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The contribution of absorption of integral nanocrystals to enhancement of Oral bioavailability of quercetin

Acta Pharmaceutica Sinica B 2021年第4期11卷 978-988页

作者： Baode Shen Chengying Shen Weifeng Zhu Hailong Yuan Department of Pharmacy Air Force Medical CenterPLABeijing 100142China Key Lab of Modern Preparation of Traditional Chinese Medicine(TCM) Ministry of EducationJiangxi University of TCMNanchang 330004China

In this study,self-discriminating hybrid nanocrystals was utilized to explore the biological fate of quercetin hybrid nanocrystals(QT-HNCs)with diameter around 280 nm(QT-HNCs-280)and550 nm(QT-HNCs-550)following oral and intravenous administration and the contribution of integral nanocrystals to Oral bioavailability enhancement of QT was estimated by comparing the absolute exposure of integral QT-HNCs and total QT in the liver.Results showed that QT-HNCs could reside in vivo as intact nanocrystals for as long as 48 h following oral and intravenous administration.A higher accumulation of integral QT-HNCs in liver and lung was observed for both oral and intravenous administration of QT-HNCs.The particle size affects the absorption and biodistribution of integral QT-HNCs and total QT.As compared to QT-HNCs-550,QT-HNCs-280 with smaller particle size is more easily absorbed,but dissolves faster in vivo,leading to higher distribution of QT(146.90 vs.117.91 h·mg/mL)but lower accumulation of integral nanocrystals(6.82 e10 vs.15.27 e10 h·[p/s]/[μW/cm2])in liver following oral administration.Due to its slower dissolution and enhanced recognition by RES,QT-HNCs-550 with larger diameter shows higher liver distribution for both of QT(1015.80 h·mg/mL)and integral nanocrystals(259.63 e10 h·[p/s]/[μW/cm2])than those of QT-HNCs-280(673.82&77.66 e10 h·[p/s]/[μW/cm2])following intravenous administration.The absolute exposure of integral QT-HNCs in liver following oral administration of QT-HNCs are 8.78%for QT-HNCs-280 and 5.88%for QT-HNCs-550,while the absolute exposure of total QT for QT-HNCs-280 and QT-HNCs-550 are 21.80%and 11.61%,respectively.Owing to imprecise quantifcation method,a surprisingly high contribution of integral QT-HNCs to Oral bioavailability enhancement of QT(40.27%for QT-HNCs-280 and 50.65%for QT-HNCs-550)was obtained.These results revealed signifcant difference in absorption and biodistrbution between integral nanocrystals and overall drugs following oral and intravenous administration of QT-HNCs,and provided a

关键词： Nanocrystals Biological fate Quercetin Pharmacokinetics Biodistribution Oral bioavailability Contribution Drug delivery

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Improved stability and Oral bioavailability of Ganneng dropping pills following transforming lignans of herpeto- spermum caudigerum into nanosuspensions

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Chinese Journal of Natural Medicines 2018年第1期16卷 70-80页

作者： LI Juan-Juan CHENG Ling SHEN Gang QIU Ling SHEN Cheng-Ying ZHENG Juan XU Rong YUAN Hai-Long Department of Pharmacy Air Force General Hospital of PLA Beijing 100142 China Department of Pharmacy Guangyuan Central Hospital Guanyuan 628000 China Department of Pharmacy Shuangliu District Maternal and Child Health Hospital Chengdu 610075 China Chengdu Institute of Chinese Herbal Medicine Chengdu 610045 China

The present study was designed to improve storage stability and Oral bioavailability of Ganneng dropping pills(GNDP) by transforming lignans of Herpetospermum caudigerum(HL) composed of herpetrione(HPE) and herpetin(HPN) into nanosuspension(HL-NS), the main active ingredient of GNDP, HL-NS was prepared by high pressure homogenization and lyophilized to transform into solid nanoparticles(HL nanoparticles), and then the formulated HL nanoparticles were perfused into matrix to obtain NS-GNDP by melting method. For a period of 3 months, the content uniformity, storage stability and pharmacokinetics test in vivo of NS-GNDP were evaluated and compared with regular GNDP at room temperature. The results demonstrated that uniformity of dosage units of NS-GNDP was acceptable according to the criteria of Chinese Pharmacopoeia 2015 J. Physical stability of NS-GNDP was investigated systemically using photon correlation spectroscopy(PCS), zeta potential measurement, and scanning electron microscopy(SEM). There was a slight increase in particles and PI of HL-NS re-dispersed from NS-GNDP after storage for 3 months, compared with new formulated NS-GNDP, which indicated a good redispersibility of the NS-GNDP containing HL-NS after storage. Besides, chemical stability of NS-GNDP was studied and the results revealed that HPE and HPN degradation was less when compared with that of GNDP, providing more than 99% of drug residue after storage for 3 months. In the dissolution test in vitro, NS-GNDP remarkably exhibited an increased dissolution velocity compared with GNDP and no distinct dissolution difference existed within 3 months. The pharmacokinetic study showed that HPE and HPN in NS-GNDP exhibited a significant increase in AUC0–t, Cmax and decrease in Tmax when compared with regular GNDP. These results indicated that NS-GNDP possessed superiority with improved storage stability and increased dissolution rate and Oral bioavailability.

