Research progress on <i>in vitro</i> lipolysis model for the evaluation of lipid formulations

WU Huiyi; LONG Xiaoying

doi:10.3969/j.issn.1006-0111.2017.06.001

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Volume 35 Issue 6

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Article Navigation > Journal of Pharmaceutical Practice and Service > 2017 > 35(6): 481-484,489

WU Huiyi, LONG Xiaoying. Research progress on in vitro lipolysis model for the evaluation of lipid formulations[J]. Journal of Pharmaceutical Practice and Service, 2017, 35(6): 481-484,489. doi: 10.3969/j.issn.1006-0111.2017.06.001

Citation:

WU Huiyi, LONG Xiaoying. Research progress on in vitro lipolysis model for the evaluation of lipid formulations[J]. Journal of Pharmaceutical Practice and Service, 2017, 35(6): 481-484,489. doi: 10.3969/j.issn.1006-0111.2017.06.001

Research progress on in vitro lipolysis model for the evaluation of lipid formulations

doi: 10.3969/j.issn.1006-0111.2017.06.001

WU Huiyi¹,
LONG Xiaoying^2
,

1.
Department of Pharmacy, Nanfang Hospital of Southern Medical University, Guangzhou 510515, China
2.
School of TCM, Guangdong Pharmaceutical University, Guangzhou 510006, China

Received Date: 2017-04-07
Rev Recd Date: 2017-09-04

Abstract

In vitro lipolysis model has become a new and promising technique to screen and evaluate oral lipid formulations. This model mimics the gastrointestinal tract environment and well reflects the fate of lipid formulations in GI tract after oral administration. This review summarizes the characteristics of lipid formulations, process of gastrointestinal digestion, applications of in vitro lipolysis model and methods for the characterization of the lipolysis process, which provides the basis for the research of oral absorption mechanism and in vivo-in vitro correlations of lipid formulations with lipolysis model.
- lipolysis model,
- lipid formulation,
- gastrointestinal,
- in vivo-in vitro correlation

