FORMULATION AND EVALUATION OF LYCOPENE LOADED COLLOIDAL MICROPARTICLES GEL
Objective: The objective of the present investigation was to design and evaluate a gel containing lycopene loaded colloidal microparticles.
Methods: The lycopene loaded colloidal microparticles were successfully prepared by Cloud point technique to form colloids using Tween 40 and Tween 60 surfactant solution and then incorporated into microparticles by solvent evaporation method using polymer like HPMC and ethyl cellulose. These colloidal microparticles were evaluated for particle size (PS), drug loading (DL), entrapment efficiency (EE), Scanning Electron Microscopy (SEM). Further, these colloidal microparticles were incorporated into a topical formulation i.e., gel. This topical formulation was then evaluated for macroscopic examination, viscosity, drug content, spreadability, antioxidant activity, in vitro permeation and release kinetics.
Results: Colloidal microparticles were successfully prepared and the particle size, drug loading and entrapment efficiency were found to be 249.45±14.2 μm, 49.8±0.96 % and 93.4±0.26 % respectively. FTIR study depicted no chemical interaction between pure drug lycopene and other excipients. The topical formulation showed sustained release and followed Korsmeyer-Peppas release kinetics model.
Conclusion: The sustained release topical formulation of lycopene was successfully prepared using Tween 40 and Tween 60 surfactant solution and combination of HPMC and ethyl cellulose and evaluated for several parameters.
2. Rizwan M, Rodriguez Blanco I, Harbottle A, Birch Machin MA, Watson RE, Rhodes LE. Tomato paste rich in lycopene protects against cutaneous photodamage in humans in vivo: a randomized controlled trial. Br J Dermatol 2011;164:154-62.
3. Mozos I, Stoian D, Caraba A, Malainer C, Horba?czuk JO, Atanasov AG. Lycopene and vascular health. Front Pharmacol 2018;9:521.
4. Andreassi M, Stanghellini E, Ettorre A, Di Stefano A, Andreassi L. Antioxidant activity of topically applied lycopene. J Eur Acad Dermatol Venereol 2004;18:52-5.
5. Fazekas Z, Gao D, Saladi R, Lu Y, Lebwohl M, Wei H. Protective effects of lycopene against ultraviolet b-induced photodamage. Nutr Cancer 2003;47:181-7.
6. Savjani KT, Gajjar AK, Savjani JK. Drug solubility: importance and enhancement techniques. ISRN Pharm; 2012. p. 1-10.
7. Okano T. Block copolymer design for camptothecin incorporation into polymeric micelles for passive tumor targeting. Pharm Res 2004;21:2001-8.
8. Cai S, Vijayan K, Cheng D, Lima EM, Discher DE. Micelles of different morphologies-advantages of worm-like filomicelles of PEO-PCL in paclitaxel delivery. Pharm Res 2007;24:2099-109.
9. Hofman JW, Carstens MG, Van Zeeland F, Helwig C, Flesch FM, Hennink WE. Photocytotoxicity of mTHPC (temoporfin) loaded polymeric micelles mediated by lipase catalyzed degradation. Pharm Res 2008;25:2065-73.
10. Vakil R, Knilans K, Andes D, Kwon GS. Combination antifungal therapy involving amphotericin B, rapamycin and 5 fluorocytosine using PEG-phospholipid micelles. Pharm Res 2008;25:2056-64.
11. Yang Y, Chen C, Yang J, Tsai T. Spray-dried microparticles containing polymeric micelles encapsulating hematoporphyrin. AAPS J 2010;12:138-46.
12. Bansal M, Jamil S. Micellar microparticles: a novel approach to topical drug delivery system. Int J Appl Pharm 2018;10:1-5.
13. Ta? D, Çete S. Micellar properties and antimicrobial activity of a mixed surfactant system constituted by sodium dodecyl sulfate and cetylpyridinium chloride. Indian J Pharm Educ 2017;51:580-7.
14. Sudhamani T, Reddy K, Kumar V, Ramadoss R, Ganesan V. Preparation and evaluation of ethyl cellulose microspheres of ibuprofen for sustained drug delivery. Int J Pharm Res Dev 2010;2:1-5.
15. Ganesan P, Soundararajan R, Shanmugam U, Ramu V. Development, characterization and solubility enhancement of comparative dissolution study of second generation of solid dispersions and microspheres for poorly water soluble drug. Asian J Pharm Sci 2015;10:433-41.
16. Nagendra R, Charan C, Joshi K, Jayanthi C. Preparation and evaluation of microparticles containing oxybutynin chloride for controlled release. Asian J Biomed Pharm Sci 2015;5:15-7.
17. Rai S, Ravikumar P. Development and evaluation of microsphere based topical formulation using design of experiments. Int J Pharm Sci 2016;78:182-92.
18. Kandav G, Bhatt D, Jindal D. Formulation and evaluation of allopurinol loaded chitosan nanoparticles. Int J Appl Pharm 2019;11:49-52.
