212 results match your criteria Asian Journal Of Pharmaceutical Sciences[Journal]


The influence of genetic polymorphisms in drug metabolism enzymes and transporters on the pharmacokinetics of different fluvastatin formulations.

Asian J Pharm Sci 2020 Mar 26;15(2):264-272. Epub 2019 Jul 26.

Department of Pharmacy, Peking University First Hospital, Beijing 100034, China.

The purpose of the present study was to investigate the impact of genetic polymorphism on fluvastatin pharmacokinetics. In addition, we compared the fluvastatin pharmacokinetics differences between extended-release (ER) 80 mg tablet and immediate-release (IR) 40 mg capsule in terms of drug metabolism enzyme and transporter genetic polymorphisms. In this open-label, randomized, two-period, two-treatment, crossover study ( = 24), effects of and polymorphisms on the pharmacokinetics of fluvastatin were analyzed. Read More

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http://dx.doi.org/10.1016/j.ajps.2019.06.002DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7193447PMC

Organic anion transporters also mediate the drug-drug interaction between imipenem and cilastatin.

Asian J Pharm Sci 2020 Mar 28;15(2):252-263. Epub 2018 Dec 28.

Department of Clinical Pharmacology, College of Pharmacy, Dalian Medical University, Dalian 116044, China.

This study aimed to clarify that organic anion transporters (OATs) mediate the drug-drug interaction (DDI) between imipenem and cilastatin. After co-administration with imipenem, the plasma concentrations and the plasma concentration-time curve () of cilastatin were significantly increased, while renal clearance and cumulative urinary excretion of cilastatin were decreased. At the same time, imipenem significantly inhibited the uptake of cilastatin in rat kidney slices and in human OAT1 (hOAT1)-HEK293 and human OAT3 (hOAT3)-HEK293 cells. Read More

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http://dx.doi.org/10.1016/j.ajps.2018.11.006DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7193450PMC

Chronic exposure to excess iron promotes EMT and cancer via p53 loss in pancreatic cancer.

Asian J Pharm Sci 2020 Mar 5;15(2):237-251. Epub 2020 Mar 5.

Department of Cell Biology and Biochemistry, Texas Tech University Health Sciences Center, Lubbock, TX 79430, USA.

Based on the evidence that hemochromatosis, an iron-overload disease, drives hepatocellular carcinoma, we hypothesized that chronic exposure to excess iron, either due to genetic or environmental causes, predisposes an individual to cancer. Using pancreatic cancer as our primary focus, we employed cell culture studies to interrogate the connection between excess iron and cancer, and combined and studies to explore the connection further. Ferric ammonium citrate was used as an exogenous iron source. Read More

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http://dx.doi.org/10.1016/j.ajps.2020.02.003DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7193456PMC

Research and development of drug delivery systems based on drug transporter and nano-formulation.

Asian J Pharm Sci 2020 Mar 4;15(2):220-236. Epub 2020 Mar 4.

College of Pharmaceutical Sciences, Zhejiang University, Hangzhou 310058, China.

In recent years, the continuous occurrence of multi-drug resistance in the clinic has made people pay more attention to the transporter. Changes in the expression and activity of transporters can cause corresponding changes in drug pharmacokinetics and pharmacodynamics. The drug-drug interactions (DDI) caused by transporters can seriously affect drug effectiveness and toxicity. Read More

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http://dx.doi.org/10.1016/j.ajps.2020.02.004DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7193453PMC

Glutamine transporters as pharmacological targets: From function to drug design.

Asian J Pharm Sci 2020 Mar 5;15(2):207-219. Epub 2020 Mar 5.

Department of DiBEST (Biologia, Ecologia e Scienze della Terra), University of Calabria, Arcavacata di Rende (CS) 87036, Italy.

Among the different targets of administered drugs, there are membrane transporters that play also a role in drug delivery and disposition. Moreover, drug-transporter interactions are responsible for off-target effects of drugs underlying their toxicity. The improvement of the drug design process is subjected to the identification of those membrane transporters mostly relevant for drug absorption, delivery and side effect production. Read More

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http://dx.doi.org/10.1016/j.ajps.2020.02.005DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7193454PMC

Amino acid transporters: Emerging roles in drug delivery for tumor-targeting therapy.

