Formulation & Development of Baclofen microemulsion incorporated into Transdermal patch
Abstract
The current study aims at developing formulations based on microemulsions for the transdermal patch of Baclofen. Castor oil was used in the oil phase, Tween-20 was used as a surfactant, propylene glycol(PG) worked as a cosurfactant, and water worked as an aqueous phase in the formation of microemulsions. Using Franz diffusion cells, in vitro permeation tests were conducted. At the conclusion of 8 hours, the in vitro permeation release of ME-3 was determined to be 88.79%, and baclofen microemulsion was later put into the transdermal patch. The most effective composition was ME-3, which included dimethyl sulfoxide as a penetration enhancer, propylene glycol as a plasticizer, and carbopol 940 as a bio-adhesive polymer. The formulation with the best penetration enhancement exhibited a 39-fold increase and contained 0.1% DMSO. It was discovered that ME-3 Patch has a 97.67% in vitro permeation release rate. According to a study, baclofen may be produced into transdermal patches with an acceptable appearance and an appropriate drug release time of 4 hours.
Keywords: (ME-)Microemulsion, HPMC, Transdermal patch, Baclofen, Carbopol- 940
Keywords:
Microemulsion, HPMC, Transdermal patch, Baclofen, Carbopol- 940DOI
https://doi.org/10.22270/jddt.v12i5.5586References
Prausnitz Mark R., Mitragotri Samir, Langer Robert. Current status and future potential of transdermal drug delivery. Nature Reviews Drug Discovery volume. Published online February 1, 2004:115-124. https://doi.org/10.1038/nrd1304
Verma S, Vaishnav Y, Verma S, Jha A. Anhydrous Nanoemulsion: An Advanced Drug Delivery System for Poorly Aqueous Soluble Drugs. Current Nanomedicine. 2017; 7(1):36-46. https://doi.org/10.2174/2468187306666160926124713
Biswal Biswajit. Formulation and Evaluation of Microemulsion Based Topical Hydrogel Containing Lornoxicam. Journal of Applied Pharmaceutical Science. Published online December 30, 2014. https://doi.org/10.7324/JAPS.2014.41214
Delgado-Charro MB, Iglesias-Vilas G, Blanco-Méndez J, López-Quintela MA, Marty JP, Guy RH. Delivery of a hydrophilic solute through the skin from novel microemulsion systems. European Journal of Pharmaceutics and Biopharmaceutics. 1997; 43(1):37-42. https://doi.org/10.1016/S0939-6411(96)00016-1
Ktistis G. A Study on the In-vitro Percutaneous Absorption of Propranolol from Disperse System. Journal of Pharmacy and Pharmacology. 1998; 50(4):412-418. Accessed August 21, 2022. https://doi.org/10.1111/j.2042-7158.1998.tb06881.x
Kreilgaard M. Influence of microemulsions on cutaneous drug delivery. Advanced Drug Delivery Reviews. 2002; 54:S77-S98. https://doi.org/10.1016/S0169-409X(02)00116-3
Lawrence MJ, Rees GD. Microemulsion-based media as novel drug delivery systems. Advanced Drug Delivery Reviews. 2000; 45(1):89-121. https://doi.org/10.1016/S0169-409X(00)00103-4
Peltola S, Saarinen-Savolainen P, Kiesvaara J, Suhonen TM, Urtti A. Microemulsions for topical delivery of estradiol. International Journal of Pharmaceutics. 2003; 254(2):99-107. https://doi.org/10.1016/S0378-5173(02)00632-4
Wisher D. Martindale: The Complete Drug Reference. 37th ed. J Med Libr Assoc. 2012; 100(1):75-76. https://doi.org/10.3163/1536-5050.100.1.018
Dario A, Stefano M.G. Di, Grossi A. Long-term intrathecal baclofen infusion in supraspinal spasticity of adulthood. Acta Neurol Scand. 2002; 105(2):83-87.
