Sistema de administración de fármacos autoemulsionante: una estrategia para mejorar la biodisponibilidad oral

Autores/as

  • Vijay K. Sharma School of Pharmaceutical Sciences, Jaipur National University
  • Aishwarya Koka Mallareddy Institute of Pharmaceutical Sciences
  • Jyoti Yadav Delhi Institute of Pharmaceutical Sciences and Research, Formerly College of Pharmacy, University of Delhi
  • Anil K. Sharma Delhi Institute of Pharmaceutical Sciences and Research, Formerly College of Pharmacy, University of Delhi
  • Raj K. Keservani School of Pharmaceutical Sciences, Rajiv Gandhi Proudyogiki Vishwavidyalaya, Bhopal

DOI:

https://doi.org/10.30827/ars.v57i3.5327

Palabras clave:

SMEDDS, tensioactivo, aceite, cosurfactante, biodisponibilidad

Resumen

Objetivo: La vía oral siempre ha sido la ruta preferida de administración de fármacos en muchas enfermedades y hasta hoy es la primera forma investigada en el desarrollo de nuevas formas de dosificación. El principal problema en las formulaciones de fármacos orales es la baja y errática biodisponibilidad, lo que resulta fundamentalmente por la escasa solubilidad en agua, con lo que plantean problemas en su formulación. Para la administración terapéutica de los grupos activos lipófilos (BCS clase II drogas), las formulaciones a base de lípidos están teniendo cada vez más atención.

Métodos: Con ese objetivo, a partir de los sitios web de PubMed, HCAplus, Thomson, y sus registros se utilizaron como fuentes principales para llevar a cabo la búsqueda de los artículos de investigación más importantes publicados sobre el tema. A continuación, la información fue analizada cuidadosamente, poniendo de relieve los resultados más importantes en la formulación y desarrollo de sistemas de administración de fármacos auto-emulsionante micro, así como su actividad terapéutica.

Resultados: El sistema de administración de fármacos autoemulsionante (SMEDDS) ha ganado más atención debido a la mejorada que permite la reducción de la biodisponibilidad oral en dosis, los perfiles temporales más consistentes de la absorción del fármaco, la orientación selectiva de fármaco (s) hacia la ventana de absorción específica en el tracto gastrointestinal, y la protección del fármaco (s) desde el entorno poco receptivo en el intestino.

Conclusiones: Este artículo proporciona una visión completa de SMEDDS como un enfoque prometedor para abordar eficazmente el problema de moléculas poco solubles.

Descargas

Los datos de descargas todavía no están disponibles.

Citas

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.

Descargas

Publicado

2016-09-20

Cómo citar

1.
Sharma VK, Koka A, Yadav J, Sharma AK, Keservani RK. Sistema de administración de fármacos autoemulsionante: una estrategia para mejorar la biodisponibilidad oral. Ars Pharm [Internet]. 20 de septiembre de 2016 [citado 29 de marzo de 2024];57(3):97-109. Disponible en: https://revistaseug.ugr.es/index.php/ars/article/view/5327

Número

Sección

Artículos de revisión