Self-Micro Emulsifying Drug Delivery Systems: A Strategy to Improve Oral Bioavailability
DOI:
https://doi.org/10.30827/ars.v57i3.5327Keywords:
SMEDDS, surfactant, oil, co-surfactant, bioavailabilityAbstract
Aim: Oral route has always been the favorite route of drug administration in many diseases and till today it is the first way investigated in the development of new dosage forms. The major problem in oral drug formulations is low and erratic bioavailability, which mainly results from poor aqueous solubility, thereby pose problems in their formulation. For the therapeutic delivery of lipophilic active moieties (BCS class II drugs), lipid based formulations are inviting increasing attention.
Methods: To that aim, from the web sites of PubMed, HCAplus, Thomson, and Registry were used as the main sources to perform the search for the most significant research articles published on the subject. The information was then carefully analyzed, highlighting the most important results in the formulation and development of self-micro emulsifying drug delivery systems as well as its therapeutic activity.
Results: Self-emulsifying drug delivery system (SMEDDS) has gained more attention due to enhanced oral bio-availability enabling reduction in dose, more consistent temporal profiles of drug absorption, selective targeting of drug(s) toward specific absorption window in GIT, and protection of drug(s) from the unreceptive environment in gut.
Conclusions: This article gives a complete overview of SMEDDS as a promising approach to effectively deal with the problem of poorly soluble molecules.
Downloads
References
Talegaonkar S, Azeem A, Ahmad FJ, Khar RK, Pathan SA, Khan ZI. Microemulsions: A Novel Approach to Enhanced Drug Delivery. Recent Pat Drug Deliv Formul. 2008; 2:238-257.
Pouton CW. Lipid formulations for oral administration of drugs: non-emulsifying, self-emulsifying and self-microemulsifying’ drug delivery systems. Eur J Pharm Sci. 2000; 11 Suppl 2: S93-8.
Jaiswal P, Aggrewal G, Kaur A. Bioavailability enhancement of poorly soluble drugs by SMEDDS- A review. J Drug Deliv Ther. 2013; 3(1): 98-109.
Shukla JB, Koli AR, Ranch KM, Parikh RK. Self microemulsifying drug delivery system. Int J Pharm Pharm Sci. 2010;1(2): 13-33.
Kumar A, Sharma S, Kamble R. Self emulsifying drug delivery system (SEDDS): future aspects. Int J Pharm Pharm Sci. 2010; 2(4): 7-13.
Verma A, Singh MK, Kumar B. Development and characterization of Flutamide containing self micro emulsifying drug delivery system (SMEDDS). Int J Pharm Pharm Sci. 2011;3(4): 60-65.
Shukla P, Prajapati SK, Sharma U, Shivhare S. A review on self micro emulsifying drug delivery system: An approach to enhance the oral bioavailability of poorly water soluble drugs. IRJP. 2012; 3(9): 16.
Bansal AK, Sarpal K, Pawar YB. Self emulsifying drug delivery systems: A strategy to improve oral bioavailability.CRIPS. 2010; 11(3): 4249.
Reiss H. Entropy-induced dispersion of bulk liquids. J Colloids Interface Sci. 1975; 53: 61-70.
Prince LM. Microemulsions. Marcel Dekker, New York, 1974.
Turner SR, Siano DB, Bock J. A Microemulsion Process for Producing Acrylamide-Alkyl Acrylamide Copolymers. U. S. Patent 1985; 4: 521-580.
Bates TR, Sequeria JA. Bioavailability of micronized Griseofulvin from corn oil in water emulsion, aqueous suspension and commercial tablet form in humans. J. Pharm. Sci. 1975; 64(5): 793-797.
Gershanik T, Benita S. Self-dispersing lipid formulations for improving oral absorption of lipophilic drugs. Eur. J. Pharm. Biopharm. 2012; 188-199.
Hauss DJ. Oral lipid-based formulations. Adv Drug Deliv Rev. 2007; 59: 667-76.
