma and biomedical sciences 2011; 2 (4):1663-1669.
15. Ahniah BK, Kim SK, Shim CK, Arien A, Dupuy B. Preparation and evaluation of encapsulation of calcitonin in lipoproteins. Journal of microencapsulation 1995; 12 (4):363–375.
16. Chung BK, Chung, Shim. Proliposomes as prolonged intranasal drug delivery systems. STP Pharma Sci. 2002; 12 (1):33–38.
17. Katare OP, Vyas SP, Dixit VK. Proliposomes of indomethacin for oral administration. J. Biochim. Biophys. Acta 1985; 817 (1):67–74.
18. Katare OP, Vyas SP, Dixit VK. Preparation and performance evaluation of plain proliposome systems for cytomembrane proteins. J. microencapsulation.1991; 8 (3):295-300.
19. Noh YC. Proliposome as a delivery system for poorly water-soluble drugs. J. microencapsulation 1984; 1(2):105-112.
20. Gupta V, Barupal AK, Ramteke S. Formulation, development and in vitro characterization of proliposomes for topical delivery of acelofenac. Indian Journal of Pharmaceutical Sciences 2010; 70(6):768-775.
21. Chen QI, Huang YU, Gu XQ Qi-neng. A study on preparation of proliposomes by spray drying method. J. Shenyang pharm univ. 1997; 1(4):166-9.
22. Bhatia A, Kumar R, Katare OP. Tamoxifen in topical liposomes: development, characterization and in-vitro evaluation. J. Pharm. Pharmaceut. Sci., 2004; 7 (2):252-259.
23. Higuchi WI. Analysis of data on the medicament release from ointments. J. Pharm. Sci. 1962; 5(1):802-803.
24. Ansel HC, Popovic NC, Allen LN. Novel approach transdermal release. Journal of Pharmaceutical dosage forms and drug delivery systems 1995; 3(1):65-63.
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