关键词： Ganneng dropping pills Lignans Herpetospermum caudigerum Nanosuspensions Stability Oral bioavailability

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Formulation of dried lignans nanosuspension with high redispersibility to enhance stability,dissolution,and Oral bioavailability

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Chinese Journal of Natural Medicines 2016年第10期14卷 757-768页

作者： SHEN Gang CHENG Ling WANG Li-Qiang ZHANG Li-Hong SHEN Bao-De LIAO Wei-Bo LI Juan-Juan ZHENG Juan XU Rong YUAN Hai-Long Department of Pharmacy Air Force General Hospital of PLABeijing 100142China Pharmacy College Chengdu University of Traditional Chinese MedicineChengdu 611137China School of Biomedical Sciences Huaqiao UniversityQuanzhou 362021China

Herpetospermum caudigerum lignans(HTL), one of the potential drugs with anti-hepatitis B virus and hepatoprotective effects, has limited clinical applications because of poor aqueous solubility and low bioavailability. Both herpetrione(HPE) and herpetin(HPN) are the most abundant ingredients in HTL and exhibit weak acidity. The purpose of the present study was to produce dried preparations of HTL(composed of HPE and HPN) nanosuspensions(HTL-NS) with high redispersibility using lyophilization technology. The HTL-NS was prepared by utilizing precipitation-combined homogenization technology based on acid-base neutralization reactions, and critical formulation and process parameters affecting the characteristics of HTL-NS were optimized. The resultant products were characterized by particle size analysis, SEM, XRD, stability, solubility, dissolution and in vivo bioavailability. HTL-NS showed near-spherical-shaped morphology and the size was 243 nm with a narrow PDI value of 0.187. The dried preparations with a relatively large particle size of 286 nm and a PDI of 0.215 were achieved by using 4%(W/V) mannitol as cryoprotectants, and had a better stability at 4 or 25 oC for 2 months, compared to HTL-NS. In the in vitro test, the dried preparations showed markedly increased solubility and dissolution velocity. Besides, in the in vivo evaluation, it exhibited significant increases in AUC0–t, C_(max), MRT and a decrease in T_(max), compared to the raw drug.. In conclusion, our results provide a basis for the development of a drug delivery system for poorly water-soluble ingredients with p H-dependent solubility.

关键词： Herpetospermum caudigerum lignans Nanosuspensions Acid-base neutralization Saturation solubility Dissolution Oral bioavailability

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Semi-elastic core-shell nanoparticles enhanced the Oral bioavailability of peptide drugs

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Chinese Chemical Letters 2020年第5期31卷 1147-1152页

作者： Shengnan Zhao Jinhua Li Fazhan Wang Ting Yu Yang Zhou Lili He Yi Zhang jian Yang School of Applied Chemistry and Biological Technology Shenzhen PolytechnicShenzhen 518055China Department of Pancreatic Surgery West China HospitalSichuan University.Chengdu 610041China College of Pharmacy Southwest Minzu UniversityChengdu 610041China

The rigidity of nanoparticles was newly reported to influence their oral delivery.Semi-elastic nanoparticles can enhance the penetration in mucus and uptake by epithelial cells.However,it is still challenging and unclear that the semi-elastic core-shell nanoparticles can enhance the Oral bioavailability of peptide drugs.This study was for the first time to validate the semi-elastic coreshell poly(lactic-co-glycolic acid)(PLGA)-lipid nanoparticles(LNPs)as the carrier of the oral peptide drug.The antihypertensive peptide Val-Leu-Pro-Val-Pro(VP5)loaded LNPs(VP5-LNPs)were prepared by a modified thin-film ultrasonic dispersion method.Uptake experiment was performed in Caco-2 and HT-29 cells and monito red by high content screening(HCS)and flow cyto metric(FCM).Pharmacokinetics of VP5-LNPs was carried out in Sprague-Dawley(SD)rats and analyzed by DAS 2.0.The optimal VP5-LNPs had an average particle size of 247.3±3.8 nm,zeta potential of-6.57±0.45 mV and excellent entrapment efficiency(EE)of 89.88%±1.23%.Transmission electron microscope(TEM)and Differential scanning calorimeter(DSC)further confirmed the core-shell structure.VP5-LNPs could increase the cellular uptake in vitro and have a 2.55-fold increase in AUC0-72 h,indicating a great promotion of the o ral bioavailability.The semi-elastic LNPs remarkably improved the oral availability of peptide and could be a promising oral peptide delivery system for peptide drugs in the future.