19. Patel BK, Parikh RH, Aboti PS. Development of oral sustained release rifampicin loaded chitosan nanoparticles by design of an experiment. J Drug Delivery 2013;1-10. http://dx.doi.org/10.1155/2013/370938
20. Najmuddin M, Ahmed A, Shelar S, Patel V, Khan T. Floating microspheres of ketoprofen: formulation and evaluation. Int J Pharm Pharm Sci 2010;2:164-8.
21. Ararath D, Velmurugan S. Formulation and evaluation of nevirapine mucoadhesive microspheres. Int J Pharm Pharm Sci 2015;7:342-8.
22. Deshmukh M, Mohite S. Formulation and characterization of olanzepine loaded mucoadhesive microspheres. Asian J Pharm Clin Res 2017;10:249-55.
23. Girotra P, Singh SK. A comparative study of orally delivered PBCA and ApoE coupled BSA nanoparticles for brain targeting of sumatriptan succinate in the therapeutic management of migraine. Pharm Res 2016;33:1682-95.
24. Venkatesh D, Karki R, Jha S, Lakshmi A, Kumar G, Goli D. Formulation and evaluation of microspheres containing fluvastatin sodium. Int J Drug Dev Res 2012;4:306-14.
25. Chowdary K, Kumar PA. Formulation and evaluation of topical drug delivery systems of ciprofloxacin. Ind J Pharm Sci 1996;58:47-50.
26. Mura P, Faucci MT, Bramanti G, Corti P. Evaluation of transcutol as a clonazepam transdermal penetration enhancer from hydrophilic gel formulations. Eur J Pharm Sci 2002;9:365-72.
27. Patel S, Changediya B, Gadhave MV, Jadhav S, Gaikwad DD. Formulation and evaluation of diclofenac sodium gel by using carbopol. Int Res J Sci Eng 2018;3:65-8.
28. Basarkar GD, Shirsath GN, Patil SB. Development of microspheres containing diclofenac diethylamine as sustained release topical formulation. Bull Pharm Res 2013;3:14-22.
29. Mohamed MI. Optimization of chlorphenesin emulgel formulation. AAPS J 2004;6:1-7.
30. Murthy TEGK, Kishore VS. Formulation and evaluation of transdermal gels of diltiazem hydrochloride. Indian J Pharm Educ Res 2008;42:272-6.
31. Queiroz MBR, Marcelino NB, Ribeiro MV, Espindola LS, Cunha F, Silva MV. Development of gel with matricaria recutita L. extract for topic application and evaluation of physical-chemical stability and toxicity. Latt Am J Pharm 2009;28:574-9.
32. Singh S, Gajra B, Rawat M, Muthu MS. Enhanced transdermal delivery of ketoprofen from bioadhesive gels. Pak J Pharm Sci 2009;22:193-8.
33. Nandgude T, Thube R, Jaiswal N, Deshmukh P, Chatap V, Hire N. Formulation and evaluation of pH induced in situ nasal gel of salbutamol sulphate. Int J Pharm Sci Nanotechnol 2008;1:177-83.
34. Moghimipour E, Salimi A, Zadeh BSM. Effect of the various solvents on the in vitro permeability of vitamin B12 through excised rat skin. Trop J Pharm Res 2013;12:671-7.
35. Dhakar RC, Maurya SD, Saluja V. From formulation variables to drug entrapment efficiency of microspheres: a technical review. J Drug Delivery Ther 2012;2:128-33.
36. Biswal I, Dinda A, Mohanty S, Dhara M, Das D, Chowdary KA, et al. Influence of Drug/Polymer ratio on the encapsulation efficiency of highly hydrophilic drug. Asian J Chem 2011;23:1973-8.
37. Sinko PJ. Micrometrics. In: Martin A. editor. Martin's Physical Pharmacy and Pharmaceutical Science. 5th ed. Baltimore: Lippincott Williams and Wilkins; 2006. p. 553–9.
38. Jagtap YM, Bhujbal RK, Ranade AN, Ranpise NS. Effect of various polymers concentrations on physicochemical properties of floating microspheres. Indian J Pharm Sci 2012;74:512-20.
39. Clearly GW. Transdermal controlled release systems. In: Langer RS, Wise DS. eds. Medical applications of controlled release. Vol. 1. Boca Raton, FL: CRC Press; S1984. p. 204-51.
40. Lucero MJ, Vigo J, Leon MJ. A study of shear and compression deformations on hydrophilic gels of tretinoin. Int J Pharm 1994;106:125-33.
41. Harish NM, Prabhu P, Charyulu RN, Gulzar MA, Subrahmanyam EV. Formulation and evaluation of in situ gels containing clotrimazole for oral candidiasis. Indian J Pharm Sci 2009;71:421-7.
42. Martin A. Physical pharmacy, kinetics. First Indian reprint. New Delhi: B. I Waverly; 1994.
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