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β-Lactoglobulin stabilized lipid nanoparticles enhance oral absorption of insulin by slowing down lipolysis

Chinese Chemical Letters 2024年第4期35卷 287-291页

作者： Lu Li Suticha Chunta Xianzi Zheng Haisheng He Wei Wu Yi Lu School of Pharmacy&Key Laboratory of Smart Drug Delivery of MOE Fudan UniversityShanghai 201203China Department of Clinical Chemistry Faculty of Medical TechnologyPrince of Songkla UniversitySongkhla 90110Thailand Shanghai Skin Disease Hospital Tongji University School of MedicineShanghai 200433China Fudan Zhangjiang Institute Shanghai 201203China

Lipid-based nanocarriers have staged a remarkable comeback in the oral delivery of proteins and peptides, but delivery efficiency is compromised by lipolysis. β-Lactoglobulin(β-lg) stabilized lipid nanoparticles, including nanoemulsions(NE@β-lg) and nanocapsules(NC@β-lg), were developed to enhance the oral absorption of insulin by slowing down lipolysis due to the protection from β-lg. Cremophor EL stabilized nanoemulsions(NE@Cre-EL) were prepared and set as a control. The lipid nanoparticles produced mild and sustained hypoglycemic effects, amounting to oral bioavailability of 3.0% ± 0.3%, 7.0% ± 1.1%, and7.7% ± 0.8% for NE@Cre-EL, NE@β-lg, and NC@β-lg, respectively. Aggregation-caused quenching(ACQ)probes enabled the identification of intact nanoparticles, which were used to investigate the in vivo and intracellular fates of the lipid nanoparticles. In vitro digestion/lipolysis and ex vivo imaging confirmed delayed lipolysis from β-lg stabilized lipid nanoparticles. NC@β-lg was more resistant to intestinal lipolysis than NE@β-lg due to the Ca^(2+)-induced crosslinking. Live imaging revealed the transepithelial transport of intact nanoparticles and their accumulation in the liver. Cellular studies confirmed the uptake of intact nanoparticles. Slowing down lipolysis via food proteins represents a good strategy to enhance the oral absorption of lipid nanoparticles and thus co-formulated biomacromolecules.

关键词： β-Lactoglobulin Lipid nanoparticles oral absorption Insulin Lipolysis Aggregation-caused quenching

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Effect of acidity of drugs on the prediction of human oral absorption by biopartitioning micellar chromatography

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Journal of Pharmaceutical Analysis 2010年第4期22卷 233-240页

作者： Xiao-Juan Ren1,Shu-Rong Wang2,Li-Ping Wu1,Yu-Jie Liu1,Cong Chen1,Li-Ming Ye11.West China School of Pharmacy,Sichuan University,Chengdu 610041 2.The Affiliated Hospital of Luzhou Medical College,Luzhou 646000,China West China School of Pharmacy Sichuan University Chengdu 610041 China Luzhou Medical College Luzhou 646000 China

Biopartitioning micellar chromatography(BMC)is a potentially high throughput and low cost alternative for in vitro prediction of drug absorption,which can mimic the drug partitioning process in biological systems.In this paper,a data set of 56 compounds representing acidic,basic,neutral and amphoteric drugs from various structure classes with human oral absorption(HOA)data available were employed to show the effect of acidity of drugs in oral absorption prediction.HOA was reciprocally correlated to the negative value of the capacity factor(kBMC)determined by BMC at pH 7.4 and 6.5.The relationships between kBMC and the corresponding HOA values of all compounds were rather poor,but the correlations were improved when the acidity of drugs was taken into consideration.Moreover,the proposed models allowed obtaining of good predictive values for both highly and poorly absorbed compounds.It is demonstrated that the constructed models derived from compounds with the same kind of charge property are of more practically meaningful and rigorous.

关键词： biopartitioning micellar chromatography oral absorption acidity

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Enhancement of oral bioavailability and anti-Parkinsonian efficacy of resveratrol through a nanocrystal formulation

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Asian Journal of Pharmaceutical Sciences 2020年第4期15卷 518-528页

作者： Sha Xiong Wei Liu Yile Zhou Yousheng Mo Yao Liu Xiaojia Chen Huafeng Pan Dongsheng Yuan QiWang Tongkai Chen Institute of Clinical Pharmacology Guangzhou University of Chinese MedicineGuangzhou 510405China Institute of Chinese Medical Sciences University of MacaoMacaoChina

