Effects of absorbent materials on a self-emulsifying drug delivery system for a poorly water soluble drug
Tóm tắt
In order to compare the effects of a solid carrier on the formulation of a solid self-microemulsifying drug delivery system (s-SMEDDS), a liquid SMEDDS was prepared with simvastatin. The SMEDDS was optimized using polyoxyl 35 castor oil [Kolliphor® EL] as a surfactant (S), diethylene glycol monoethylether [Transcutol® P] as a co-surfactant (C), and prophyleneglycol monocaprylate [Capryol 90] as the oil phase (O). The microemulsion area at the surfactant to co-surfactant ratio (1:1) was evaluated, and the SMEDDS at an S and C/O ratio of 7:3 was selected. Four types of adsorbents with high specific areas were used: Aerosil® 200, Sylysia® 350, Neusilin® US2, Neusilin® UFL2. SEM, DSC, and PXRD results revealed rough-surfaced particles that represent the amorphous state of s-SMEDDS. The optimized formulation with Neusilin® UFL2 markedly improved drug release. The present study concluded that s-SMEDDS was effectively formulated via adsorption with solid carriers.
Tài liệu tham khảo
Agarwal V, Siddiqui A, Ali H, Nazzal S (2009) Dissolution and powder flow characterization of solid self-emulsified drug delivery system (SEDDS). Int J Pharm 366:44–52
Alinaghi A, Tan A, Rao S, Prestidge C (2014) Impact of solidification on the performance of lipid-based colloidal carriers: oil-based versus self-emulsifying systems. Curr Drug Deliv 12:16–25
Cerpnjak K, Zvonar A, Vrecer F, Gašperlin M (2014) Development of a solid self-microemulsifying drug delivery system (SMEDDS) for solubility enhancement of naproxen. Drug Dev Ind Pharm 1–10
Chen C-C, Wu M-L, Doerksen RJ, Ho C-T, Huang T-C (2015) Andrographolide induces apoptosis via down-regulation of glyoxalase 1 and HMG-CoA reductase in HL-60 cells. J Funct Foods 14:226–235
Dixit AR, Rajput SJ, Patel SG (2010) Preparation and bioavailability assessment of SMEDDS containing valsartan. AAPS PharmSciTech 11:314–321
Draheim C, de Crécy F, Hansen S, Collnot E-M, Lehr C-M (2015) A design of experiment study of nanoprecipitation and nano spray drying as processes to prepare PLGA nano-and microparticles with defined sizes and size distributions. Pharm Res 1–16
Franceschinis E, Santomaso A, Benda L, Perissutti B, Voinovich D, Realdon N (2015) Influence of process variables on the properties of simvastatin self-emulsifying granules obtained through high shear wet granulation. Powder Technol 274:173–179
Gao P, Akrami A, Alvarez F, Hu J, Li L, Ma C, Surapaneni S (2009) Characterization and optimization of AMG 517 supersaturatable self-emulsifying drug delivery system (S-SEDDS) for improved oral absorption. J Pharm Sci 98:516–528
Griffin BT, Kuentz M, Vertzoni M, Kostewicz ES, Fei Y, Faisal W, Stillhart C, O’Driscoll CM, Reppas C, Dressman JB (2014) Comparison of in vitro tests at various levels of complexity for the prediction of in vivo performance of lipid-based formulations: case studies with fenofibrate. Eur J Pharm Biopharm 86:427–437
Grill AE, Koniar B, Panyam J (2014) Co-delivery of natural metabolic inhibitors in a self-microemulsifying drug delivery system for improved oral bioavailability of curcumin. Drug Deliv Transl Res 4:344–352
Gulotta A, Saberi AH, Nicoli MC, McClements DJ (2014) Nanoemulsion-based delivery systems for polyunsaturated (ω-3) oils: formation using a spontaneous emulsification method. J Agric Food Chem 62:1720–1725
Jannin V, Musakhanian J, Marchaud D (2008) Approaches for the development of solid and semi-solid lipid-based formulations. Adv Drug Deliv Rev 60:734–746
Javeer SD, Patole R, Amin P (2013) Enhanced solubility and dissolution of simvastatin by HPMC-based solid dispersions prepared by hot melt extrusion and spray-drying method. J Pharm Investig 43:471–480
Kang BK, Lee JS, Chon SK, Jeong SY, Yuk SH, Khang G, Lee HB, Cho SH (2004) Development of self-microemulsifying drug delivery systems (SMEDDS) for oral bioavailability enhancement of simvastatin in beagle dogs. Int J Pharm 274:65–73
Kanzarkar M, Pathak PP, Vaidya M, Brumlik C, Choudhury A (2015) Oral insulin-delivery system for diabetes mellitus. Pharm Pat Anal 4:29–36
Kesisoglou F, Panmai S, Wu Y (2007) Nanosizing—oral formulation development and biopharmaceutical evaluation. Adv Drug Deliv Rev 59:631–644