Chambin O, Janin V. Interest of multifunctional lipid excipients: case of Gelucire® 44/14. Drug Dev Ind Pharm. 2005; 31: 527-534.
Charman WN, Porter CJ. Physiochemical and physiological mechanisms for the effects of food on drug absorption: The role of lipids and pH. J Pharm. Sci. 1997; 86(3): 269-282.
Chaudhary B, Maheshwari K. Self-emulsifying drug delivery system: a novel approach for enhancement of bioavailability. J Pharm. Sci. Biosci. 2011; 31-36.
Gershanik T, Benita S. Self-dispersing lipid formulations for improving oral absorption of lipophilic drugs. Eur. J. Pharm. Biopharm. 2012; 188-199.
Attama AA and Mpamaugo VE. Pharmacodynamics of piroxicam from self-emulsifying lipospheres formulated with homolipids extracted from Capra hircus. Drug Deliv. 2006;13:133-137.
Jannin V, et al.. Approaches for the development of solid and semi-solid lipid-based formulations. Adv Drug Deliv Rev. 2008; 60:734-746.
Dong L. et al.. A novel osmotic delivery system, L-OROS SOFTCAP. Proceedings of the International Symposium on Controlled Release of Bioactive Materials. 2000;July, Paris (CD ROM).
Yi T, Wan J, Xu H,Yang X. A new solid self-microemulsifying formulation prepared by spray-drying to improve the oral bioavailability of poorly water soluble drugs. Eur J Pharm Biopharm. 2008;70:439-444.
Ito Y, et al.. Oral solid gentamicin preparation using emulsifier and adsorbent. J Control Release. 2005; 105: 23-31. 18.
Venkatesan N. et al.. Liquid filled nanoparticles as a drug delivery tool for protein therapeutics. Biomaterials. 2005; 26:7154-7163.
Seo A, et al..,The preparation of agglomerates containing solid dispersions of diazepam by melt agglomeration in a high shear mixer. Int J Pharm. 2003; 259; 161-171.
Gupta MK, et al.., Enhanced drug dissolution and bulk properties of solid dispersions granulated with a surface adsorbent. Pharm Dev Technol.2001; 6:563-572.
Gupta MK, et al.. Hydrogen bonding with adsorbent during storage governs drug dissolution from solid dispersion granules. Pharm. Res.2002; 19: 1663-1672.
Verreck G, Brewster ME. Melt extrusion-based dosage forms, excipients and processing conditions for pharmaceutical formulations. Bull Tech Gattefosse.2004; 97:85-95.
Newton M, et al.. The influence of formulation variables on the properties of pellets containing a self-emulsifying mixture. J Pharm Sci.2001; 90: 987-995.
Newton JM, et al.. Formulation variables on pellets containing self-emulsifying systems. Pharm Tech Eur.2005; 17: 29-33.
Newton JM, et al.. The rheological properties of self-emulsifying systems, water and microcrystalline cellulose. Eur J Pharm Sci.2005; 26:176-183.
Tuleu C, et al.. Comparative bioavailability study in dogs of a self-emulsifying formulation of progesterone presented in a pellet and liquid form compared with an aqueous suspension of progesterone. J Pharm Sci.2004; 93: 1495-1502.
Iosio T, et al.. Bi-layered self-emulsifying pellets prepared by co-extrusion and spheronization: influence of formulation variables and preliminary study on the in vivo absorption. Eur J Pharm Biopharm. 2008; 69(2): 686-697.
Myers SL, Shively ML. Preparation and characterization of emulsifiable glasses oil-in-water and waterin-oil-in-water emulsion. J Colloid Interface Sci.1992; 149: 271-278.
Bamba J, et al.. Cryoprotection of emulsions in freeze-drying: freezing process analysis. Drug Dev Ind Pharm.1995; 21:1749-1760.
Christensen KL, et al.. Technical optimization of redispersible dry emulsions. Int J Pharm .2001; 212: 195202.