References

[1]	Pouton CW. Formulation of poorly water-soluble drugs for oral administration:Physicochemical and physiological issues and the lipid formulation classification system[J]. Eur J Pharm Sci, 2006, 29(3-4):278-287.
[2]	Porter CJ, Pouton CW, Cuine JF, et al. Enhancing intestinal drug solubilisation using lipid-based delivery systems[J]. Adv Drug Deliv Rev, 2008, 60(6):673-691.
[3]	Pouton CW. Lipid formulations for oral administration of drugs:non-emulsifying, self-emulsifying and self-microemulsifying' drug delivery systems[J]. Eur J Pharm Sci, 2000, 11(Suppl 2):S93-98.
[4]	Carri re F. Impact of gastrointestinal lipolysis on oral lipid-based formulations and bioavailability of lipophilic drugs[J]. Biochimie. 2016, 125:297-305.
[5]	Kalantzi L, Persson E, Polentarutti B, et al. Canine intestinal contents vs. simulated media for the assessment of solubility of two weak bases in the human small intestinal contents[J]. Pharm Res, 2006, 23(6):1373-1381.
[6]	van Tilbeurgh H, Sarda L, Verger R, et al. Structure of the pancreatic lipase-procolipase complex[J]. Nature, 1992, 359(6391):159-162.
[7]	Lowe ME. The triglyceride lipases of the pancreas[J]. J Lipid Res, 2002, 43(12):2007-2016.
[8]	Shiau YF. Mechanisms of intestinal fat absorption[J]. Am J Physiol, 1981, 240(1):G1-G9.
[9]	Nordskog BK, Phan CT, Nutting DF, et al. An examination of the factors affecting intestinal lymphatic transport of dietary lipids[J]. Adv Drug Deliv Rev, 2001, 50(1-2):21-44.
[10]	Mattson FH, Benedict JH, Martin JB, et al. Intermediates formed during the digestion of triglycerides[J]. J Nutr, 1952, 48(3):335-344.
[11]	Naylor LJ, Bakatselou V, Dressman JB. Comparison of the mechanism of dissolution of hydrocortisone in simple and mixed micelle systems[J]. Pharm Res, 1993, 10(6):865-870.
[12]	Humberstone AJ, Porter CJ, Charman WN. A physicochemical basis for the effect of food on the absolute oral bioavailability of halofantrine[J]. J Pharm Sci, 1996, 85(5):525-529.
[13]	Mu H, Hoy CE. The digestion of dietary triacylglycerols[J]. Prog Lipid Res, 2004, 43(2):105-133.
[14]	Zangenberg NH, Mullertz A, Kristensen HG, et al. A dynamic in vitro lipolysis model.Ⅱ:evaluation of the model[J]. Eur J Pharm Sci, 2001, 14(3):237-244.
[15]	Porter CJ, Trevaskis NL, Charman WN. Lipids and lipid-based formulations:Optimizing the oral delivery of lipophilic drugs[J]. Nat Rev Drug Discov, 2007, 6(3):231-248.
[16]	Fatouros DG, Müllertz A. In vitro lipid digestion models in design of drug delivery systems for enhancing oral bioavailability[J]. Expert Opin Drug Metab Toxicol, 2008, 4(1):65-76.
[17]	曾棋平, 张晶, 刘志宏, 等. 脂解模型在脂质给药系统体外评价中的应用研究进展[J]. 药学实践杂志, 2014, 32(2):85-87.
[18]	Dening TJ, Rao S, Thomas N, et al. Montmorillonite-lipid hybrid carriers for ionizable and neutral poorly water-soluble drugs:Formulation, characterization and in vitro lipolysis studies[J]. Int J Pharm, 2017, 526(1):95-105.
[19]	Kazi M, Al-Qarni H, Alanazi FK. Development of oral solid self-emulsifying lipid formulations of risperidone with improved in vitro dissolution and digestion[J]. Eur J Pharm Biopharm, 2017, 114:239-249.
[20]	林婉婷, 龙晓英, 吴慧仪, 等. 灰黄霉素纳米乳体外脂解过程中药物动态分布研究[J]. 中国药学杂志, 2015, 50(6):512-520.
[21]	Xiao L, Yi T, Liu Y, et al. The in vitro lipolysis of lipid-based drug delivery systems:A newly identified relationship between drug release and liquid crystalline phase[J]. Biomed Res Int, 2016,2016:2364317.
[22]	Siqueira SD, M llertz A, Gr eser K, et al. Influence of drug load and physical form of cinnarizine in new SNEDDS dosing regimens:in vivo and in vitro evaluations[J]. AAPS J. 2017, 19(2):587-594.
[23]	Tanaka Y, Hara T, Waki R, et al. Regional differences in the components of luminal water from rat gastrointestinal tract and comparison with other species[J]. J Pharm Pharm Sci, 2012, 15(4):510-518.
[24]	Fatouros DG, Bergenstahl B, Mullertz A. Morphological observations on a lipid-based drug delivery system during in vitro digestion[J]. Eur J Pharm Sci, 2007, 31(2):85-94.
[25]	Roshan GD, Aagaard AE, Pedersen JS, et al. Experimental Set-up with flow-through cell with SAXS studies of in-situ degradation of drug formulations under gastro-intestinal mimicking conditions[R]. 13th International Conference of Small Angle Scattering, Kyoto:2006.
[26]	Sassene PJ, Knopp MM, Hesselkilde JZ, et al. Precipitation of a poorly soluble model drug during in vitro lipolysis:characterization and dissolution of the precipitate[J]. J Pharm Sci, 2010, 99(12):4982-4991.
[27]	Fernandez S, Jannin V, Chevrier S, et al. In vitro digestion of the self-emulsifying lipid excipient Labrasol by gastrointestinal lipases and influence of its colloidal structure on lipolysis rate[J]. Pharm Res, 2013, 30(12):3077-3087.