Kim KH, Park J-B, Choi W-J, Lee HS, Kang C-Y (2011) Preparation and characterization of simvastatin solid dispersion using aqueous solvent. J Pharm Investig 41:239–247
Liu J, Cao F, Zhang C, Ping Q (2013) Use of polymer combinations in the preparation of solid dispersions of a thermally unstable drug by hot-melt extrusion. Acta Pharm Sin B 3:263–272
Narayana L, Chella N, Kumar D, Shastri NR (2015) Design of a novel type IV lipid-based delivery system for improved delivery of drugs with low partition coefficient. J Liposome Res 1–9
Park J-B, Lee G-H, Kang J-W, Jeon I-S, Kim J-M, Kim K-B, Kang C-Y (2013) Improvement of photostability and dissolution profile of isradipine using inclusion complex. J Pharm Investig 43:55–61
Park J-B, Park Y-J, Kang C-Y, Lee B-J (2014) Modulation of microenvironmental pH and utilization of alkalizers in crystalline solid dispersion for enhanced solubility and stability of clarithromicin. Arch Pharmacal Res 1–10
Park J-B, Prodduturi S, Morott J, Kulkarni VI, Jacob MR, Khan SI, Stodghill SP, Repka MA (2015) Development of an antifungal denture adhesive film for oral candidiasis utilizing hot melt extrusion technology. Expert Opin Drug Deliv 12:1–13
Patil P, Paradkar A (2006) Porous polystyrene beads as carriers for self-emulsifying system containing loratadine. AAPS PharmSciTech 7:E199–E205
Pouton CW, Porter CJ (2008) Formulation of lipid-based delivery systems for oral administration: materials, methods and strategies. Adv Drug Deliv Rev 60:625–637
Prasad D, Chauhan H, Atef E (2013) Studying the effect of lipid chain length on the precipitation of a poorly water soluble drug from self-emulsifying drug delivery system on dispersion into aqueous medium. J Pharm Pharmacol 65:1134–1144
Qi X, Qin J, Ma N, Chou X, Wu Z (2014) Solid self-microemulsifying dispersible tablets of celastrol: formulation development, characterization and bioavailability evaluation. Int J Pharm 472:40–47
Roger E, Lagarce F, Garcion E, Benoit J-P (2009) Lipid nanocarriers improve paclitaxel transport throughout human intestinal epithelial cells by using vesicle-mediated transcytosis. J Control Release 140:174–181
Salonen J, Laitinen L, Kaukonen A, Tuura J, Björkqvist M, Heikkilä T, Vähä-Heikkilä K, Hirvonen J, Lehto V-P (2005) Mesoporous silicon microparticles for oral drug delivery: loading and release of five model drugs. J Control Release 108:362–374
Singh D, Pathak K (2013) Hydrogen bond replacement—unearthing a novel molecular mechanism of surface solid dispersion for enhanced solubility of a drug for veterinary use. Int J Pharm 441:99–110
Tang B, Cheng G, Gu J-C, Xu C-H (2008) Development of solid self-emulsifying drug delivery systems: preparation techniques and dosage forms. Drug Discov Today 13:606–612
Wang K, Qi J, Weng T, Tian Z, Lu Y, Hu K, Yin Z, Wu W (2014) Enhancement of oral bioavailability of cyclosporine A: comparison of various nanoscale drug-delivery systems. Int J Nanomed 9:4991
Weerapol Y, Limmatvapirat S, Jansakul C, Takeuchi H, Sriamornsak P (2015) Enhanced dissolution and oral bioavailability of nifedipine by spontaneous emulsifying powders: effect of solid carriers and dietary state. Eur J Pharm Biopharm
Woo JS, Song Y-K, Hong J-Y, Lim S-J, Kim C-K (2008) Reduced food-effect and enhanced bioavailability of a self-microemulsifying formulation of itraconazole in healthy volunteers. Eur J Pharm Sci 33:159–165
Wu L, Qiao Y, Wang L, Guo J, Wang G, He W, Yin L, Zhao J (2015) A self-microemulsifying drug delivery system (SMEDDS) for a novel medicative compound against depression: a preparation and bioavailability study in rats. AAPS PharmSciTech 1–8
Zhang Z, Bu H, Gao Z, Huang Y, Gao F, Li Y (2010) The characteristics and mechanism of simvastatin loaded lipid nanoparticles to increase oral bioavailability in rats. Int J Pharm 394:147–153
Zhao T, Maniglio D, Chen J, Chen B, Motta A, Migliaresi C (2015) Design and optimization of self-nanoemulsifying formulations for lipophilic drugs. Nanotechnology 26:125102
Zu Y, Li N, Zhao X, Li Y, Ge Y, Wang W, Wang K, Liu Y (2014) In vitro dissolution enhancement of micronized l-nimodipine by antisolvent re-crystallization from its crystal form H. Int J Pharm 464:1–9