Hansen T, et al.. Process characteristics and compaction of spray-dried emulsions containing a drug dissolved in lipid. Int J Pharm.2004; 287:55-66.
Jang DJ, et al.. Improvement of bioavailability and photostability of amlodipine using redispersible dry emulsion. Eur J Pharm Sci.2006; 28:405-411.
Itoh K, et al.. Improvement of physicochemical properties of N-4472 part I Formulation design by using selfmicroemulsifying system. Int J Pharm. 2002; 238:153-160.
Gao P, Morozowich W. Development of supersaturatable selfemulsifying drug delivery system formulations for improving the oral absorption of poorly soluble drugs. Expert Opin Drug Discov.2006; 3: 97110.
Gao P, et al.. Development of a supersaturable SEDDS (S-SEDDS) formulation of paclitaxel with improved oral bioavailability. J Pharm Sci.2003; 92: 2386-2398.
Li P, et al.. Development and characterization of a solid microemulsion preconcentrate system for oral delivery of poorly water soluble drugs. Controlled Release Society Annual Meeting, Long Beach, C.A, 2007;June.
Li P, et al.. Novartis Pharmaceuticals Corp. Spontaneously dispersible pharmaceutical compositions. WO2006/050123.
Ito Y, et al.. Preparation and evaluation of oral solid heparin using emulsifier and adsorbent for in vitro and in vivo studies. Int J Pharm.2006; 317:114-119.
Schwarz J. Solid self-emulsifying dosage form for improved delivery of poorly soluble hydrophobic compounds and the process for preparation thereof. US Patent 20030072798. 2003; April 17.
Wei LL, et al.. Investigations of a novel self-emulsifying osmotic pump tablet containing carvedilol. Drug Dev Ind Pharm.2007; 33:990-998.
Gandhi R, et al.. Extrusion and spheronization in the development of oral controlled-release dosage forms. PSTT 2, 1999; 160-170.
Serajuddin ATM. Solid dispersion of poorly water-soluble drugs.early promises, subsequent problems, and recent breakthroughs. J Pharm Sci.1999; 88:1058-1066.
Vasanthavada M, Serajuddin ATM. Lipid-based self-emulsifying solid dispersions. In: Oral Lipid-Based Formulations: Enhancing Bioavailability of Poorly Water-Soluble Drugs (Hauss, D.J., ed.), Informa Healthcare, 2007; 149-184.
Serajuddin ATM, et al.. Effect of vehicle amphiphilicity on the dissolution and bioavailability of a poorly water-soluble drug from solid dispersions. J Pharm Sci.1988; 77: 414-417.
Khoo SM, et al.. The formulation of halofantrine as either non-solubilising PEG 6000 or solubilising lipid based solid dispersions. physical stability and absolute bioavailability assessment. Int J Pharm.2000; 205:6578.
Kim JY, Ku YS. Enhanced absorption of indomethacin after oral orrectal administration of a selfemulsifying system containing indomethacin to rats. Int J Pharm.2000; 194: 81-89.
Chae GS, et al.. Enhancement of the stability of BCNU using self-emulsifying drug delivery systems (SEDDS) and in vitro antitumor activity of self-emulsified BCNU-loaded PLGA wafer. Int J Pharm.2005; 301:6-14.
Downloads
Published
How to Cite
Issue
Section
License
The articles, which are published in this journal, are subject to the following terms in relation to the rights of patrimonial or exploitation:
- The authors will keep their copyright and guarantee to the journal the right of first publication of their work, which will be distributed with a Creative Commons BY-NC-SA 4.0 license that allows third parties to reuse the work whenever its author, quote the original source and do not make commercial use of it.
b. The authors may adopt other non-exclusive licensing agreements for the distribution of the published version of the work (e.g., deposit it in an institutional telematic file or publish it in a monographic volume) provided that the original source of its publication is indicated.
c. Authors are allowed and advised to disseminate their work through the Internet (e.g. in institutional repositories or on their website) before and during the submission process, which can produce interesting exchanges and increase citations of the published work. (See The effect of open access).
