FORMULATION AND IN VITRO CHARACTERIZATION SOLID SELF EMULSIFYING DRUG DELIVERY SYSTEM OF RAMIPRIL PREPARED BY ADSORPTION TECHNIQUE


Madhavi K, Shikha A, Suresh B

Abstract


Objective: The primary goal of the present work was to formulate solid self-emulsifying drug delivery systems (S-SEDDS) in order to improve the solubility of the highly lipophilic antihypertensive drug, ramipril.

Methods: SEDDS are generally liquid form preparations obtained by homogeneously mixing oils, surfactants and co-surfactants along with drug component. Based on solubility studies Capmul PG8 NF, Gelucire 44/14 and Transcutol P were selected as oil, surfactant, co-surfactant respectively in order to prepare liquid SEDDS (L-SEDDS). Nine different liquid SEDDS were prepared and subjected to various evaluation tests in order to obtain optimized L-SEDDS. Finally, the optimized formulation was converted to S-SEDDS by physical adsorption technique using an inert carrier. Further, S-SEDDS were also subjected to solid state characterization.

Results: Out of 9 different L-SEDDS, S9 formulation was optimized as it formed thermodynamically stable emulsion without any drug precipitation and phase separation on storage and also showed least globule size (22.56 nm). The optimized formulation was loaded onto inert carrier (Sylysia FCP 350) to obtain S-SEDDS. S-SEDDS showed acceptable flow properties. They were further processed for solid state characterization such as XRD, DSC and SEM and the results confirmed the transformation of native crystalline nature of drug to an amorphous state. FTIR analysis also confirmed no drug-excipient interaction. S-SEDDS showed improved in vitro dissolution behaviour of ramipril over that of pure drug.

Conclusion: Ramipril S-SEDDS retained emulsification characteristics of L-SEDDS. Further, S-SEDDS was encapsulated in hard gelatin capsules and this formulation proved to have improved solubility for ramipril.

Keywords: Liquid self-emulsifying drug delivery system (L-SEDDS), Solid self-emulsifying drug delivery system(S-SEDDS), Ramipril, Emulsification, Sylysia FCP 350.

| PDF | HTML |

References


Lipinski CA. Poor aqueous solubility-an industry wide problem in drug discovery. Am Pharm Rev 2002;5:82–5.

Pouton CW. Lipid formulations for oral administration of drugs: nonemulsifying, self-emulsifying and ‘self-microemulsifying’ drug delivery systems. Eur J Pharm Sci 2000;11(Suppl 2):S93–S98.

Kapsi SG, Ayres JW. Processing factors in development of solid solution formulation of itraconazole for enhancement of drug dissolution and bioavailability. Int J Pharm 2001;229:193–203.

Popescu C, Manda P, Juluri A, Janga K, Cidda M, Murthy SN. Enhanced dissolution efficiency of zaleplon solid dispersions via modified β-cyclodextrin molecular inclusion complexes. J Pharm Pharm Sci 2015;1:12-21.

Zidan AS, Sammour OA, Hammad MA, Megrab NA, Habib MJ, Khan MA. Quality by design: understanding the product variability of a self nanoemulsified drug delivery system of cyclosporine. Asian J Pharm Sci 2007;6:2409–23.

Robert GS. Solubilizing excipients in oral and injectable formulations. Pharm Res 2004;21:201–30.

Kovacs I, Jusztin M, Takacs E, Balaz S. US Patent No. 5; 1996. p. 583, 105.

Khoo SM, Humberstone AJ, Porter CJH, Edwards GA, Charman WN. Formulation design and bioavailability assessment of lipidic selfemulsifying formulations of halofantrine. Int J Pharm 1998;167:155-64.

Amit AK, Vandana BP. Design and evaluation of self-emulsifying drug delivery systems (SEDDS) of nimodipine. AAPS Pharm Sci Tech 2008;9:191-6.

Dixit RP, Nagarsenker MS. Self-nanoemulsifying granules of ezetimibe: Design, optimization and evaluation. Eur J Pharm Sci 2008;35:183–92.

Sammour OA, Hammad MA, Megrab NA, Zidan AS. Formulation and optimization of mouth dissolve tablets containing rofecoxib solid dispersions. AAPS PharmSciTech 2006;7:E167-E175.

Valleri M, Mura P, Maeshrelli F, Cirri M, Ballerini R. Development and evaluation of glyburide fast dissolving tablets using solid dispersion technique. Drug Dev Ind Pharm 2004;30:525-34.

Jung SL, Marc A, Ebel P, Raymond M, Wim EH, Jan F. Circulation kinetics and biodistribution of dual-labeled polymersomes with modulated surface charge in tumor-bearing mice: comparison with stealth liposomes. J Controlled Release 2011;155:282-8.

Yoo JH, Shanmugam S, Thapa P, Lee ES, Balakrishnan P, Baskaran R, et al. Novel self-nanoemulsifying drug delivery system for enhanced solubility and dissolution of lutein. Arch Pharm Res 2010;33:417–26.

Pouton CW. Formulation of self-emulsifying drug delivery systems. Adv Drug Delivery Rev 1997;25:47–58.

Shah NH, Carvajal MT, Patel CI, Infeld MH, Malick AW. Self-emulsifying drug delivery systems (SEDDS) with polyglycolyzed glycerides for improving in vitro dissolution and oral absorption of lipophilic drugs. Int J Pharm 1994;106:15-23.

Gershanik T, Haltner E, Leh CM, Benita S. Charge-dependent interaction of self-emulsifying oil formulations with Caco-2 cells monolayers: binding, effects on barrier function and cytotoxicity. Int J Pharm 2000;211:29–36.

Wei LL, Sun PN, Nie SF, Pan WS. Preparation and evaluation of SEDDS and SMEDDS containing Carvedilol. Drug Dev Ind Pharm 2005;31:785–94.




About this article

Title

FORMULATION AND IN VITRO CHARACTERIZATION SOLID SELF EMULSIFYING DRUG DELIVERY SYSTEM OF RAMIPRIL PREPARED BY ADSORPTION TECHNIQUE

Date

07-01-2016

Additional Links

Manuscript Submission

Journal

International Journal of Current Pharmaceutical Research
Vol 8, Issue 1, 2016 Page: 40-45

Online ISSN

0975-7066

Statistics

268 Views | 174 Downloads

Authors & Affiliations

Madhavi K
Department of Pharmaceutics, Swami Vivekanand College of Pharmacy, Indore 452020, Madhya Pradesh, India,

Shikha A
Department of Pharmaceutics, Swami Vivekanand College of Pharmacy, Indore 452020, Madhya Pradesh, India,

Suresh B
Department of Pharmaceutics, St. Peter’s Institute of Pharmaceutical Sciences, Warangal 506001, Telangana, India


Refbacks

  • There are currently no refbacks.