An overview of preparation and characterization of solid binary system and its application on transdermal film with variation of plasticizers
DOI:
https://doi.org/10.1590/s2175-97902022e191123%20Keywords:
Ondansetron, Solubility, Inclusion complex, Permeation, Transdermal filmAbstract
Chemotherapy induced nausea and vomiting (CINV) and post-operative nausea and vomiting (PONV) is a problem, often occurs in patient. Inspite of high bioavailability, the demerits such as: hepatic first pass metabolism and invasive nature of oral and parenteral dosage forms can be avoided with anti-emetic therapy of transdermal device. The major objective of the present study is to modify the hydrochloride (HCl) form of Ondansetron (OND) to the base form followed by improvement of solubility and permeability of OND by employing solid dispersion (SD) loaded patches. Preformulation study, as observed, begins with an approach to enthuse solubility of OND by SD technique choosing different carriers. The choice of carriers was rationalized by phase solubility study. Several combinations of transdermal films were prepared with pure drug, carriers and SDs with plasticizer Ka values of OND-HPβCD binary system were found lower (54.43 to 187.57 M-1) than that of OND-PVP K-30 binary system (1156.77 to 12203.6 M-1). The drug content of SDs and patches were found satisfactory. Better permeation rate (236.48±3.66 µg/3.935 cm2) with promising flux enhancement (8.30 fold) was found with DBP loaded SD patch (P6*). Hence, enhancement of solubility and permeability of P6* ensures that it can successfully enhance the bioavailability.
Downloads
References
Ahad A, Al-Jenoobi FI, Al-Mohizea AM, Akhtar N,Raish M, Aqil M. Systemic delivery of β-blockers via transdermal route for hypertension. Saudi Pharm J. 2015;23(6):587-602.
Ahad A, Aqil M, Kohli K, Sultana Y, Mujeeb M, Ali A. Transdermal drug delivery: the inherent challenges and technological advancements. Asian J Pharm Sci.2010;5(6):276-289.
Alany R. Topical and transdermal formulation and drug delivery. Pharm Dev Tech. 2017;22(4):457-457.
Banerjee S, Chattopadhyay P, Ghosh A, Bhattacharya SS, Kundu A, Veer V. Accelerated stability testing of a transdermal patch composed of serine and pralidoxime chloride for prophylaxis against (±)-anatixin a poisoning. J. Food Drug Anal. 2014;22(2):264-270.
Bergo P, Sobral PJA. Effects of plasticizer on physical properties of pigskin gelatin films. Food Hydrocol. 2006;21(8):1285-1289.
Chien YW. Development of transdermal drug delivery system. Drug DevInd Pharm. 1987;13(4-5):589-651.
Cilurzo F, Gennari CGM, Minghetti P. Adhesive properties: a critical issue in transdermal patch development. Expart Opin Drug Deliv. 2012;9(1):33-45.
Das MK, Ghosal SK. Ex vivo and in vivo evaluation of transdermal formulation of trazodone hydrochloride. Acta Pol Pharm. 2008;65(4):481-486.
Das SK, Kahali N, Bose A, Khanam J. Physicochemical characterization and in vitro dissolution performance of ibuprofen-Captisol® (sulfobutylether sodium salt of β-CD) inclusion complexes. J Mol Liq. 2018;261:239-249.
Desai KGH. Enhanced skin permeation of rofecoxib using topical microemulsion gel. DrugDev Res. 2004;63(1):33-40.
Di L, Kerns EH. Drug like properties: Concepts, Structures design and Methods. 2nd Ed. United Kingdom (UK): Academic press, 2016, pp. 497-510.
Elsabee MZ, Abdou ES. Chitosan based edible films and coatings: a review. Mater SciEng C Mater Biol Appl. 2013;33(4):1819-1841.
Gal A, Nussinovitch A. Plasticizers in the manufacture of novel skin-bioadhesive patches. Int J Pharm. 2009;370(1-2):103-109
Ghanghoria R, Kesharwani P, Agashe HB, Jain NK. Transdermal delivery of cyclodextrin-solubilized curcumin.Drug DelivTransl Res. 2013;3(3):272-285.