Asian J Pharm Sci 2020 Mar 5;15(2):192-206. Epub 2020 Mar 5.

Department of Pharmacy, The First Affiliated Hospital of China Medical University, Shenyang 110001, China.

Amino acid transporters, which play a vital role in transporting amino acids for the biosynthesis of mammalian cells, are highly expressed in types of tumors. Increasing studies have shown the feasibility of amino acid transporters as a component of tumor-targeting therapy. In this review, we focus on tumor-related amino acid transporters and their potential use in tumor-targeting therapy. Read More

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http://dx.doi.org/10.1016/j.ajps.2019.12.002DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7193455PMC

Stimulatory effect on the transport mediated by organic anion transporting polypeptide 2B1.

Asian J Pharm Sci 2020 Mar 13;15(2):181-191. Epub 2019 Nov 13.

Tohoku University Hospital, Department of Pharmaceutical Sciences, Miyagi 980-8574, Japan.

Drug-drug interaction (DDI) is one of causes of adverse drug events and can result in life-threatening consequences. Organic anion-transporting polypeptide (OATP) 2B1 is a major uptake transporter in the intestine and contributes to transport various clinically used therapeutic agents. The intestine has a high risk of DDI, because it has a special propensity to be exposed to a high concentration of drugs. Read More

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http://dx.doi.org/10.1016/j.ajps.2019.10.004DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7193449PMC

Pharmacologic inducers of the uric acid exporter ABCG2 as potential drugs for treatment of gouty arthritis.

Asian J Pharm Sci 2020 Mar 7;15(2):173-180. Epub 2019 Nov 7.

Department of Cell Biology and Biochemistry, Texas Tech University Health Sciences Center, Lubbock, TX 79430, United States.

Uric acid is the end product of purine catabolism and its plasma levels are maintained below its maximum solubility in water (6-7 mg/dl). The plasma levels are tightly regulated as the balance between the rate of production and the rate of excretion, the latter occurring in urine (kidney), bile (liver) and feces (intestinal tract). Reabsorption in kidney is also an important component of this process. Read More

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http://dx.doi.org/10.1016/j.ajps.2019.10.002DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7193448PMC

The role of transporters in cancer redox homeostasis and cross-talk with nanomedicines.

Asian J Pharm Sci 2020 Mar 3;15(2):145-157. Epub 2020 Mar 3.

Department of Pharmacy, The Second Affiliated Hospital and Yuying Children's Hospital of Wenzhou Medical University, Wenzhou 325027, China.

Tumor cell usually exhibits high levels of reactive oxygen species and adaptive antioxidant system due to the metabolic, genetic, and microenvironment-associated alterations. The altered redox homeostasis can promote tumor progression, development, and treatment resistance. Several membrane transporters are involved in the resetting redox homeostasis and play important roles in tumor progression. Read More

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http://dx.doi.org/10.1016/j.ajps.2020.02.001DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7193452PMC

The solute carrier transporters and the brain: Physiological and pharmacological implications.

Asian J Pharm Sci 2020 Mar 13;15(2):131-144. Epub 2019 Nov 13.

School of Pharmaceutical Sciences, Key Laboratory of Bioorganic Phosphorus Chemistry and Chemical Biology (Ministry of Education), Tsinghua University, Beijing 100084, China.

Solute carriers (SLCs) are the largest family of transmembrane transporters that determine the exchange of various substances, including nutrients, ions, metabolites, and drugs across biological membranes. To date, the presence of about 287 SLC genes have been identified in the brain, among which mutations or the resultant dysfunctions of 71 SLC genes have been reported to be correlated with human brain disorders. Although increasing interest in SLCs have focused on drug development, SLCs are currently still under-explored as drug targets, especially in the brain. Read More

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http://dx.doi.org/10.1016/j.ajps.2019.09.002DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7193445PMC

Intestinal OCTN2- and MCT1-targeted drug delivery to improve oral bioavailability.

Asian J Pharm Sci 2020 Mar 4;15(2):158-173. Epub 2020 Mar 4.

