全部 标题 作者
关键词 摘要

OALib Journal期刊
ISSN: 2333-9721
费用:99美元

查看量下载量

相关文章

更多...

单纯形网格法优化设计姜黄素-胡椒碱复方自微乳制剂处方

Keywords: 单纯形网格法,姜黄素,胡椒碱,自微乳给药系统,处方优化,质量评价

Full-Text   Cite this paper   Add to My Lib

Abstract:

该研究的目的在于制备姜黄素-胡椒碱复方自微乳给药系统(Cur-PIP-SMEDDS),并对其质量进行评价。该研究通过选择合适的油相、表面活性剂和助表面活性剂,以姜黄素和胡椒碱为模型药物,采用单纯形网格法优化设计Cur-PIP-SMEDDS处方;以乳剂的载药量、平均粒径为评价指标,通过DesignExpert8.06软件进行试验设计和模型构建,响应面数据分析优化和验证最佳处方组成。通过观察微乳外观和微观形态并测定其粒径、电位、包封率及载药量对其进行质量评价。结果显示优化得Cur-PIP-SMEDDS最佳处方为丙二醇单辛酸酯(Capryol90)-聚氧乙烯氢化蓖麻油(CremophorRH40)-二乙二醇单乙基醚(TranscutolHP)(10:60:30),所形成的微乳外观澄清、透明,呈圆球型,粒径分布均匀,平均粒径为(15.33±0.80)nm,姜黄素和胡椒碱的载药量分别为40.90,0.97mg·g-1,包封率分别为94.98%,90.96%。研究表明Cur-PIP-SMEDDS可以显著改善姜黄素的水溶性和稳定性,有望提高姜黄素的口服生物利用度,以期为其剂型开发提供新的思路和方法,进而促进其在临床上的应用。

