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CHEN Lina, CHEN Jianming. The influence of log P value of insoluble drugs on drug-loading properties of nano-lipid emulsion[J]. Journal of Pharmaceutical Practice and Service, 2015, 33(6): 513-517. doi: 10.3969/j.issn.1006-0111.2015.06.009
Citation: CHEN Lina, CHEN Jianming. The influence of log P value of insoluble drugs on drug-loading properties of nano-lipid emulsion[J]. Journal of Pharmaceutical Practice and Service, 2015, 33(6): 513-517. doi: 10.3969/j.issn.1006-0111.2015.06.009

The influence of log P value of insoluble drugs on drug-loading properties of nano-lipid emulsion

doi: 10.3969/j.issn.1006-0111.2015.06.009
  • Received Date: 2015-06-08
  • Rev Recd Date: 2015-10-08
  • Objective To study the influence on common logarithm of partition-coefficient (log P) value of insoluble drugs on nano-lipid emulsion properties, including drug-loading amount, in vitro release, and phase distribution etc. Methods 6 insoluble drugs, nimodipine (NIM), docetaxel (DTX), curcumin (CUR), paclitaxel (PTX), teniposide (TEN), silybin (SLB), were selected as the model drugs, to investigate the relationship between log P value and nano-lipid emulsion of the dissolubility in PEG400, the amount of drug-loading, particle diameter, Zeta potential, in vitro release, and phase distribution respectively. Results With the increase of log P value, drug solubility in PEG400 first increased and then decreased, drug-loading in nano-lipid emulsion increased, release rate in vitro of drug slowed down, drug distribution in oil phase increased while in emulsion layer decreased. Log P value has no correlation with particle diameter and Zeta potential. Conclusion The properties of drug-loading nano-lipid emulsion can be preliminarily judged by log P values and the solubility in PEG400 of drugs.
  • [1] Jing X, Deng L, Gao B, et al. A novel polyethylene glycol mediated lipid nanoemulsion as drug delivery carrier for paclitaxel[J]. Nanomedicine, 2014, 10(2): 371-380.
    [2] 张婷婷,徐 文,胡生亮,等. 水飞蓟宾在不同介质中平衡溶解度和表观分配系数的测定[J]. 中国药学杂志,20006,41(20):1569-1571.
    [3] 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): 475-485.
    [4] Shaikh J, Ankola DD, Beniwal V, et al. Nanoparticle encapsulation improves oral bioavailability of curcumin by at least 9-fold when compared to curcumin administered with piperine as absorption enhancer[J]. Eur J Pharm Sci, 2009, 37(3-4): 223-230.
    [5] 高晓黎,孙殿甲,程利勇,等. 去氢骆驼蓬碱注射用乳剂中药物的相分布和体外释放研究[J].中成药,2000,22(2):111-115.
    [6] Korinth G, Wellner T, Schaller K. H, et al. Potential of the octanol-water partition coefficient (logP) to predict the dermal penetration behaviour of amphiphilic compounds in aqueous solutions[J]. Toxicol Lett, 2012, 215(1): 49-53.
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    [8] Maiti K, Mukherjee K, Gantait A, et al. Curcumin-phospholipid complex: preparation, therapeutic evaluation and pharmacokinetic study in rats[J]. Int J Pharm, 2007, 330(1-2): 155-163.
    [9] Zanotto-Filho A, Coradini K, Braganhol E, et al. Curcumin-loaded lipid-core nanocapsules as a strategy to improve pharmacological efficacy of curcumin in glioma treatment[J]. Eur J Pharm Biopharm, 2013, 83(2): 156-167.
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The influence of log P value of insoluble drugs on drug-loading properties of nano-lipid emulsion

doi: 10.3969/j.issn.1006-0111.2015.06.009

Abstract: Objective To study the influence on common logarithm of partition-coefficient (log P) value of insoluble drugs on nano-lipid emulsion properties, including drug-loading amount, in vitro release, and phase distribution etc. Methods 6 insoluble drugs, nimodipine (NIM), docetaxel (DTX), curcumin (CUR), paclitaxel (PTX), teniposide (TEN), silybin (SLB), were selected as the model drugs, to investigate the relationship between log P value and nano-lipid emulsion of the dissolubility in PEG400, the amount of drug-loading, particle diameter, Zeta potential, in vitro release, and phase distribution respectively. Results With the increase of log P value, drug solubility in PEG400 first increased and then decreased, drug-loading in nano-lipid emulsion increased, release rate in vitro of drug slowed down, drug distribution in oil phase increased while in emulsion layer decreased. Log P value has no correlation with particle diameter and Zeta potential. Conclusion The properties of drug-loading nano-lipid emulsion can be preliminarily judged by log P values and the solubility in PEG400 of drugs.

CHEN Lina, CHEN Jianming. The influence of log P value of insoluble drugs on drug-loading properties of nano-lipid emulsion[J]. Journal of Pharmaceutical Practice and Service, 2015, 33(6): 513-517. doi: 10.3969/j.issn.1006-0111.2015.06.009
Citation: CHEN Lina, CHEN Jianming. The influence of log P value of insoluble drugs on drug-loading properties of nano-lipid emulsion[J]. Journal of Pharmaceutical Practice and Service, 2015, 33(6): 513-517. doi: 10.3969/j.issn.1006-0111.2015.06.009
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