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通讯作者: 陈斌, bchen63@163.com

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沈阳化工大学材料科学与工程学院沈阳 110142

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Research progress on in vitro lipolysis model for the evaluation of lipid formulations

1. Department of Pharmacy, Nanfang Hospital of Southern Medical University, Guangzhou 510515, China

2. School of TCM, Guangdong Pharmaceutical University, Guangzhou 510006, China

Received Date: 2017-04-07

Rev Recd Date: 2017-09-04

Key words:

Abstract: In vitro lipolysis model has become a new and promising technique to screen and evaluate oral lipid formulations. This model mimics the gastrointestinal tract environment and well reflects the fate of lipid formulations in GI tract after oral administration. This review summarizes the characteristics of lipid formulations, process of gastrointestinal digestion, applications of in vitro lipolysis model and methods for the characterization of the lipolysis process, which provides the basis for the research of oral absorption mechanism and in vivo-in vitro correlations of lipid formulations with lipolysis model.

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Reference (27)

[1]	Pouton CW. Formulation of poorly water-soluble drugs for oral administration:Physicochemical and physiological issues and the lipid formulation classification system[J]. Eur J Pharm Sci, 2006, 29(3-4):278-287.
[2]	Porter CJ, Pouton CW, Cuine JF, et al. Enhancing intestinal drug solubilisation using lipid-based delivery systems[J]. Adv Drug Deliv Rev, 2008, 60(6):673-691.
[3]	Pouton CW. Lipid formulations for oral administration of drugs:non-emulsifying, self-emulsifying and self-microemulsifying' drug delivery systems[J]. Eur J Pharm Sci, 2000, 11(Suppl 2):S93-98.
[4]	Carri re F. Impact of gastrointestinal lipolysis on oral lipid-based formulations and bioavailability of lipophilic drugs[J]. Biochimie. 2016, 125:297-305.
[5]	Kalantzi L, Persson E, Polentarutti B, et al. Canine intestinal contents vs. simulated media for the assessment of solubility of two weak bases in the human small intestinal contents[J]. Pharm Res, 2006, 23(6):1373-1381.
[6]	van Tilbeurgh H, Sarda L, Verger R, et al. Structure of the pancreatic lipase-procolipase complex[J]. Nature, 1992, 359(6391):159-162.
[7]	Lowe ME. The triglyceride lipases of the pancreas[J]. J Lipid Res, 2002, 43(12):2007-2016.
[8]	Shiau YF. Mechanisms of intestinal fat absorption[J]. Am J Physiol, 1981, 240(1):G1-G9.
[9]	Nordskog BK, Phan CT, Nutting DF, et al. An examination of the factors affecting intestinal lymphatic transport of dietary lipids[J]. Adv Drug Deliv Rev, 2001, 50(1-2):21-44.
[10]	Mattson FH, Benedict JH, Martin JB, et al. Intermediates formed during the digestion of triglycerides[J]. J Nutr, 1952, 48(3):335-344.
[11]	Naylor LJ, Bakatselou V, Dressman JB. Comparison of the mechanism of dissolution of hydrocortisone in simple and mixed micelle systems[J]. Pharm Res, 1993, 10(6):865-870.
[12]	Humberstone AJ, Porter CJ, Charman WN. A physicochemical basis for the effect of food on the absolute oral bioavailability of halofantrine[J]. J Pharm Sci, 1996, 85(5):525-529.
[13]	Mu H, Hoy CE. The digestion of dietary triacylglycerols[J]. Prog Lipid Res, 2004, 43(2):105-133.
[14]	Zangenberg NH, Mullertz A, Kristensen HG, et al. A dynamic in vitro lipolysis model.Ⅱ:evaluation of the model[J]. Eur J Pharm Sci, 2001, 14(3):237-244.
[15]	Porter CJ, Trevaskis NL, Charman WN. Lipids and lipid-based formulations:Optimizing the oral delivery of lipophilic drugs[J]. Nat Rev Drug Discov, 2007, 6(3):231-248.
[16]	Fatouros DG, Müllertz A. In vitro lipid digestion models in design of drug delivery systems for enhancing oral bioavailability[J]. Expert Opin Drug Metab Toxicol, 2008, 4(1):65-76.