Guy R, Green MR, Kealey T. Modeling acne in vitroJ Invest Dermatol. 1996;106(1):176-82.
Hassan N, Khar RK, Ali M, Ali J. Development and evaluation of buccalbioadhesive tablet of an anti-emetic agent ondansetron. AAPS Pharm Tech. 2009;10(4):1085-1092.
Higuchi T, Connor’s KA. Phase solubility techniques. In: Reilly CN, editor. Advances in Analytical Chemistry and Instrumentation. New York: Interscience; 1965. p. 117-212.
Jana S, Ali SA, Nayak AK, Sen KK, Basu SK. Development of topical gel containing aceclofenac-crospovidone solid dispersion by "Quality by Design (QbD)" approach. ChemEngg Res Des. 2014;92(11):2095-2105.
Kahali N, Khanam J. A novel HPLC method validation based on analytical techniques of metoclopramide benzamide derivative (Metoclopramide base) and its determination from solid dispersion by solvent evaporation method. J App Pharm Sci. 2018;8(2):18-26.
Kahali N, Khanam J, Ghosh N. An attempt to enhance solubility of metoclopramide base by Solid dispersion strategy and its application on development of Transdermal device. Brazilian J Pharm Sci. 2021;57:1-22.
Kalimuthu Y, Khanam J. Enhancement of carvedilol solubility by solid dispersion technique using cyclodextrins, water soluble polymers and hydroxyl acid. J Pharm Biomed Anal.2014;96:10-20.
Kandavilli S, Nair V, Panchagnula R. Polymers in transdermal drug delivery systems. Pharm Tech. 2002;26:62-81.
Kathe K, Kathpalia H. Film forming systems for topical and transdermal drug delivery. Asian JPharm Sci. 2017;12(6):487-497.
Kaur IP, Geetha TM, Kakkar V. Treatment of skin cancer using sesamol-loaded solid lipid nanoparticles. In: Souto EB, editor. Lipid nanocarriers in cancer diagnosis and therapy. 1st ed. United Kingdom (UK): A Smithers Group Company. 2011. p. 510-526.
Khan S, Kataria P, Nakhat P, Yeole P. Taste Masking of ondansetron hydrochloride by polymer carrier system and formulation of rapid-disintegrating tablets. AAPS Pharm Tech. 2007;8(2):1-7.
Loftsson T, Masson M. Cyclodextrins in topical drug formulations: theory and practice. Int JPharm. 2001;225(1-2):15-30.
Minghetti P, Cilurzo F, Montanari L. Evaluation of adhesive properties of patches based on acrylic matrices. Drug Dev Ind Pharm. 1999; 25(1): 1-6.
Moldoveanu S, David V. Phase transfer in sample preparation. Modern sample preparation for chromatography. Amsterdam: The Netherlands. 2015. p. 3-446.
Mukherjee B, Mahapatra S, Gupta R, Patra B, Tiwari A, Arora P. A comparison between povidone-ethylcellulose and povidone-eudrajit transdermal dexamethasone matrix patches based on in vitro skin permeation. Eur J Pharm Biopharm. 2005;59(3):475-483.
Palem CR, Battu SK, Maddineni S, Gannu R, Repka MA, Yamsani MR. Oral transmucosaldelivery of domperidone from immediate release films produced via hot-melt extrusion technology. Pharm Dev Tech nol. 2013;18(1):186-195.
Paradkar A, Ambike AA, Jadhav KB, Mahadik KR. Characterization of curcumin-PVP solid dispersion obtained by spray drying. Int J Pharm . 2004;271(1-2):281-286.
Patel DP, Setty CM, Mistry GN, Patel SL, Patel TJ, Mistry PC, etal.Development and evaluation of ethyl cellulose-based transdermal films of furosemide for improved In Vitro skin permeation. AAPS Pharm Tech. 2009;10(2):437-442.
