Formulation and Evaluation of Betulin Loaded Transdermal Patches
Abstract
Objectives: To develop and evaluate Transdermal patches of Betulin along with various polymers for controlled release action.
Method: Suitable method such as Solvent Casting Technique of Film Casting Technique are used for preparation of Transdermal patch.
Result: The prepared Transdermal patches were transparent, smooth, uniform and flexible. The method adopted for preparation of system was found satisfactory.
Conclusion: Various formulations were developed by using hydrophilic and hydrophobic polymers like HPMC E5 and EC respectively in single and combinations by solvent evaporation technique with incorporation of penetration enhancer such as dimethylsulfoxide and dibutyl phthalate as plasticizer. Formulation F7 containing equal ratio of HPMC E5: EC (5:5) showed maximum percentage drug content 95.44%. A suitable UV Spectroscopy method for the analysis of Betulin was developed. Betulin showed maximum absorption at wave length 215 nm in isotonic phosphate buffer (pH 7.4) solutions. The pre-formulation studies involving description, solubility, melting point, partition coefficient of the drug were found to be comparable with the standard. The Transdermal patch of Betulin was prepared successfully by solvent evaporation method. Transdermal patch of Betulin for Transdermal drug delivery was evaluated. Calibration curve was obtained; Transdermal film was prepared, overcome limitations regarding bioavailability of drug was done.
Keywords: Controlled DDS, Transdermal DDS, Betulin, Transdermal Patch, solvent evaporation method.
Keywords:
Controlled DDS, Transdermal DDS, Betulin, Transdermal Patch, solvent evaporation methodDOI
https://doi.org/10.22270/jddt.v14i5.6578References
Panchagnula R, Transdermal delivery of drugs, Ind J Pharmacol ,1997; 29:140-56.
Kshirsagar NA, Drug delivery systems, Ind J Pharmacol, 2000; 32:54-61.
Gupta JRD, Tripathi P, Irchhiaya R, Garud N, Dubey P, Patel J, Formulation and evaluation of matrix type transdermal patches of Glibenclamide, Int J Pharm Sci Drug Res, 2009; 1(1): 46-50. https://doi.org/10.25004/IJPSDR.2009.010111
Vyas SP, Roop KK. Controlled drug delivery concepts and advances,New Delhi: Vallabh prakash publishers, 2005;1:411-47.
Maurya SD, Aggarwa S l, Tilak VK, Dhakar RC, Singh A, Maurya G, Enhanced transdermal delivery of indinavir sulfate via transfersomes, Pharmacie Globale (IJCP). 2010; 1(06)
Yasukawa K, Takido M, Matsumoto T, Takeuchi M, Nakagawa S, Sterol and triterpene derivatives from plants inhibit the effects of a tumor promoter, and sitosterol and Betulin inhibit tumor formation in mouse skin two-stage carcinogenesis, Oncology,1991;48:72-76. https://doi.org/10.1159/000226898 PMid:1898988
Wick W, Grimmel C, Wagenknecht B, Dichgans J, Weller M, Betulin-induced apoptosis in glioma cells: A sequential requirement for new protein synthesis, formation of reactive oxygen species, and caspase processing, J. Pharmacol. Exp. Ther,1999;289:1306-1312.
Evan GI, Vousden KH. Proliferation, cell cycle and apoptosis in cancer, Nature, 2001;411:342-348. https://doi.org/10.1038/35077213 PMid:11357141
Tan Y, Yu R, Pezzuto JM, Betulin-induced programmed cell death in human melanoma cells involves mitogen-activated protein kinase activation, Clin. Cancer Res., 2003;9:2866-2875.