关键词： Semi-elastic nanoparticles Oral bioavailability Lipid nanoparticles Antihypertensive peptide Pharmacokinetics

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Pharmacokinetic behaviors and Oral bioavailability of oridonin in rat plasma

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Acta Pharmacologica Sinica 2006年第12期27卷 1642-1646页

作者： Wen XU~2 Jin SUN~2 Ting-ting ZHANG~2 Bo MA~2 Sheng-miao CUI~3 Da-wei CHEN~2 Zhong-gui HE~(2,4)2 Department of Pharmaceutics,School of Pharmacy,Shenyang Pharmaceutical University,Shenyang 110016,China 3 Department of Pharmacy,Guangdong Pharmaceutical University,Guangzhou 510006,China Department of Pharmaceutics School of Pharmacy Shenyang Pharmaceutical University Shenyang China Department of Pharmacy Guangdong Pharmaceutical University Guangzhou China

Aim:To study the intravenous and oral pharmacokinetic behavior of oridonin andits extent of absolute Oral bioavailability in rats.Methods:Oridonin was adminis-tered to rats via iv(5,10 and 15 mg/kg),po(20,40 and 80 mg/kg)or ip administra-tion(10 mg/kg).The concentrations of oridonin in rat plasma were determined bya high performance liquid chromatography with electrospray ionization mass spec-trometric detection(HPLC/ESI-MS)method and the pharmacokinetic parameterswere determined by non-compartmental analysis.Results:The plasma concen-tration of oridonin after intravenous administration decreased polyexponentially,and the pharmacokinetic parameters of oridonin were dose-independent withinthe examined range.Oridonin was absorbed rapidly after oral gavage with a t(max)ofless than 15 min;the extent of absolute bioavailability of oridonin following oraladministration was 4.32%,4.58% and 10.8%.The extent of absolute bioavailabilityof oridonin following intraperitoneal administration was 12.6%.Conclusion:Firstorder rate pharmacokinetics were observed for oridonin within the range of ivdoses,while the extent of absolute Oral bioavailability was rather low and dose-dependent.The low and dose-dependent extent of Oral bioavailability may be dueto the saturation of first-pass effects.

关键词： oridonin pharmacokinetics intravenous Oral bioavailability intraperitoneal injections rats

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Enhancement of Oral bioavailability and Anti-Parkinsonian Efficacy of Resveratrol by a Nanocrystal Formulation

Enhancement of Oral Bioavailability and Anti-Parkinsonian Ef...

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2018年第十二届中国药物制剂大会

作者：熊莎 Wei Liu Xiaojia Chen Qi Wang Dongsheng Yuan Tongkai Chen Institute of Clinical Pharmacology Guangzhou University of Chinese Medicine State Key Laboratory of Quality Research in Chinese Medicine Institute of Chinese Medical Sciences University of Macau

