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Acta Pharmaceutica Sinica. B

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https://read.qxmd.com/read/30766791/exploring-the-utility-of-the-chasing-principle-influence-of-drug-free-snedds-composition-on-solubilization-of-carvedilol-cinnarizine-and-r3040-in-aqueous-suspension
#1
ScheylaDaniela Siqueira Jørgensen, Thomas Rades, Huiling Mu, Kirsten Graeser, Anette Müllertz
This study assessed the influence of the composition of drug-free SNEDDS co-dosed with aqueous suspensions of carvedilol (CAR), cinnarizine (CIN) or R3040 on drug solubilization in a two-compartment in vitro lipolysis model. Correlation of drug log P or solubility in SNEDDS with drug solubilization during in vitro lipolysis in the presence of drug-free SNEDDS was assessed. SNEDDS with varying ratios of soybean oil:Maisine 35-1 (1:1, w / w ) and Kolliphor RH40, with ethanol at 10% ( w / w ) were used. SNEDDS were named F65, F55 and F20 (numbers refer to the percentage of lipids) and aqueous suspensions without drug-free SNEDDS (F0) were also analyzed...
January 2019: Acta Pharmaceutica Sinica. B
https://read.qxmd.com/read/30766790/interaction-between-human-serum-albumin-and-cholesterol-grafted-polyglutamate-as-the-potential-carriers-of-protein-drugs
#2
Xiangxue Lyu, Qiufen Zhang, Dehai Liang, Yanbin Huang
Currently there is no successful platform technology for the sustained release of protein drugs. It seems inevitable to specifically develop new materials for such purpose, and hence the understanding of protein-material interactions is highly desirable. In this study, we synthesized cholesterol-grafted polyglutamate (PGA- g -Chol) as a hydrophobically-modified polypeptide, and thoroughly characterized its interaction with a model protein (human serum albumin) in the aqueous solution by using circular dichroism, fluorescence methods, and light scattering...
January 2019: Acta Pharmaceutica Sinica. B
https://read.qxmd.com/read/30766789/deep-learning-for-in-vitro-prediction-of-pharmaceutical-formulations
#3
Yilong Yang, Zhuyifan Ye, Yan Su, Qianqian Zhao, Xiaoshan Li, Defang Ouyang
Current pharmaceutical formulation development still strongly relies on the traditional trial-and-error methods of pharmaceutical scientists. This approach is laborious, time-consuming and costly. Recently, deep learning has been widely applied in many challenging domains because of its important capability of automatic feature extraction. The aim of the present research is to apply deep learning methods to predict pharmaceutical formulations. In this paper, two types of dosage forms were chosen as model systems...
January 2019: Acta Pharmaceutica Sinica. B
https://read.qxmd.com/read/30766788/efficient-lung-cancer-targeted-drug-delivery-via-a-nanoparticle-msc-system
#4
Xusheng Wang, Haiyan Chen, Xiaowei Zeng, Wenpeng Guo, Yu Jin, Shan Wang, Ruiyun Tian, Yanjiang Han, Ling Guo, Jimin Han, Yaojiong Wu, Lin Mei
Low targeting efficiency limits the applications of nanoparticles in cancer therapy. The fact that mesenchymal stem cells (MSC) trapped in the lung after systemic infusion is a disadvantage for cell therapy purposes. Here, we utilized MSC as lung cancer-targeted drug delivery vehicles by loading nanoparticles (NP) with anti-cancer drug. MSC showed a higher drug intake capacity than fibroblasts. In addition, MSC showed predominant lung trapping in both rabbit and monkey. IR-780 dye, a fluorescent probe used to represent docetaxel (DTX) in NP, delivered via MSC accumulated in the lung...
January 2019: Acta Pharmaceutica Sinica. B
https://read.qxmd.com/read/30766787/pharmacometabolomic-prediction-of-individual-differences-of-gastrointestinal-toxicity-complicating-myelosuppression-in-rats-induced-by-irinotecan
#5
Yiqiao Gao, Wei Li, Jiaqing Chen, Xu Wang, Yingtong Lv, Yin Huang, Zunjian Zhang, Fengguo Xu
Pharmacometabolomics has been already successfully used in toxicity prediction for one specific adverse effect. However in clinical practice, two or more different toxicities are always accompanied with each other, which puts forward new challenges for pharmacometabolomics. Gastrointestinal toxicity and myelosuppression are two major adverse effects induced by Irinotecan (CPT-11), and often show large individual differences. In the current study, a pharmacometabolomic study was performed to screen the exclusive biomarkers in predose serums which could predict late-onset diarrhea and myelosuppression of CPT-11 simultaneously...