Resveratrol(RES),a non-flavonoid polyphenol extracted from a wide variety of plants,exhibits neuroprotective activities against Parkinson’s disease(PD).However,undesirable water solubility of RES reduces its oral bioavailability and demonstrates lowefficacy in blood and brain,thus limiting its application.In present study,a nanocrystal formulation of RES(RES-NCs)was developed to enhance its oral bioavailability and delivery into brain for PD treatment.RES-NCs were fabricated with hydroxypropyl methylcellulose(HPMC)stabilizer via antisolvent precipitation approach.The obtained RES-NCs displayed the particle size of 222.54±1.66 nm,the PDI of 0.125±0.035,the zeta potential of−9.41±0.37mV,and a rapid in vitro dissolution rate.Molecular dynamics simulation of RES and HPMC revealed an interaction energy of−68.09 kJ/mol and a binding energy of−30.98±0.388 kJ/mol,indicating that the spontaneous binding between the two molecules is through van der Waals forces.RES-NCs conferred enhanced cellular uptake as well as improved permeability relative to pure RES.In addition,RES-NCs were able to protect neurons against cytotoxicity induced by MPP+.Meanwhile,RES-NCs exerted no significant toxic effects on zebrafish embryos and larvae,and did not influence their survival and hatching rates.When orally administered to rats,RES-NCs exhibited more favorable pharmacokinetics than pure RES,with higher plasma and brain concentrations.More importantly,MPTP-induced PD mice showed notable improvements in behavior,attenuated dopamine deficiency,and elevated levels of dopamine and its metabolites after the treatment with RES-NCs.Furthermore,immunoblot analysis revealed that the neuroprotective role of RES-NCsmay be at least partially mediated by Akt/Gsk3βsignaling pathway.Taken altogether,RES-NCs can serve as a potential treatment modality for PD,offering means of improving RES oral bioavailability and brain accumulation.

关键词： Nanocrystals Resveratrol oral absorption Brain permeability Anti-Parkinsonian efficacy

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Enhanced digestion inhibition and mucus penetration of F127-modified self-nanoemulsions for improved oral delivery

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Asian Journal of Pharmaceutical Sciences 2018年第4期13卷 326-335页

作者： Wenyi Song Yuting Yang Miaorong Yu Quanlei Zhu Mohammadali Soleimani Damaneh Haijun Zhong Yong Gan Department of Pharmacy Medical College of Nanchang University Shanghai Institute of Materia Medica Chinese Academy of Sciences University of Chinese Academy of Sciences Division of Anti-tumor Pharmacology State Key Laboratory of Drug ResearchShanghai Institute of Materia MedicaChinese Academy of Sciences

Self-nanoemulsifying systems(SNEs) have excellent ability to improve the solubility ofpoorly water-soluble drugs(PWSD). However, SNEs are likely to be degraded in gastroin-testinal(GIT) when their surface is recognized by lipase/co-lipase enzyme complex, result-ing in rapid release and precipitation of encapsulated drugs. The precipitates are then cap-tured and removed by intestinal mucus, reducing the delivery efficacy of SNEs. Herein, theamphiphilic polymer Pluronic? F127 was incorporated into long and short-chain triglyc-erides(LCT, SCT) based SNEs to diminish the recognition and therefore minimized theirdegradation by enzymes and clearance by mucus. The SNEs were characterized in termsof particle size, zeta potential and stability. Ex vivo multiple particles tracking studies wereperformed by adding particle solution into fresh rat mucus. Cellular uptake of SNEs wereconducted by using E12 cells, the absorption and distribution in small intestine were alsostudied after oral administration in male Sprague-Dawley(SD) rats. The in vitro digestionrate of SNEs were found to be in following order SCT-SNE > SCT-F127-SNE > LCT-SNE > LCT-F127-SNE. Moreover, the LCT-F127-SNE was found to be most effective in enhancing cellularuptake, resulting in 3.5-fold, 2.1-fold and 1.7-fold higher than that of SCT-SNE, LCT-SNE andSCT-F127-SNE, respectively. After incubating the SNE with E12 cells, the LCT-F127-SNE ex-hibited the highest amount regarding both mucus penetration and cellular uptake, with anuptake amount number(via bicinchoninic acid(BCA) analysis) of 3.5-fold, 2.1-fold and 1.7-fold higher than that of SCT-SNE, LCT-SNE and SCT-F127-SNE, respectively. The in vivo results revealed that orally administered LCT-F127-SNE could significantly increase the bioavailability of Cyclosporine A(CsA), which was approximately 2.43-fold, 1.33-fold and 1.80-fold higher than that of SCT-SNE, SCT-F127-SNE and LCT-SNE, respectively. We address in this work that F127-modified SNEs have potentials to improve oral drug absorption by significan

关键词： Self-nanoemulsifying system(SNEs) oral absorption Enzymatic degradation Mucus penetration Pluronic^(■) F127

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Therapeutic Effects of Curcumin Nanoemulsions on Prostate Cancer