Thurnher D, Turhani D, Pelzmann M, Wannemacher B, Knerer B, Formanek M, Wacheck V, Selzer E, Betulin: a new cytotoxic compound against malignant head and neck cancer cells, Head Neck,2003;25:732-740. https://doi.org/10.1002/hed.10231 PMid:12953308
Ehrhardt H, Fulda S, Fuhrer M, Debatin KM, Jeremias I,Betulin-induced apoptosis in leukemia cells. Leukemia,2004;18:1406-1412. https://doi.org/10.1038/sj.leu.2403406 PMid:15201849
Schmidt ML, Kuzmanoff KL, Ling-Indeck L, Pezzuto JM, Betulin induces apoptosis in human neuroblastoma cell lines, Eur. J. Cancer, 1997;33:2007-2010. https://doi.org/10.1016/S0959-8049(97)00294-3 PMid:9516843
Fulda S, Jeremias I, Steiner HH, Pietsch T, Debatin KM, Betulin: a new cytotoxic agent against malignant brain-tumor cells. Int. J. Cancer,1999;82:435-441.
https://doi.org/10.1002/(SICI)1097-0215(19990730)82:3<435::AID-IJC18>3.0.CO;2-1
Rajendran P, Jaggi M, Singh MK, Mukherjee R, Burman AC, Pharmacological evaluation of C-3 modified Betulin derivatives with potent anticancer activity, Invest. New Drugs, 2008;26:25-34. https://doi.org/10.1007/s10637-007-9081-4 PMid:17851638
Chauhan lti, Meenakshi B, Formulation and evaluation of transdermal drug delivery of Raloxifene hydrochloride. International Journal of Pharmaceutical Sciences and Research, 2010;1(12):72-79.
Gajanan D, Dinesh J, Vinod P, Formulation and evaluation of transdermal drug delivery system of Clopodogrel bisulfate. Asian Journal of Pharmacy and Life Sciences, 2011; 1(3):269-278.
Kavitha K, Rajendra MM, Design and evaluation of transdermal films of Lornoxicam, International Journal of Pharma and Bio Sciences, 2011;2(2):54-62.
Subash SP, Muneer TK, Panneerselvam T, Mohd Azharuddin, Shabaraya AR, Controlled drug delivery of Diltiazem hydrochloride as transdermal patches: a novel approch on formulation evaluation in vitro and in vivo parameters, Research in Pharmacy,2011; 1(2):17-19.
Nilesh BR, Hardikar SR, Ashok BV, Formulation and evaluation of transdermal patches of Ropinirole HCL, Research Journal of Pharmaceutical, Biological and Chemical Sciences 2011; 2(1):138-148.
Chiu MH, Prenner EJ, Differential scanning calorimetry: An invaluable tool for a detailed thermodynamic characterization of macromolecules and their interactions, J Pharm Bioallied Sci, 2011; 3(1):39-59. https://doi.org/10.4103/0975-7406.76463 PMid:21430954 PMCid:PMC3053520
Gbaguidi F, Accrombessi G, Moudachirou M, Leclercq JQ, HPLC quantification of two isomeric triterpenic acids isolated from Mitracarpus scaber and antimicrobial activity on Dermatophilus congolensis, J Pharm Biomed Anal, 2005; 39:990-995. https://doi.org/10.1016/j.jpba.2005.05.030 PMid:16043321
Sathyapriya LS, Jayaprakash S, Prabhu RS, Abirami A, Subramanian K, Nagarajan M, An approach to the formulation and evaluation of transdermal DDS of isoxsuprine HCl, Int J Pharm Sci Tech, 2008;1(1):22-8.
Saxena M, Mutalik S, Reddy MS, Formulation and evaluation of transdermal patches of metoclopramide hydrochloride, Ind drugs, 2006;43(9):740-45.