January 2019: Acta Pharmaceutica Sinica. B
https://read.qxmd.com/read/30766786/novel-fluorescent-probes-of-10-hydroxyevodiamine-autophagy-and-apoptosis-inducing-anticancer-mechanisms
#6
Shuqiang Chen, Guoqiang Dong, Shanchao Wu, Na Liu, Wannian Zhang, Chunquan Sheng
Natural product evodiamine and its derivatives represent a promising class of multi-target antitumor agents. However, the clinical development of these compounds has been hampered by a poor understanding of their antitumor mechanisms. To tackle this obstacle, herein, novel fluorescent probes were designed to elucidate the antitumor mode of action of 10-hydroxyevodiamine. This compound was proven to be distributed in the mitochondria and lysosomes and to act by autophagy and apoptosis mechanisms.
January 2019: Acta Pharmaceutica Sinica. B
https://read.qxmd.com/read/30766785/cordycepin-promotes-browning-of-white-adipose-tissue-through-an-amp-activated-protein-kinase-ampk-dependent-pathway
#7
Guihong Qi, Yue Zhou, Xiaopo Zhang, Jiaqi Yu, Xin Li, Xiaoxue Cao, Chongming Wu, Peng Guo
Obesity is a worldwide epidemic. Promoting browning of white adipose tissue (WAT) contributes to increased energy expenditure and hence counteracts obesity. Here we show that cordycepin (Cpn), a natural derivative of adenosine, increases energy expenditure, inhibits weight gain, improves metabolic profile and glucose tolerance, decreases WAT mass and adipocyte size, and enhances cold tolerance in normal and high-fat diet-fed mice. Cpn markedly increases the surface temperature around the inguinal WAT and turns the inguinal fat browner...
January 2019: Acta Pharmaceutica Sinica. B
https://read.qxmd.com/read/30766784/preparation-and-characterization-of-multimodal-hybrid-organic-and-inorganic-nanocrystals-of-camptothecin-and-gold
#8
Christin P Hollis, Alan K Dozier, Barbara L Knutson, Tonglei Li
We demonstrate a novel inorganic-organic crystalline nanoconstruct, where gold atoms were imbedded in the crystal lattices as defects of camptothecin nanocrystals, suggesting its potential use as simultaneous agents for cancer therapy and bioimaging. The incorporation of gold, a potential computed tomography (CT) contrast agent, in the nanocrystals of camptothecin was detected by transmission electron microscope (TEM) and further quantified by energy dispersive X-ray spectrometry (EDS) and inductively coupled plasma-optical emission spectrometers (ICP-OES)...
January 2019: Acta Pharmaceutica Sinica. B
https://read.qxmd.com/read/30766783/development-of-carrier-free-nanocrystals-of-poorly-water-soluble-drugs-by-exploring-metastable-zone-of-nucleation
#9
Xiaoting Ren, Jianping Qi, Wei Wu, Zongning Yin, Tonglei Li, Yi Lu
There has been increasing interest in research and development of nanocrystals for the delivery of poorly water-soluble drugs that can be directly produced from solution. Compared with traditional carrier-based or encapsulation designs, drug nanocrystals circumvent possible side-effects due to carrier polymers and poor stability issues associated with encapsulation. The production of carrier-free nanocrystals requires careful control of nucleation and thus a thorough understanding of the relevant solution's metastable zone...
January 2019: Acta Pharmaceutica Sinica. B
https://read.qxmd.com/read/30766782/supersaturated-polymeric-micelles-for-oral-silybin-delivery-the-role-of-the-soluplus-pvpva-complex
#10
Chunliu Zhu, Shuang Gong, Jinsong Ding, Miaorong Yu, Ejaj Ahmad, Yi Feng, Yong Gan
Increasing the degree of supersaturation of drugs and maintaining their proper stability are very important in improving the oral bioavailability of poorly soluble drugs by a supersaturated drug delivery system (SDDS). In this study, we reported a complex system of Soluplus-Copovidone (Soluplus-PVPVA) loaded with the model drug silybin (SLB) that could not only maintain the stability of a supersaturated solution but also effectively promote oral absorption. The antiprecipitation effect of the polymers on SLB was observed using the solvent-shift method...