Duthey B, Hübner A, Diehl S, Boehncke S, Pfeffer J, Boehncke WH. Anti-inflammatory effects of the GABAB receptor agonist baclofen in allergic contact dermatitis. Experimental Dermatology. 2010; 19(7):661-666. https://doi.org/10.1111/j.1600-0625.2010.01076.x
Nabi-Meibodi M, Navidi B, Navidi N, Vatanara A, Reza Rouini M, Ramezani V. Optimized double emulsion-solvent evaporation process for production of solid lipid nanoparticles containing baclofene as a lipid insoluble drug. Journal of Drug Delivery Science and Technology. 2013; 23(3):225-230. https://doi.org/10.1016/S1773-2247(13)50034-7
S.M. Foroutan, A.R. Shaafati, A. Khodam. Bioequivalence Studies Of Two Formulations Of Baclofen Tablet In Healthy Volunteers. IRANIAN JOURNAL OF PHARMACEUTICAL RESEARCH . 2003; 2(3):153-155.
Delhaas E M, Brouwers J R. Intrathecal baclofen overdose: report of 7 events in 5 patients and review of the literature. Int J Clin Pharmacol Ther Toxicol . 1991; 29(7):274-280.
Chandrashekar N, Shobha Rani R. Physicochemical and pharmacokinetic parameters in drug selection and loading for transdermal drug delivery. Indian Journal of Pharmaceutical Sciences. 2008; 70(1):94. https://doi.org/10.4103/0250-474X.40340
Aulton BPharm FAAPS FSP FRPharmS ME, Taylor BPharm FRPharmS KM. Aulton’s Pharmaceutics: The Design and Manufacture of Medicines.; 2018. www.konkur.in
Garti N, Aserin A, Tiunova I, Fanun M. A DSC study of water behavior in water-in-oil microemulsions stabilized by sucrose esters and butanol. Colloids and Surfaces A: Physicochemical and Engineering Aspects. 2000; 170(1):1-18. https://doi.org/10.1016/S0927-7757(00)00486-6
Ghosh PK, Majithiya RJ, Umrethia ML, Murthy RSR. Design and development of microemulsion drug delivery system of acyclovir for improvement of oral bioavailability. AAPS PharmSciTech. 2006; 7(3):E172-E177. https://doi.org/10.1208/pt070377
Chen H, Chang X, Weng T, et al. A study of microemulsion systems for transdermal delivery of triptolide. Journal of Controlled Release. 2004; 98(3):427-436. https://doi.org/10.1016/j.jconrel.2004.06.001
Kumar B, Jain SK, Prajapati SK. Effect of Penetration Enhancer DMSO on In-Vitro Skin Permeation of Acyclovir Transdermal Microemulsion Formulation. International Journal of Drug Delivery. 2011; 3(1):83-94. https://doi.org/10.5138/ijdd.2010.0975.0215.03057
Prajapati ST, Patel CG, Patel CN. Formulation and Evaluation of Transdermal Patch of Repaglinide. ISRN Pharmaceutics. 2011; 2011:1-9. https://doi.org/10.5402/2011/651909
Garala Kevin, Shinde Anilkumar. Formulation and in-vitro characterization of monolithic matrix transdermal systems using HPMC/Eudragit S 100 polymer blends. International Journal of Pharmacy and Pharmaceutical Sciences. 2009; 1(1).
Kusum Devi V, Saisivam S, Maria GR, Deepti PU. Design and Evaluation of Matrix Diffusion Controlled Transdermal Patches of Verapamil Hydrochloride. Drug Development and Industrial Pharmacy. 2003; 29(5):495-503. https://doi.org/10.1081/DDC-120018638
Gupta R, Mukherjee B. Development and In Vitro Evaluation of Diltiazem Hydrochloride Transdermal Patches Based on Povidone–EthylCellulose Matrices. Drug Development and Industrial Pharmacy. 2003; 29(1):1-7. https://doi.org/10.1081/DDC-120016678
Minghetti P, Cilurzo F, Casiraghi A. Measuring Adhesive Performance in Transdermal Delivery Systems. American Journal of Drug Delivery. 2004; 2(3):193-206. https://doi.org/10.2165/00137696-200402030-00004
Pierre MBR, Ricci E, Tedesco AC, Bentley MVLB. Oleic Acid as Optimizer of the Skin Delivery of 5-Aminolevulinic Acid in Photodynamic Therapy. Pharmaceutical Research. 2006; 23(2):360-366. https://doi.org/10.1007/s11095-005-9261-x
Costa P, Sousa Lobo JM. Modeling and comparison of dissolution profiles. European Journal of Pharmaceutical Sciences. 2001; 13(2):123-133. https://doi.org/10.1016/S0928-0987(01)00095-1
Published
Abstract Display: 1134 
PDF Downloads: 1017 PDF Downloads: 212 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
.