Sankar V, Benito JD, Sivanand V, Ravichandran V, Raghuraman S, Velrajan G et, Design and evaluation of nifedipine transdermal patches, Ind J Pharm Sci, 2003; 65(5):510
Gupta JRD, Tripathi P, Irchhiaya R, Garud N, Dubey P, Patel JR, Formulation and evaluation of matrix type transdermal patches of Glibenclamide, Int J Pharm Sci Drug Res,2009;1(1): 46-50. https://doi.org/10.25004/IJPSDR.2009.010111
Dandagi PM, Manavi FV, Gadag AP, Mastiholimath VS, Jagdeesh T, Formulation of ransdermal drug delivery of ketotifen fumarate, Ind J Pharm Sci, 2003; 65(3):239-43
Shivhare UD, Dorlikar VP, Bhusari KP, Mathur VB, Mirani BN,Effect of polymeric compositions on pharmacotechnical properties of carvedilol transdermal film. Int J Pharm Sci Nanotech, 2009;1(2):457-64 https://doi.org/10.37285/ijpsn.2009.2.1.10
Krishnaiah YS, Satyanarayana V, Bhaskar P, Influence of limonene on the bioavailability of nicardipine hydrochlorothiazide from membrane modulated transdermal therapeutic systems in human volunteers, Int J Pharm,2002;247:91-102 https://doi.org/10.1016/S0378-5173(02)00401-5 PMid:12429488
Murthy TEGK, Kishore VS, Effect of casting solvent and polymer on permeability of propranolol hydrochloride through membrane controlled transdermal drug delivery system, Ind J Pharm Sci, 2007;69(5):646-50 https://doi.org/10.4103/0250-474X.38469
Jamakandi VG, Mulla JS, Vinay BL, Shivakumar HN, Formulation, characterization, and evaluation of matrix-type transdermal patches of a model antihypertensive drug, Asian J Pharma Sci, 2009;3(1): 59-65. https://doi.org/10.4103/0973-8398.49177
Devi KV, Saisivam S, Maria GR, Deepti PU, Design and evaluate of matrix diffusion controlled transdermal patches of verapmil hydrochloride, Drug Dev Ind pharm,2003; 29(5):495-503. https://doi.org/10.1081/DDC-120018638 PMid:12779279
Dandagi PM, Manavi FV, Gadag AP, Mastiholimath VS, Jagdeesh T, Formulation of transdermal drug delivery of ketotifen fumarate, Ind J Pharm Sci, 2003; 65(3):239-43.
Kulkarni RV, Mutalik S, Hiremath D, Effect of plasticizers on the permeability and mechanical properties of eudragit films for transdermal application. Ind J Pharm Sci, 2002; 64(1):28-31.
Panigrahi L, Ghosal SK, Formulation and evaluation of pseudolatex transdermal drug delivery system of terbutaline sulphate, Ind J Pharm. Sci; 2002:79-82.
Ubaidulla U, Reddy MVS, Ruckmani K, Ahmad FJ, Khar RK, Transdermal therapeutic system of carvedilol: Effect of hydrophilic and hydrophobic matrix on in vitro and in vivo characteristics, AAPS Pharm Sci Tech,2007; 8(1):1-8. https://doi.org/10.1208/pt0801002 PMid:17408218 PMCid:PMC2750430
Panigrahi L, Ghosal SK, Formulation and evaluation of pseudolatex transdermal drug delivery system of terbutaline sulphate, Ind J Pharm. Sci; 2002:79-82
Published
Abstract Display: 542 
PDF Downloads: 463 PDF Downloads: 88 How to Cite
Issue
Section
Authors who publish with this journal agree to the following terms:
- Authors retain copyright and grant the journal right of first publication with the work simultaneously licensed under a Creative Commons Attribution-NonCommercial 4.0 International (CC BY-NC 4.0). that allows others to share the work with an acknowledgment of the work's authorship and initial publication in this journal.
- Authors are able to enter into separate, additional contractual arrangements for the non-exclusive distribution of the journal's published version of the work (e.g., post it to an institutional repository or publish it in a book), with an acknowledgment of its initial publication in this journal.
- Authors are permitted and encouraged to post their work online (e.g., in institutional repositories or on their website) prior to and during the submission process, as it can lead to productive exchanges, as well as earlier and greater citation of published work (See The Effect of Open Access).
How to Cite
.