Resveratrol（RES）, a non-flavonoid polyphenol extracted from a wide variety of plants, possesses neuroprotective activity for the treatment of Parkinson’s disease（PD）. However, the poor water solubility of RES results in low Oral bioavailability, which causes low exposure of RES in the blood and brain, and limits its anti-Parkinsonian efficacy and clinical application. In this study, a nanocrystal formulation of RES（RESNCs） was developed to improve its solubility and Oral bioavailability and thus to treat PD. The RES-NCs were fabricated using an anti-solvent precipitation approach where hydroxypropyl methylcellulose（HPMC） was optimized as the stabilizer. The obtained RES-NCs had a particle size of 222.54 ± 1.66 nm with a PDI of 0.12 ± 0.03, and the RES-NCs exhibited a fast dissolution rate in vitro. Differential scanning calorimetry（DSC） and powder X-ray diffraction（PXRD） results demonstrated that the RES was maintained in the crystalline state in the fabricated nanocrystals. Molecular dynamics simulation of RES and HPMC exhibited an interaction and binding energy of-68.09 kJ/mol and-30.98 ± 0.388 kJ/mol, respectively with van der Waals interactions in the spontaneous binding. The cellular uptake and permeability of RES-NCs were much higher than those of the raw RES in Madin-Darby Canine Kidney（MDCK） cells（p＜0.01）. In addition, the RES-NCs afforded a significant neuroprotective effect against 1-methyl-4-phenylpyridinium ion（MPP+）-induced damage in SH-SY5 Y cells. Meanwhile, the zebrafish embryos and larvae treated with RES-NCs did not show any obvious toxic effects during the entire experiment. When RES-NCs were orally administrated to rats, the drug was absorbed quickly and a maximum plasma concentration of 2.97 ± 0.46 μg/ml was reached in 2.11 ± 0.05 h. Compared to the unformulated RES, the Cmax and AUC0-24 h of RES-NCs were increased nearly 3.09-and 3.52-fold, respectively, indicating that the RES-NCs could effectively enhance RES oral absorption. The RES-NCs also resulted in markedly higher brain Cmax and AUC0

关键词： Nanocrystals Resveratrol Oral bioavailability Anti-Parkinsonian Efficacy Parkinson’s disease

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One-step self-assembled nanomicelles for improving the Oral bioavailability of nimodipine

One-step self-assembled nanomicelles for improving the oral ...

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2018年第十二届中国药物制剂大会

作者：罗静雯 Zhi-Rong Zhang Tao Gong Yao Fu Key Laboratory of Drug-Targeting and Drug Delivery System of the Education Ministry Sichuan Engineering Laboratory for Plant-Sourced Drug and Sichuan Research Center for Drug Precision Industrial Technology West China School of Pharmacy Sichuan University

Our study aimed to develop a self-assembled nanomicelle for oral administration of nimodipine(NIM) with poor water solubility. The NIM-loaded self-assembled nanomicelles were prepared according to the one-step self-assembled technique. Briefly, NIM and Solutol HS15 were added in the flask by gently stirring at 60°C for 30 minutes. Using Solutol HS15, the NIM loaded self-assembled nanomicelles displayed a near spherical morphology with a narrow size distribution of 12.57 ± 0.21 nm(PDI = 0.071 ± 0.011). Compared with Nimotop(NIM tablets), the intestinal absorption of NIM from NIM nanomicelle in rats was improved by 3.13-and 2.25-fold in duodenum and jejunum at 1 h after oral administration. The cellular transport of NIM nanomicelle in Caco-2 cell monolayers was significantly enhanced compared to Nimotop?. Regarding the transport pathways, clathrin, lipid raft/caveolae and macropinocytosis mediated the cell uptake of NIM nanomicelles, while P-glycoprotein and endoplasmic reticulum/Golgi complex(ER/Golgi) pathways were involved in the exocytosis. Pharmacokinetic study showed that the AUC of NIM nanomicelles was 3.72-fold that of Nimotop? via oral administration in rats. Moreover, the NIM concentration in brain from NIM nanomicelle was dramatically improved. Therefore, Solutol HS15 based self-assembled nanomicelles represent a promising delivery system to enhance the Oral bioavailability of NIM.

关键词： Nanomicelles Self-assembly Nimodipine Oral bioavailability Transport mechanism

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Potentials of proniosomes for improving the Oral bioavailability of poorly water-soluble drugs

Potentials of proniosomes for improving the oral bioavailabi...

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2012年中国药学大会暨第十二届中国药师周

作者：宋双双沈阳药科大学

本研究的目的是制备一种用于装载难溶性药物的、流动性和稳定性极好的前体囊泡制剂并且评价其作为口服给药系统的生物利用度。将司盘60、胆固醇、山梨醇、长春西汀通过薄膜分散法制备成前体囊泡粉末。将适量的前体囊泡粉末与水混合后,... 详细信息

本研究的目的是制备一种用于装载难溶性药物的、流动性和稳定性极好的前体囊泡制剂并且评价其作为口服给药系统的生物利用度。将司盘60、胆固醇、山梨醇、长春西汀通过薄膜分散法制备成前体囊泡粉末。将适量的前体囊泡粉末与水混合后,囊泡会自发形成。本论文对前体囊泡粉末和由其形成的自主装囊泡混悬液的包封率、粒径、形态学特征、体外溶出和释放、物理稳定性和体内生物利用度进行了评价。前体囊泡粉末具有良好的流动性。投射电子显微镜下观察到由前体囊泡自主装形成的囊泡混悬液呈现圆球状。X射线显示药物以无定形或分子状态存在于前体囊泡粉末中。从体外溶出和释放研究中可看出前体囊泡粉末确实提高了长春西汀的溶出速率和溶出量。而且,自组装的囊泡混悬液显示出缓慢释放药物的特性。与长春西汀混悬液相比,由前体囊泡粉末自主装形成的囊泡混悬液确实提高了长春西汀在新西兰兔中的生物利用度。本研究表明前体囊泡粉末大大提高了制剂的物理和化学稳定性,具有一定的工业前景。