[17]	曾棋平, 张晶, 刘志宏, 等. 脂解模型在脂质给药系统体外评价中的应用研究进展[J]. 药学实践杂志, 2014, 32(2):85-87.
[18]	Dening TJ, Rao S, Thomas N, et al. Montmorillonite-lipid hybrid carriers for ionizable and neutral poorly water-soluble drugs:Formulation, characterization and in vitro lipolysis studies[J]. Int J Pharm, 2017, 526(1):95-105.
[19]	Kazi M, Al-Qarni H, Alanazi FK. Development of oral solid self-emulsifying lipid formulations of risperidone with improved in vitro dissolution and digestion[J]. Eur J Pharm Biopharm, 2017, 114:239-249.
[20]	林婉婷, 龙晓英, 吴慧仪, 等. 灰黄霉素纳米乳体外脂解过程中药物动态分布研究[J]. 中国药学杂志, 2015, 50(6):512-520.
[21]	Xiao L, Yi T, Liu Y, et al. The in vitro lipolysis of lipid-based drug delivery systems:A newly identified relationship between drug release and liquid crystalline phase[J]. Biomed Res Int, 2016,2016:2364317.
[22]	Siqueira SD, M llertz A, Gr eser K, et al. Influence of drug load and physical form of cinnarizine in new SNEDDS dosing regimens:in vivo and in vitro evaluations[J]. AAPS J. 2017, 19(2):587-594.
[23]	Tanaka Y, Hara T, Waki R, et al. Regional differences in the components of luminal water from rat gastrointestinal tract and comparison with other species[J]. J Pharm Pharm Sci, 2012, 15(4):510-518.
[24]	Fatouros DG, Bergenstahl B, Mullertz A. Morphological observations on a lipid-based drug delivery system during in vitro digestion[J]. Eur J Pharm Sci, 2007, 31(2):85-94.
[25]	Roshan GD, Aagaard AE, Pedersen JS, et al. Experimental Set-up with flow-through cell with SAXS studies of in-situ degradation of drug formulations under gastro-intestinal mimicking conditions[R]. 13th International Conference of Small Angle Scattering, Kyoto:2006.
[26]	Sassene PJ, Knopp MM, Hesselkilde JZ, et al. Precipitation of a poorly soluble model drug during in vitro lipolysis:characterization and dissolution of the precipitate[J]. J Pharm Sci, 2010, 99(12):4982-4991.
[27]	Fernandez S, Jannin V, Chevrier S, et al. In vitro digestion of the self-emulsifying lipid excipient Labrasol by gastrointestinal lipases and influence of its colloidal structure on lipolysis rate[J]. Pharm Res, 2013, 30(12):3077-3087.

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Research progress on in vitro lipolysis model for the evaluation of lipid formulations

doi: 10.3969/j.issn.1006-0111.2017.06.001

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通讯作者: 陈斌, bchen63@163.com

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Research progress on in vitro lipolysis model for the evaluation of lipid formulations

doi: 10.3969/j.issn.1006-0111.2017.06.001

1. Department of Pharmacy, Nanfang Hospital of Southern Medical University, Guangzhou 510515, China

2. School of TCM, Guangdong Pharmaceutical University, Guangzhou 510006, China

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Research progress on in vitro lipolysis model for the evaluation of lipid formulations

doi: 10.3969/j.issn.1006-0111.2017.06.001

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References

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通讯作者: 陈斌, bchen63@163.com

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Research progress on in vitro lipolysis model for the evaluation of lipid formulations

doi: 10.3969/j.issn.1006-0111.2017.06.001

1. Department of Pharmacy, Nanfang Hospital of Southern Medical University, Guangzhou 510515, China 2. School of TCM, Guangdong Pharmaceutical University, Guangzhou 510006, China

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1. Department of Pharmacy, Nanfang Hospital of Southern Medical University, Guangzhou 510515, China

2. School of TCM, Guangdong Pharmaceutical University, Guangzhou 510006, China