School of Pharmacy, Guang Xi University of Chinese Medicine, Nanning 530200, China.

Various drug transporters are widely expressed throughout the intestine and play important roles in absorbing nutrients and drugs, thus providing high quality targets for the design of prodrugs or nanoparticles to facilitate oral drug delivery. In particular, intestinal carnitine/organic cation transporter 2 (OCTN2) and mono-carboxylate transporter protein 1 (MCT1) possess high transport capacities and complementary distributions. Therefore, we outline recent developments in transporter-targeted oral drug delivery with regard to the OCTN2 and MCT1 proteins in this review. Read More

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http://dx.doi.org/10.1016/j.ajps.2020.02.002DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7118283PMC

Apoptosis of A549 cells by small interfering RNA targeting survivin delivery using poly-β-amino ester/guanidinylated O-carboxymethyl chitosan nanoparticles.

Asian J Pharm Sci 2020 Jan 27;15(1):121-128. Epub 2018 Nov 27.

Department of Pharmacy, China Pharmaceutical University, Nanjing 211198, China.

Gene-based therapeutics has emerged as a promising approach for human cancer therapy. Among a variety of non-viral vectors, polymer vectors are particularly attractive due to their safety and multivalent groups on their surface. This study focuses on guanidinylated O-carboxymethyl chitosan (GOCMCS) along with poly-β-amino ester(PBAE) for siRNA delivery. Read More

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http://dx.doi.org/10.1016/j.ajps.2018.09.009DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7066049PMC
January 2020

Simvastatin nanoliposome induces myocardial and hepatic toxicities due to its absorption enhancement in mice.

Asian J Pharm Sci 2020 Jan 25;15(1):112-120. Epub 2019 May 25.

School of Basic Medical Science, Shihezi University, Shihezi 832008, China.

Nanoliposome is a useful dosage form to increase solubility and absorption of simvastatin (SMV), and consequently improves its therapeutic effects. However, toxicity of SMV could also be elevated accompanied by the absorption enhancement, which is a decisive factor for the clinical application of SMV nanoliposome (SMV-Lipo), but has not been studied systematically and reported so far. In this study, organ toxicity of SMV-Lipo was evaluated in mice in the presence and absence of isoproterenol and compared to those of free SMV. Read More

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http://dx.doi.org/10.1016/j.ajps.2019.02.002DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7066038PMC
January 2020

Monitoring film coalescence from aqueous polymeric dispersions using atomic force microscopy: Surface topographic and nano-adhesion studies.

Asian J Pharm Sci 2020 Jan 3;15(1):104-111. Epub 2018 Nov 3.

UCL School of Pharmacy, 29-39 Brunswick Square, London WC1N1AX, UK.

The aim of the investigation was to develop the use of topographic and nano-adhesion atomic force microscopy (AFM) studies as a means of monitoring the coalescence of latex particles within films produced from a pharmaceutically relevant aqueous dispersion (EudragitNE30D). Films were prepared via spin coating and analysed using AFM, initially via tapping mode for topographic assessment followed by force-distance measurements which allowed assessment of site-specific adhesion. The results showed that colloidal particles were clearly observed topographically in freshly prepared samples, with coalescence detected on curing via the disappearance of discernible surface features and a decrease in roughness indices. Read More

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http://dx.doi.org/10.1016/j.ajps.2018.09.008DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7066041PMC
January 2020

Comparison of different cationic polymers efficacy in fabrication of alginate multilayer microcapsules.

Asian J Pharm Sci 2020 Jan 30;15(1):95-103. Epub 2018 Dec 30.

Department of Pharmaceutics, School of Pharmacy, Shahid Beheshti University of Medical Sciences, Tehran 1991953381, Iran.

In past decades, alginate-based multilayer microcapsules have been given important attention in various pharmaceutical investigations. Alginate-poly l lysine-alginate (APA) is studied the most. Due to the similarity between the structure of polyethyleneimine (PEI) and poly-L-lysine (PLL) and also lower price of PEI than PLL, this study was conducted to compare the efficacy of linear (LPEI) and branch (BPEI) forms of PEI with PLL as covering layers in fabrication of microcapsules. Read More

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http://dx.doi.org/10.1016/j.ajps.2018.11.007DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7066046PMC
January 2020

Redox-responsive biocompatible nanocarriers based on novel heparosan polysaccharides for intracellular anticancer drug delivery.