关键词： proniosomes poorly water-soluble drugs vinpocetine reconstituted/proniosome-derived niosomes Oral bioavailability

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Phospholipid-bile salts-mixed micelles incorporated in oral fast dissolving films for improving the Oral bioavailability of poorly water soluble drugs

Phospholipid-bile salts-mixed micelles incorporated in oral ...

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“好医生杯”中药制剂创新与发展论坛

作者： Qingyuan Lv Minggui Lin Chao Yu Baode Shen He Xu Chengying Shen Ling Dai Hailong Yuan Jin Han Department of Pharmacy 302 Military Hospital Institute of Tuberculosis 309 Military Hospital

The phospholipid-bile salts-mixed micelles(PL-BS-MMs)are potent carriers used for oral absorption of drugs that are poorly soluble in water;however,there are many limitations associated with liquid formulations.In the current study,the feasibility of preparing a solid PL-BS-MMs by incorporating liquid PL/SDC-MMs with solid fast dissolving oral films(FDOFs)carriers was examined.FDOFs incorporated with Cucurbitacin B(Cu B)loaded PL-BS-MMs have been developed and characterised.FDOFs were produced by solvent casting method.The formulation presenting the best characteristics before solidifying and after reconstitution.FDOFs containing Cu B loaded PL/SDC-MMs was easily reconstituted in a transparent and clear solution giving back a colloidal system with spherical micelles in the submicron range.The pharmacokinetics study showed that the FDOFs containing PL/SDC-MMs not only kept the absorption properties as same as liquid PL/SDC-MMs,but also significantly increased the Oral bioavailability of Cu B compared to the Cu B solution(poral administration.Furthermore,the integration with the FDOFs could also provide a simple and cost-effective manner for the solidification of PL/SDC-MMs.

关键词： Cucurbitacin B phospholipid-bile salts-mixed micelles fast dissolving oral films Oral bioavailability poorly water soluble drugs

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Chylomicron-mimicked Bio-self-assembling MSNs to improve bioavailability of oral Drugs via Promoting Lymphatic Transport

Chylomicron-mimicked Bio-self-assembling MSNs to improve bio...

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2018年第十二届中国药物制剂大会

作者：毛玉玲 Qinfu ZHAO Da WANG Siling WANG Department of Pharmaceutics School of Pharmacy Shenyang Pharmaceutical University

Lymphatic transport of oral drugs allows extraordinary gains in bioavailability and efficacy through avoidance of first-pass hepatic metabolism and reservation drugs at lymphatic tissues against lymphmediated diseases. This drug absorption pathway plays a win-win role in both pharmacokinetics and pharmacodynamics for antiretroviral therapy to fully suppress HIV. Herein, with the inspiration of triglyceride digestion process in the daily diet, we engineered a triglyceride-mimicked mesoporous silica nanocarrier（namely TMCMS） to promote lymphatic transport of antiretroviral drugs. Taking lopinavir（LNV） as a model antiretroviral drug with hurdles of poor solubility, high first pass effect and off-target disposition, TMCMS vector exhibited several properties belonging to ideal nanocarriers of high drug load, amorphous dispersion and controlled release in gastrointestinal tract, and also a perfect hydrolysis performance similar to TG pre-uptake. Subsequently, TMCMS showed a serious of TG-mimetic transport features across intestinal epithelial cells: hydrolysis–re-esterification–chylomicron assembly, participating into such a biochemical process and self-assembling to a chylomicron-associated TMCMS（namely TMCMS@CM） in enterocytes. As a result, TMCMS brought 10.6 folds Oral bioavailability through circumventing first-pass metabolism through lymphatic transport pathway. Our study provides evidences of using the bio-selfassembling TMCMS nanocarrier to facilitate bioavailability and efficacy via lymphatic transport of oral drugs.

关键词： lymphatic transport antiretroviral therapy Oral bioavailability first-pass metabolism lymphatic target mesoporous silica nanocarrier lopinavir

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