Preparation of transdermal monolithic systems of indapamide by solvent casting method and the use of vegetable oils as permeation enhancer G.

G.S. Sanap, G.Y. Dama, A.S. Hande, S.P. Karpe, S.V. Nalawade, R.S. Kakade, U.Y. Jadhav

Abstract


Transdermal drug delivery systems of indapamide have been formulated by using solvent casting method. Monolithic systems were prepared by using hydroxy propyl methyl cellulose (HPMC) and ethyl cellulose (EC) polymers by incorporating glycerine and dibutyl phthalate as plasticizers, respectively. All the patches were uniform with respect to physicochemical and scanning electron microscopy (SEM) evaluation. Th e in vitro drug release studies indicated that HPMC containing fi lms have shown better release than that of EC containing fi lms without any permeation enhancer. A total of eight monolithic systems were prepared by using a drug polymer ratio of 1:4 and incorporated diff erent vegetable oils as permeation enhancers in diff erent concentrations. Th e prepared systems released
the drug in the following order: F3 > F4 > F7 > F5 > F8 > F6 > F1 > F2. Th e various permeation parameters such as fl ux, permeability coeffi cient, enhancement ratio and diff usion rate constants were determined for all the formulations. Th e maximum fl ux of 9.08 × 102 mg/ cm2 h was observed with HPMC monolithic system containing 30% w/w olive oil. A signifi cant improvement of fl ux was observed in
the following order: olive oil > linseed oil > sunfl ower oil > cottonseed oil > coconut oil > castor oil. Further improvement of fl ux was observed, when 30% w/w olive oil was applied directly onto the skin prior to the studies. Th e in vitro release studies revealed that the release was sustained up to 24 h and it follows zero-order kinetics. All the fi lms were found to be stable at 37°C and 45°C with respect to their physical parameters and drug content.
Key words: EC, HPMC, linseed oil, olive oil, permeation enhancers, sunfl ower oil, transdermal

Full Text:

PDF

References


Jing AS, Weimin S. The adverse drug reaction of indapamide Pract.

J Med Pharm 2003;11:843-4.

Smith RV, Stewart JT. Procurement and characterization of

standard reference materials. 4th ed. Philadelphia: 1981.

Munden BJ, Dekay HG, Banker GS. Evaluation of polymeric

materials and screening of film coating agent. J Pharm Sci

;53:395-401.

Raghavendra K, Doddayya H, Marshal SC. Comparative

evaluation of polymeric Þ lms for transdermal application. East

Pharma 2000;516:109-11.

Kusum Devi V, Saisivam S. Design and evaluation of matrix diff usion

controlled transdermal patches of verapamil hydrochloride. Drug

Dev Ind Pharm 2003;29:95-103.

Bhalla HL, Shah AA. Controlled release matrices for ketoprofen.

Indian Drugs 1991;28:420-2.

Flynn GL, Durrheim H. Permeation through hairless mouse

skin II: Membrane sectioning techniques and inß uence on alkanol

permeabilities. J Pharm Sci 1981;70:52-6.

Narasimha Murthy S, Mini Sateesh, Hamsa V. Drug release from

terbutaline sulphate transdermal Þ lms across human cadaver skin.

Indian J Pharm Sci 1997;59:75-6.

Brain R, Mathews. Regulatory aspects of stability testing in Europe.

Drug Dev Ind Pharm 1999;25: 831-56.

Gwak HS, Kim SU, Chun IK. Eff ect of vehicles and enhancers on

the in vitro permeation of melatonin through hairless mouse skin,

Arch Pharm Res 2002;25:392-6.

Pongjanyakul T, Prakongpan S, Priprem A. Acrylic matrix type

nicotine transdermal patches: In vitro evaluation and batch-tobatch

uniformity. Drug Dev Ind Pharm 2003;29:843-53.

Rama Rao N, Sudhakar Rao G. Compatibility study between

pregelatinized starch as excipients and various commonly used

drugs using diff erential scanning calorimetry. Int J Pharm Excip

;1:103-6.

Mohammed FA, Khedr H. Preparation and in vitro/in vivo

evaluation of the buccal bioadhesive properties of slow-release

tablets containing miconazole nitrate. Drug Dev Ind Pharm

;29:321-37.

Arora P, Mukherjee B. Design, development, physicochemical

and in vitro, in vivo evaluation of transdermal patches containing

diclofenac diethylammonium salt. J Pharm Sci 2002;91:2078-88.

Okpo SO, Fatokun F, Adeyemi OO. Analgesic and antiin

ß ammatory activity of Crinum glaucum aqueous extract. J Ethno

Pharm 2001;78:207-11.

Andersson TL, Stehle B, Davidsson B, Höglund P. Bioavailability of

esrtadiol from two matrix transdermal delivery systems: Menorest

and Climara. Maturitas 2000;35:57-64.

Kim JH, Lee CH, Choi HK. Transdermal delivery of physostigmine:

Eff ect of enhancers and pressure sensitive adhesives. Drug Dev

Ind Pharm 2002;28:833-9.




DOI: http://dx.doi.org/10.22377/ijgp.v2i2.47

Refbacks

  • There are currently no refbacks.