Asian J Pharm Sci 2020 Jan 17;15(1):83-94. Epub 2018 Dec 17.

School of Pharmaceutical Sciences, Jiangnan University, Wuxi 214122, China.

Heparosan is a natural precursor of heparin biosynthesis in mammals. It is stable in blood circulation but can be degraded in lysosomes, showing good biocompatibility and long circulation features. So heparosan can be designed as anticancer drug carriers to increase tumor selectivity and improve the therapeutic effect. Read More

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http://dx.doi.org/10.1016/j.ajps.2018.11.005DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7066043PMC
January 2020

Redox-sensitive, PEG-shielded carboxymethyl PEI nanogels silencing MicroRNA-21, sensitizes resistant ovarian cancer cells to cisplatin.

Asian J Pharm Sci 2020 Jan 1;15(1):69-82. Epub 2018 Dec 1.

Center for Nanotechnology in Drug Delivery, Shiraz University of Medical Sciences, Shiraz 71345, Iran.

A series of branched polyethylenimine (PEI) modifications including PEGylation (PEG2k-PEI) for steric shielding, redox-sensitive crosslinking for synthesis PEG2k-PEI-ss nanogels and subsequent carboxymethylation (PEG2k-CMPEI-ss) for modulation of the polymer pk have been introduced for cellular delivery of Anti-miR-21. The synthesis was characterized using H NMR, FTIR, TNBS, potentiometric titration, particle size and ζ potential. Loading of Anti-miR-21 at various N/P ratios was investigated by gel retardation, ethidium bromide dye exclusion, heparin sulfate competition and DNase I digestion experiments. Read More

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http://dx.doi.org/10.1016/j.ajps.2018.10.006DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7066047PMC
January 2020

Multi-dimensional visualization for the morphology of lubricant stearic acid particles and their distribution in tablets.

Asian J Pharm Sci 2020 Jan 1;15(1):60-68. Epub 2019 Mar 1.

School of Pharmacy, Shenyang Pharmaceutical University, Shenyang 110016, China.

The shapes of particles and their distribution in tablets, controlled by pretreatment and tableting process, determine the pharmaceutical performance of excipient like lubricant. This study aims to provide deeper insights to the relationship of the morphology and spatial distribution of stearic acid (SA) with the lubrication efficiency, as well as the resulting tablet property. Unmodified SA particles as flat sheet-like particles were firstly reprocessed by emulsification in hot water to obtain the reprocessed SA particles with spherical morphology. Read More

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http://dx.doi.org/10.1016/j.ajps.2019.01.001DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7066036PMC
January 2020

A review on anti-bacterials to combat resistance: From ancient era of plants and metals to present and future perspectives of green nano technological combinations.

Asian J Pharm Sci 2020 Jan 12;15(1):42-59. Epub 2019 Jun 12.

A.U. College of Pharmaceutical Sciences, Visakhapatnam 530003, India.

In the primitive era, humans benefited partially from plants and metals to treat microbial infections. Later these infections were cured with antibiotics but further suffered from resistance issues. In searching of an alternative, researchers developed an adjuvant therapy but were hampered by spreading resistance. Read More

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http://dx.doi.org/10.1016/j.ajps.2019.03.002DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7066045PMC
January 2020

Advances in nanotechnology-based delivery systems for EGFR tyrosine kinases inhibitors in cancer therapy.

Asian J Pharm Sci 2020 Jan 5;15(1):26-41. Epub 2019 Jul 5.

Department of Medical Oncology, State Key Laboratory of Biotherapy and Cancer Center, West China Hospital, West China Medical School, Sichuan University, and Collaborative Innovation Center for Biotherapy, Chengdu 610041, China.