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Journal of Huazhong University of Science and Technology(Medical Sciences) 2017年第3期37卷 371-378页

作者：关延彬周树瑶张玉琼王佳乐田雨冬贾永艳孙彦君 school of pharmacy henan university of traditional chinese medicineZhengzhou 450001China collaborative innovation center for respiratory disease diagnosis and treatment&chinese medicine development of henan province Zhengzhou 450001China department of urology the first affiliated hospital of zhengzhou universityZhengzhou 450000China

The therapeutic potential of curcumin(Cur) is hampered by its poor aqueous solubility and low bioavailability. The aim of this study was to determine whether Cur nanoemulsions enhance the efficacy of Cur against prostate cancer cells and increase the oral absorption of Cur. Cur nanoemulsions were developed using the self-microemulsifying method and characterized by their morphology, droplet size and zeta potential. The results showed that the cytotoxicity and cell uptake were considerably increased with Cur nanoemulsions compared to free Cur. Cur nanoemulsions exhibited a significantly prolonged biological activity and demonstrated better therapeutic efficacy than free Cur, as assessed by apoptosis and cell cycle studies. In situ single-pass perfusion studies demonstrated higher effective permeability coefficient and absorption rate constant for Cur nanoemulsions than for free Cur. Our study suggested that Cur nanoemulsions can be used as an effective drug delivery system to enhance the anticancer effect and oral bioavailability of Cur.

关键词： curcumin nanoemulsion prostate cancer anticancer efficacy oral absorption

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Intestinal Permeability of Glycosides(aglycone) from Rhodiola in the Human Caco-2 Cell Monolayer Model

Intestinal Permeability of Glycosides(aglycone) from Rhodiol...

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2013全国中药与天然药物高峰论坛暨第十三届全国中药和...

作者： Tian-Xiang Ma Jiu-Hong Wu Department of Pharmacy 306 Hospital of PLA

The bidirectional intestinal permeability of 4 glycosides(aglycone) from anti-radiation Chinese medicinal herb Rhodiola,including Salidroside,Rosavin,Rosarin,and Tyrosol, was studied by using the Caco-2 cell monolayer... 详细信息

关键词： Rhodiola glycosides oral absorption Caco-2 cell monolayer

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氧化苦参碱磷脂复合物的制备、评价及药代动力学研究(英文)

氧化苦参碱磷脂复合物的制备、评价及药代动力学研究(英文)

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第二届中药现代化新剂型新技术国际学术会议

作者：袁海龙杨明游荣辉李仙义张倩韩玉梅肖小河解放军302医院暨解放军中药研究所江西中医学院中药现代制剂教育部重点实验室成都中医药大学

The aim of the present study was to prepare oxymatrine-phospholipid complex to enhance oral bioavailability of oxymatrine and to study its physicochemical properties and to compare the pharmacokinetic characteristics and bioavailability after oral administration of oxymatrine-phospholipid complex and oxymatrine in rats. Using tetrahydrofuran as a reaction medium, oxymatrine and phospholipids were resolved into the medium, after the organic solvent was removed under vacuum condition, oxymatrine-phospholipid complex was formed. The new complex’s physicochemical properties including scanning electron microscopy (SEM), transmission electron microscopy (TEM), differential scanning calorimetry (DSC), 1R, X-ray diffraction (XRD), particle size distribution and solubility were tested. The hepatocytes permeability of oxymatrine-phospholipid complex and oxymatrine were investigated. The concentrations of oxymatrine after oral administration of oxymatrine-phospholipids complex and oxymatrine at different time in rats were determined by HPCE. The pharmacokinetic parameters were computed by software program 3p87. The data showed that oxymatrine and phospholipids in the oxymatrine-phospholipid complex were combined by non-covalent bond, not forming a new compound and the solubility of oxymatrine -phospholipid complex in n-octanol was effectively enhanced. The better hepatocytes permeability was obtained by the phospholipid complex. We found that mean plasma concentration-time curve of oxymatrine after oral administration of oxymatrine-phospholipid complex and oxymatrine in rats was both in accordance with open two-compartment model with first-order absorption. Pharmacokinetic parameters of oxymatrine and the complex in rats were Tmax 1.86 and 1.76 h, Cmax 0.14 and 0.38 μg ml-1, AUC0-∞ 1.97 and 6.21 μg/ml h, respectively. The bioavailability of oxymatrine in rats was increased remarkably after oral administration of oxymatrine-phospholipid complex comparing to oxymatrine. This was mainly due to an impressive improvement of the

关键词： Oxymatrine Phospholipid complex Physicochemical properties Hepatocytes permeability Bioavailability Pharmacokinetics oral absorption

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