References

[1]  Witkin J M, Li X. Curcumin, an active constiuent of the ancient medicinal herb Curcuma longa L.: some uses and the establishment and biological basis of medical efficacy[J]. CNS Neurol Disord Drug Targets,2013, 12(4):487.
[2]  Shehzad A, Rehman G, Lee Y S. Curcumin in inflammatory diseases[J]. Biofactors, 2013, 39(1): 69.
[3]  Ali T, Shakir F, Morton J. Curcumin and inflammatory bowel disease: biological mechanisms and clinical implication[J]. Digestion, 2012,85(4):249.
[4]  Lim T G, Lee S Y, Huang Z, et al.Curcumin suppresses proliferation of colon cancer cells by targeting CDK2[J].Cancer Prev Res (Phila), 2014,7(4):466.
[5]  Terlikowska K, Witkowska A, Terlikowski S.Curcumin in chemoprevention of breast cancer[J].Postepy Hig Med Dosw, 2014,68:571.
[6]  Ahmad N, Umar S, Ashafaq M, et al. Acomparative study of PNIPAM nanoparticles of curcumin, demethoxycurcumin, and bisdemethoxycurcumin and their effects on oxidative stress markers in experimental stroke[J].Protoplasma, 2013, 250(6): 1327.
[7]  Kalani A, Kamat P K, Kalani K, et al. Epigenetic impact of curcumin on stroke prevention[J]. Metab Brain Dis, 2014, doi:10.1007/s11011-014-9537-0.
[8]  Chin D, Huebbe P, Pallauf K, et al. Neuroprotective properties of curcumin in Alzheimer\'s disease——merits and limitations[J]. Curr Med Chem, 2013, 20(32):3955.
[9]  Wang Y, Yin H, Wang L,et al. Curcumin as a potential treatment for Alzheimer\'s disease: a study of the effects of curcumin on hippocampal expression of glial fibrillary acidic protein[J].Am J Chin Med,2013, 41(1):59.
[10]  Yang J, Song S, Li J, et al. Neuroprotective effect of curcumin on hippocampal injury in 6-OHDA-induced Parkinson\'s disease rat [J].Pathol Res Pract, 2014 , 210(6): 357.
[11]  Ji H F, Shen L. The multiple pharmaceutical potential of curcumin in Parkinson\'s disease[J]. CNS Neurol Disord Drug Targets, 2014,13(2):369.
[12]  Szolcsanyi J, Bartho L, Capsaicin-sensitive afferents and their role in gastroprotective: an update[J]. J Physiol Paris, 2001, 95(1/6): 181.
[13]  Morikawa T, Matsuda H,Yamaguchi I, et al. New amidies and gastroprotective constituents from the fruit of Piper chaba[J]. Planta Med,2004,70(2):152.
[14]  Qureshi S, Shah A H, Ageel A M. Toxicity studies on alpiniagalanga and curcuma longa[J]. Planta Med, 1992, 58:124.
[15]  Shankar T N, Shantha N V, Ramesh H P, et al.Toxicity studies on turmeric (Curcuma longa): acute toxicity studies in rats, guineapigs and monkeys[J]. Indian J Exp Biol, 1980,18(1):73.
[16]  Cheng A L, Hsu C H, Lin J K, et al.Phase I clinical trial of curcumin, a chemopreventive agent, in patients with high-risk or pre-malignant lesions[J]. Anticancer Res, 2001,21(4B):2895.
[17]  Lao C D, Rufn M T, Normolle D, et al.Dose escalation of a curcuminoid formulation[J]. BMC Complement Altern Med, 2006,6:10.
[18]  Prasad S, Tyagi A K, Aggarwal B B. Recent developments in delivery, bioavailability, absorption and metabolism of curcumin: the golden pigment from golden spice[J]. Cancer Res Treat, 2014, 46(1):2.
[19]  Singh D V, Godbole M M, Misra K. A plausible explanation for enhanced bioavailability of P-gp substrates in presence of piperine: simulation for next generation of P-gp inhibitors [J]. J Mol Model, 2013,19(1):227.
[20]  Rinwa P, Kumar A. Piperine potentiates the protective effects of curcumin against chronic unpredictable stress-induced cognitive impairment and oxidative damage in mice[J]. Brain Res, 2012, 1488: 38.
[21]  Oliveira R G, Alencar-Filho E B, Vasconcellos M L. The influence of piperine on the bioavailability of drugs: a molecular approach[J]. Química Nova, 2014, 37(1): 69.
[22]  Shoba G, Joy D, Joseph T, et al. Influence of piperine on the pharmacokinetics of curcumin in animals and human volunteers[J]. Planta Med, 1998, 64(4):353.
[23]  Kakarala M, Brenner D E, Korkaya H, et al. Targeting breast stem cells with the cancer preventive compounds curcumin and piperine[J].Breast Cancer Res Treat, 2010, 122(3):777.
[24]  Wu X, Xu J, Huang X, et al.Self-microemulsifying drug delivery system improves curcumin dissolution and bioavailability[J]. Drug Dev Ind Pharm, 2011, 37(1):15.
[25]  Kohli K, Chopra S, Dhar D, et al. Self-emulsifying drug delivery systems: an approach to enhance oral bioavailability[J]. Drug Discov Today, 2010, 15(21/22): 958.
[26]  Hu L, Jia Y, Niu F, et al. Preparation and enhancement of oral bioavailability of curcumin using microemulsions vehicle[J]. J Agric Food Chem, 2012, 60(29):7137.
[27]  Setthacheewakul S,Mahattanadul S,Phadoongsombut N, et al. Development and evaluation of self-microemulsifying liquid and pellet formulations of curcumin, and absorption studies in rats[J]. Eur J Pharm Biopharm, 2010,76(3):475.
[28]  吴雪梅, 刘茂柏, 方令平, 等. 姜黄素与胡椒碱复方自乳化给药系统的处方优化 [J]. 中国医院药学杂志, 2013,33(12):933.
[29]  Zhao Y, Wang C, Chow A H, et al. Self-nanoemulsifying drug delivery system (SNEDDS) for oral delivery of Zedoary essential oil: formulation and bioavailability studies[J]. Int J Pharm, 2010,383(1/2):170.
[30]  Zhao L, Zhang L, Meng L, et al. Design and evaluation of a self-microemulsifying drug delivery system for apigenin[J]. Drug Dev Ind Pharm, 2013, 39(5):662.
[31]  Khoo S M, Humberstone A J, Porter C J H, et al. Formulation design and bioavailability assessment of lipidic self-emulsifying formulations of halofantrine[J]. Int J Pharm, 1998, 167(1/2):155.
[32]  Muhammed Majeed, Vladimir Badmaev, Rajendran R. Use of piperine as a bioavailability enhancer: United States, 5972382[P]. 1999-10-26.
[33]  Shaikh J, Ankola D D, Beniwal V, et al. Nanoparticle encapsulation improves oral bioavailability of curcuminby at least 9-fold when compared to curcumin administeredwith piperine as absorption enhancer [J]. Eur J Pharm Sci, 2009, 37(3/4): 223.
[34]  Bhutania M K, Bishnoi M, Kulkarni S K. Anti-depressant like effect of curcumin and its combination with piperine inunpredictable chronic stress-induced behavioral, biochemical andneurochemical changes [J]. Pharmacol Biochem Behav, 2009, 92(1): 39.
[35]  Liu Y, Zhang P, Feng N, et al, Optimization and in situ intestinal absorption of self-microemulsifying drug delivery system of oridonin[J]. Int J Pharm, 2009, 365(1/2):136.
[36]  江兴龙,贾运涛,张良珂,等.星点设计-效应面法优化葛根素自微乳化释药系统[J].第三军医大学学报,2012,34(14):1414.
[37]  肖璐,易涛,刘颖,等.效应面法优化新型自微乳化口腔速溶膜[J].药学学报,2011,46(5):586.
[38]  Zhang L, Zhu W W, Yang C F, et al. A novel folate-modified self-microemulsifying drug delivery system of curcumin for colon targeting[J]. Int J Nanomed, 2012,7:151.

Full-Text

Contact Us

service@oalib.com

QQ:3279437679

WhatsApp +8615387084133