Oral tyrosine kinase inhibitors (TKIs) against epidermal growth factor receptor (EGFR) family have been introduced into the clinic to treat human malignancies for decades. Despite superior properties of EGFR-TKIs as small molecule targeted drugs, their applications are still restricted due to their low solubility, capricious oral bioavailability, large requirement of daily dose, high binding tendency to plasma albumin and initial/acquired drug resistance. Nanotechnology is a promising tool to improve efficacy of these drugs. Read More

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http://dx.doi.org/10.1016/j.ajps.2019.06.001DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7066044PMC
January 2020

Transdermal drug delivery systems in diabetes management: A review.

Asian J Pharm Sci 2020 Jan 22;15(1):13-25. Epub 2019 Jun 22.

School of Pharmacy, Monash University Malaysia, Bandar Sunway 47500, Malaysia.

Diabetes mellitus is a chronic disease in which there is an insufficient production of insulin by the pancreas, or the insulin produced is unable to be utilized effectively by the body. Diabetes affects more than 415 million people globally and is estimated to strike about 642 million people in 2040. The WHO reported that diabetes will become the seventh biggest cause of mortality in 2030. Read More

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http://dx.doi.org/10.1016/j.ajps.2019.04.006DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7066029PMC
January 2020

Current multifunctional albumin-based nanoplatforms for cancer multi-mode therapy.

Asian J Pharm Sci 2020 Jan 1;15(1):1-12. Epub 2019 Mar 1.

Wuya College of Innovation, Shenyang Pharmaceutical University, Shenyang 110016, China.

Albumin has been widely applied for rational design of drug delivery complexes as natural carriers in cancer therapy due to its distinct advantages of biocompatibility, abundance, low toxicity and versatile property. Hence, various types of multifunctional albumin-based nanoplatforms (MAlb-NPs) that adopt multiple imaging and therapeutic techniques have been developed for cancer diagnosis and treatment. Stimuli-responsive release, including reduction-sensitive, pH-responsive, concentration-dependent and photodynamic-triggered, is important to achieve low-toxicity cancer therapy. Read More

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http://dx.doi.org/10.1016/j.ajps.2018.12.006DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7066042PMC
January 2020

Development of a method to quantify total and free irinotecan and 7-ethyl-10-hydroxycamptothecin (SN-38) for pharmacokinetic and bio-distribution studies after administration of irinotecan liposomal formulation.

Asian J Pharm Sci 2019 Nov 11;14(6):687-697. Epub 2018 Sep 11.

Wuya College of Innovation, Shenyang Pharmaceutical University, Shenyang 110016, China.

In 2015, liposomal formulation of irinotecan (ONIVYDE) has been approved by FDA and widely applied in the treatment of pancreatic cancer. ONIVYDE is a novel liposome formulation, entrapping CPT-11 in the aqueous core of vesicles using a modified gradient loading method. Due to toxicity concerns, it is essential to explore a rapid and reliable method to effectively isolate and quantify the non-liposomal, namely, free CPT-11and total CPT-11 in plasma. Read More

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http://dx.doi.org/10.1016/j.ajps.2018.08.003DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7032223PMC
November 2019

Piperacillin enhances the inhibitory effect of tazobactam on β-lactamase through inhibition of organic anion transporter 1/3 in rats.

Asian J Pharm Sci 2019 Nov 7;14(6):677-686. Epub 2018 Dec 7.

Department of Clinical Pharmacology, College of Pharmacy, Dalian Medical University, Dalian 116044, China.

To assess the mechanism of the pharmacokinetic interaction between piperacillin and tazobactam, renal excretion and pharmacokinetic studies of piperacillin/tazobactam were investigated in normal and bacteremia rats. A bacteremia model was established to investigate the pharmacokinetic properties of piperacillin and tazobactam under different conditions. Renal slices were taken to examine the uptake of piperacillin and tazobactam. Read More

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http://dx.doi.org/10.1016/j.ajps.2018.11.003DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7032209PMC
November 2019

Cooperative effect of polyvinylpyrrolidone and HPMC E5 on dissolution and bioavailability of nimodipine solid dispersions and tablets.

Asian J Pharm Sci 2019 Nov 18;14(6):668-676. Epub 2018 Sep 18.

Wuya College of Innovation, Shenyang Pharmaceutical University, Shenyang 110016, China.