January 2019: Acta Pharmaceutica Sinica. B
https://read.qxmd.com/read/30766781/drug-nanoclusters-formed-in-confined-nano-cages-of-cd-mof-dramatic-enhancement-of-solubility-and-bioavailability-of-azilsartan
#11
Yuanzhi He, Wei Zhang, Tao Guo, Guoqing Zhang, Wei Qin, Liu Zhang, Caifen Wang, Weifeng Zhu, Ming Yang, Xiaoxiao Hu, Vikramjeet Singh, Li Wu, Ruxandra Gref, Jiwen Zhang
Tremendous efforts have been devoted to the enhancement of drug solubility using nanotechnologies, but few of them are capable to produce drug particles with sizes less than a few nanometers. This challenge has been addressed here by using biocompatible versatile γ -cyclodextrin ( γ -CD) metal-organic framework (CD-MOF) large molecular cages in which azilsartan (AZL) was successfully confined producing clusters in the nanometer range. This strategy allowed to improve the bioavailability of AZL in Sprague-Dawley rats by 9...
January 2019: Acta Pharmaceutica Sinica. B
https://read.qxmd.com/read/30766780/intestinal-uptake-of-barley-protein-based-nanoparticles-for-%C3%AE-carotene-delivery
#12
Guangyu Liu, Ying Zhou, Lingyun Chen
Our previous study introduced a barley protein microparticle for encapsulation of hydrophobic drug/nutraceutical, which could release nanoparticles upon gastric digestion and deliver encapsulated compound to a simulated intestinal environment intact. This work focused on evaluating the potential of liberated nanoparticles to improve the absorption of encapsulated compounds ( e.g ., β -carotene) using in vitro Caco-2 cell and ex vivo small intestine models. Nanoparticles obtained from gastric digestion of barley protein microparticles had a spherical shape and an average size of 351 nm...
January 2019: Acta Pharmaceutica Sinica. B
https://read.qxmd.com/read/30766779/selenium-layered-nanoparticles-serving-for-oral-delivery-of-phytomedicines-with-hypoglycemic-activity-to-synergistically-potentiate-the-antidiabetic-effect
#13
Wenji Deng, Huan Wang, Baojian Wu, Xingwang Zhang
Diabetes mellitus (DM) remains a great challenge in treatment due to pathological complexity. It has been proven that phytomedicines and natural medicines have prominent antidiabetic effects. This work aimed to develop selenium-layered nanoparticles (SeNPs) for oral delivery of mulberry leaf and Pueraria Lobata extracts (MPE), a group of phytomedicines with significant hypoglycemic activities, to achieve a synergic antidiabetic effect. MPE-loaded SeNPs (MPE-SeNPs) were prepared through a solvent diffusion/ in situ reduction technique and characterized by particle size, ζ potential, morphology, entrapment efficiency (EE) and drug loading (DL)...
January 2019: Acta Pharmaceutica Sinica. B
https://read.qxmd.com/read/30766778/the-effects-of-ph-surfactant-ion-concentration-coformer-and-molecular-arrangement-on-the-solubility-behavior-of-myricetin-cocrystals
#14
Shuzhen Ren, Mingyu Liu, Chao Hong, Guowen Li, Jiabin Sun, Jianying Wang, Lei Zhang, Yan Xie
Pharmaceutical cocrystals are a promising technology that can be used to improve the solubility of poor aqueous compounds. The objective of this study was to systematically investigate the solubility of myricetin (MYR) cocrystals, including their kinetic solubility, thermodynamic solubility, and intrinsic dissolution rate (IDR). The effects of pH, surfactant, ion concentration, and coformers on the cocrystal solubility were evaluated. Furthermore, single crystal structures of MYR, myricetin-isonicotinamide (MYR-INM) and myricetin-caffeine (MYR-CAF) cocrystals were analyzed to discuss the possible reasons for the enhancement of cocrystal solubility from the perspective of the spatial structure...