Patil H, Tiwari RV, Upadhye SB, Vladyka RS, Repka MA. Formulation and development of pH-independent/dependent sustained release matrix tablets of ondansetronHCl by a continuous twin-screw melt granulation process. Int J Pharm . 2015;496(1):33-41.
Pattnaik S, Swain A, Mallick S, Lin Q. Effect of casting solvent on crystallinity of ondansetron in transdermal films. Int J Pharm . 2011;406(1-2):106-110.
Prajapati ST, Patel CG, Patel, CN. Formulation and evaluation of transdermal patch of repaglinide. ISRN Pharm. 2011;2011:1-9.
Prausnitz MR, Langer R. Transdermal drug delivery. Nat Biotechnol. 2008;26(11):1261-1268.
Puri A, Bhattaccharjee SA, Zhang W, Clark M, Singh ON, Doncel GE, et al. Development of a transdermal delivery system for tenofoviralafenamide, a prodrug of tenofovir with potent antiviral activity against HIV and HBV. Pharmaceutics. 2019;11(173):1-29.
Rao PR, Diwan PV. Permeability studies of cellulose acetate free films for transdermal use: influence of plasticizers. Pharm ActaHelv. 1997;72(1):47-51.
Ravikumar R, Ganesh M, Ubaidulla U, Choi EY, Jang HT. Preparation, characterization, and in vitro diffusion study of nonwoven electrospunnanofiber of curcumin-loaded cellulose acetate phthalate polymer. Saudi Pharm J.2017;25(6):921-926.
Rogers TL, Hypromellose: Rowe RC, Sheskey PJ, Quinn ME, (Eds.), Handbook of Pharmaceutical Excipients. London: Pharmaceutical Press. 2009. p. 326-329.
Salem II, Lopez JMR, Galan AC. Ondansetron Hydrochloride. In: Brittain HG editor. Analytical Profiles of Drug Substances and Excipients.U.S.A: Elsevier Academic press. 2001. p. 301-338.
Schmook FP, Meingassner JG, Billich A. Comparison of human skin or epidermis models with human and animal skin in in-vitro percutaneous absorption. Int J Pharm . 2001;215(1-2):51-60.
Singh A, Bali A. Formulation and characterization of transdermal patches for controlled delivery of duloxetine hydrochloride. J Anal Sci Tech. 2016;25:1-13.
Soliman SM, Malak NSA, El Gazayerly ON, Abdel Rahim, AA. Preparation of celecoxib solid dispersions for dermal application: in vitro characterization and skin irritation test. J Drug Del Sci Tech. 2011; 21(6):509-516.
Subedi RK, Oh SY, Chun MK, Choi HK. Recent Advances in Transdermal Drug Delivery. Arch Pharm Res. 2010;33:339-351.
Suthar RM, Chotai NP, Patel HK, Patel SR, Shah DD, Jadeja MB. In vitro dissolution enhancement of ondansetron by solid dispersion in superdisintegrants. Dissol Technol. 2013;20(4):34-38.
Thakur G, Singh A, Singh I. Formulation and evaluation of transdermal composite films of chitosan-montmorillonite for the delivery of curcumin. Int J Pharm Investig. 2016;6(1):23-31.
Walters KA, Transdermal drug delivery systems: Swarbrick K, Boylan JC, (Eds.). Encyclopedia of Pharmaceutical Technology. New York, Marcel Dekker, 1999. p. 306-320.
Wu C, Williams III RO, O’Donnell K, Dong Y, Lang B, Li H, et al. Formulation and delivery of improved amorphous fenofibrate solid dispersions prepared by thin film freezing. Eur J Pharm Biopharm . 2012;82(3):534-544.
Zheng L, Reza F. Influence of colloidal silicon dioxide on gel strength, robustness, and adhesive properties of diclofenac gel formulation for topical application. AAPS Pharm Tech. 2014;16(3):636-644.
Downloads
Published
Issue
Section
License
Copyright (c) 2022 Brazilian Journal of Pharmaceutical Sciences
This work is licensed under a Creative Commons Attribution 4.0 International License.
All content of the journal, except where identified, is licensed under a Creative Commons attribution-type BY.
The on line journal has open and free access.
