Role of solid carriers in pharmaceutical performance of solid supersaturable SEDDS of celecoxib

被引:70
作者
Chavan, Rahul B. [1 ]
Modi, Sameer R. [1 ]
Bansal, Arvind K. [1 ]
机构
[1] Natl Inst Pharmaceut Educ & Res, Dept Pharmaceut, Sas Nagar 160062, Punjab, India
关键词
SEDDS; Solid carrier; Silicon dioxide; Porosity; Surface area; Hydrophobicity-hydrophilicity; In vitro drug release; DRUG-DELIVERY-SYSTEMS; LIPID-BASED FORMULATIONS; BIOPHARMACEUTICAL PERFORMANCE; ORAL BIOAVAILABILITY; CRYSTAL HABIT; DISSOLUTION; OPTIMIZATION; RELEASE; LIQUID; STABILITY;
D O I
10.1016/j.ijpharm.2015.09.011
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
Self emulsifying drug delivery system (SEDDS) has been increasingly used for improving the oral bioavailability of poorly water soluble drugs. SEDDS can be solidified by adsorbing them on different solid carriers. In the present study, the impact of properties of solid carrier on drug release profile from solid SEDDS was investigated. Celecoxib (CEL) loaded supersaturable SEDDS (S-SEDDS) was prepared and optimized by using optimal response surface design. Optimum composition of S-SEDDS corresponded to 10: 45: 45% v/v ratio of oil (Capryol 90), surfactant (Tween 20) and cosurfactant (Transcutol HP) with Soluplus (40 mg) as precipitation inhibitor. Different grades of silicon dioxide were selected based on their properties like surface area, porosity and hydrophobicity-hydrophilicity, and used for preparation of solid S-SEDDS (SS-SEDDS) by adsorption method. All SS-SEDDS formulations in release studies, gave droplet size, PDI and zeta potential similar to S-SEDDS. The percent drug release after 120 min from CEL powder, S-SEDDS and SS-SEDDS with Sylysia 350 fcp, Aerosil 300 Pharma, Aerosil 200 Pharma and Aerosil R 972 Pharma was found to be 0.58%, 100%, 38.44%, 9.63%, 2.53% and 5.99%, respectively. Drug release profiles were compared by using model independent methods. The differential drug release behavior of SS-SEDDS was attributed to the different physico-chemical properties of solid carriers. SS-SEDDS with Sylysia 350 fcp showed higher drug release and greater dissolution efficiency. Oral bioavailability study also demonstrated 2.34 fold increase in C-max and 4.82 fold increase in AUC (0-24 h) when compared with CEL powder. This study highlights the rational for selection of solid carriers in the formulation development of solid SEDDS. (C) 2015 Elsevier B.V. All rights reserved.
引用
收藏
页码:374 / 384
页数:11
相关论文
共 44 条
[1]   Dissolution and powder flow characterization of solid self-emulsified drug delivery system (SEDDS) [J].
Agarwal, Vikas ;
Siddiqui, Akhtar ;
Ali, Hazem ;
Nazzal, Sami .
INTERNATIONAL JOURNAL OF PHARMACEUTICS, 2009, 366 (1-2) :44-52
[2]  
[Anonymous], 2014, J. Appl. Pharm. Res.
[3]   Enhanced oral bioavailability of dexibuprofen by a novel solid Self-emulsifying drug delivery system (SEDDS) [J].
Balakrishnan, Prabagar ;
Lee, Beom-Jin ;
Oh, Dong Hoon ;
Kim, Jong Oh ;
Hong, Myung Ja ;
Jee, Jun-Pil ;
Kim, Jung Ae ;
Yoo, Bong Kyu ;
Woo, Jong Soo ;
Yong, Chul Soon ;
Choi, Han-Gon .
EUROPEAN JOURNAL OF PHARMACEUTICS AND BIOPHARMACEUTICS, 2009, 72 (03) :539-545
[4]   New dosage formulations for targeted delivery of cyclo-oxygenase-2 inhibitors - Focus on use in the elderly [J].
Bansal, Shyam S. ;
Joshi, Abhijeet ;
Bansal, Arvind K. .
DRUGS & AGING, 2007, 24 (06) :441-451
[5]   Development, Optimization, and Characterization of Solid Self-Nanoemulsifying Drug Delivery Systems of Valsartan Using Porous Carriers [J].
Beg, Sarwar ;
Swain, Suryakanta ;
Singh, Harendra Pratap ;
Patra, Ch Niranjan ;
Rao, M. E. Bhanoji .
AAPS PHARMSCITECH, 2012, 13 (04) :1416-1427
[6]   Adsorption of gases in multimolecular layers [J].
Brunauer, S ;
Emmett, PH ;
Teller, E .
JOURNAL OF THE AMERICAN CHEMICAL SOCIETY, 1938, 60 :309-319
[7]   Optimized formulation of solid self-microemulsifying sirolimus delivery systems [J].
Cho, Wonkyung ;
Kim, Min-Soo ;
Kim, Jeong-Soo ;
Park, Junsung ;
Park, Hee Jun ;
Cha, Kwang-Ho ;
Park, Jeong-Sook ;
Hwang, Sung-Joo .
INTERNATIONAL JOURNAL OF NANOMEDICINE, 2013, 8 :1673-1682
[8]   Challenges and opportunities in the encapsulation of liquid and semi-solid formulations into capsules for oral administration [J].
Cole, Ewart T. ;
Cad, Dorninique ;
Benameur, Hassan .
ADVANCED DRUG DELIVERY REVIEWS, 2008, 60 (06) :747-756
[9]   Solid self-microemulsifying drug delivery system of ritonavir [J].
Deshmukh, Ashish ;
Kulkarni, Shirishkumar .
DRUG DEVELOPMENT AND INDUSTRIAL PHARMACY, 2014, 40 (04) :477-487
[10]   A stability-indicating HPLC method to determine celecoxib in capsule formulations [J].
Dhabu, PM ;
Akamanchi, KG .
DRUG DEVELOPMENT AND INDUSTRIAL PHARMACY, 2002, 28 (07) :815-821