January 2019: Acta Pharmaceutica Sinica. B
https://read.qxmd.com/read/30766777/emerging-transporter-targeted-nanoparticulate-drug-delivery-systems
#15
REVIEW
Hongyan Su, Yan Wang, Shuo Liu, Yue Wang, Qian Liu, Guangxuan Liu, Qin Chen
Transporter-targeted nanoparticulate drug delivery systems (nano-DDS) have emerged as promising nanoplatforms for efficient drug delivery. Recently, great progress in transporter-targeted strategies has been made, especially with the rapid developments in nanotherapeutics. In this review, we outline the recent advances in transporter-targeted nano-DDS. First, the emerging transporter-targeted nano-DDS developed to facilitate oral drug delivery are reviewed. These include improvements in the oral absorption of protein and peptide drugs, facilitating the intravenous-to-oral switch in cancer chemotherapy...
January 2019: Acta Pharmaceutica Sinica. B
https://read.qxmd.com/read/30766776/adapting-liposomes-for-oral-drug-delivery
#16
REVIEW
Haisheng He, Yi Lu, Jianping Qi, Quangang Zhu, Zhongjian Chen, Wei Wu
Liposomes mimic natural cell membranes and have long been investigated as drug carriers due to excellent entrapment capacity, biocompatibility and safety. Despite the success of parenteral liposomes, oral delivery of liposomes is impeded by various barriers such as instability in the gastrointestinal tract, difficulties in crossing biomembranes, and mass production problems. By modulating the compositions of the lipid bilayers and adding polymers or ligands, both the stability and permeability of liposomes can be greatly improved for oral drug delivery...
January 2019: Acta Pharmaceutica Sinica. B
https://read.qxmd.com/read/30766775/advances-in-coamorphous-drug-delivery-systems
#17
Qin Shi, Sakib M Moinuddin, Ting Cai
In recent years, the coamorphous drug delivery system has been established as a promising formulation approach for delivering poorly water-soluble drugs. The coamorphous solid is a single-phase system containing an active pharmaceutical ingredient (API) and other low molecular weight molecules that might be pharmacologically relevant APIs or excipients. These formulations exhibit considerable advantages over neat crystalline or amorphous material, including improved physical stability, dissolution profiles, and potentially enhanced therapeutic efficacy...
January 2019: Acta Pharmaceutica Sinica. B
https://read.qxmd.com/read/30766774/application-of-flash-nanoprecipitation-to-fabricate-poorly-water-soluble-drug-nanoparticles
#18
REVIEW
Jinsong Tao, Shing Fung Chow, Ying Zheng
Nanoparticles are considered to be a powerful approach for the delivery of poorly water-soluble drugs. One of the main challenges is developing an appropriate method for preparation of drug nanoparticles. As a simple, rapid and scalable method, the flash nanoprecipitation (FNP) has been widely used to fabricate these drug nanoparticles, including pure drug nanocrystals, polymeric micelles, polymeric nanoparticles, solid lipid nanoparticles, and polyelectrolyte complexes. This review introduces the application of FNP to produce poorly water-soluble drug nanoparticles by controllable mixing devices, such as confined impinging jets mixer (CIJM), multi-inlet vortex mixer (MIVM) and many other microfluidic mixer systems...
January 2019: Acta Pharmaceutica Sinica. B
https://read.qxmd.com/read/30766773/editorial-persistent-endeavors-for-the-enhancement-of-dissolution-and-oral-bioavailability
#19
EDITORIAL
Wei Wu, Yi Lu, Jianping Qi
No abstract text is available yet for this article.
January 2019: Acta Pharmaceutica Sinica. B
https://read.qxmd.com/read/30505666/the-enzymatic-biosynthesis-of-acylated-steroidal-glycosides-and-their-cytotoxic-activity
#20
Ming Liu, Jian-Qiang Kong
Herein we describe the discovery and functional characterization of a steroidal glycosyltransferase (SGT) from Ornithogalum saundersiae and a steroidal glycoside acyltransferase (SGA) from Escherichia coli and their application in the biosynthesis of acylated steroidal glycosides (ASGs). Initially, an SGT gene, designated as OsSGT1, was isolated from O. saundersiae . OsSGT1-containing cell free extract was then used as the biocatalyst to react with 49 structurally diverse drug-like compounds. The recombinant OsSGT1 was shown to be active against both 3 β - and 17 β -hydroxyl steroids...
October 2018: Acta Pharmaceutica Sinica. B
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