Solid dispersion (SD) systems have been extensively used to increase the dissolution and bioavailability of poorly water-soluble drugs. To circumvent the limitations of polyvinylpyrrolidone (PVP) dispersions, HPMC E5 was applied in the formulation process and scaling-up techniques, simultaneously. In this study, SD of nimodipine (NMP) and corresponding tablets were prepared through solvent method and fluid bed granulating one step technique, respectively. Read More

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http://dx.doi.org/10.1016/j.ajps.2018.08.005DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7032151PMC
November 2019

A cabazitaxel liposome for increased solubility, enhanced antitumor effect and reduced systemic toxicity.

Asian J Pharm Sci 2019 Nov 20;14(6):658-667. Epub 2018 Nov 20.

College of Pharmaceutical Sciences, Zhejiang University, Hangzhou 310058, China.

The potential side effects of cabazitaxel (CBZ) in the field of cancer treatment have become a great limitation to its further clinical application. Liposomal delivery is a well-established approach to increase the therapeutic index of hydrophobic drugs. In this study, a PEG-modified liposome was developed for efficiently encapsulating CBZ, thus enhancing its specific tumor inhibition effect and reducing the systemic toxicity. Read More

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http://dx.doi.org/10.1016/j.ajps.2018.10.004DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7032206PMC
November 2019

Improved dissolution and oral absorption by co-grinding active drug probucol and ternary stabilizers mixtures with planetary beads-milling method.

Asian J Pharm Sci 2019 Nov 12;14(6):649-657. Epub 2018 Dec 12.

School of Pharmacy, Shenyang Pharmaceutical University, Benxi 117004, China.

The objective of this work is to construct a nanosuspension drug delivery system of probucol, a BCS II drug, in order to improve its dissolution and oral bioavailability. The wet milling procedure using planetary beads-milling equipment was utilized to grind the raw probucol to ultrafine nanoparticle/nanocrystal aqueous suspension that was further solidified by freeze-drying process. Cellulose derivatives of different substitution groups and molecular weights, including HPMC, HPC, and MC, were evaluated as the primary stabilizer of probucol nanosuspension. Read More

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http://dx.doi.org/10.1016/j.ajps.2018.12.001DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7032176PMC
November 2019

Synthesis, characterization and evaluation of honokiol bisphosphate prodrugs protects against rats' brain ischemia-reperfusion injury.

Asian J Pharm Sci 2019 Nov 15;14(6):640-648. Epub 2018 Dec 15.

Chengdu Medical College, Chengdu 610500, China.

Honokiol (HK) usage is greatly restricted by its poor aqueous solubility and limited oral bioavailability. We synthesized and characterized a novel phosphate prodrug of honokiol (HKP) for and use. HKP greatly enhanced the aqueous solubility of HK (127. Read More

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http://dx.doi.org/10.1016/j.ajps.2018.11.004DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7032162PMC
November 2019

A novel oral prodrug-targeting transporter MCT 1: 5-fluorouracil-dicarboxylate monoester conjugates.

Asian J Pharm Sci 2019 Nov 25;14(6):631-639. Epub 2019 Apr 25.

Wuya College of Innovation, Shenyang Pharmaceutical University, Shenyang 110016, China.

Monocarboxylate transporter 1 (MCT1) is responsible for oral absorption of short-chain monocarboxylic acids from small intestine, hence, it's likely to serve as an ideal design target for the development of oral prodrugs. However, potential application of MCT1 to facilitate the oral delivery is still unclear. Irregular oral absorption, poor permeability and bioavailability greatly limit the oral delivery efficiency of 5-fluorouracil (5-FU). Read More

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http://dx.doi.org/10.1016/j.ajps.2019.04.001DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7032090PMC
November 2019

Evaluation of the Mrp2-mediated flavonoid-drug interaction potential of quercetin in rats and models.

Asian J Pharm Sci 2019 Nov 16;14(6):621-630. Epub 2019 Jan 16.

Division of Biopharmaceutics, College of Pharmacy, Kyung Hee University, Seoul 02447, Republic of Korea.

Quercetin is a biologically active flavonoid that has been used as a popular health supplement. It is reported that quercetin may cause flavonoid-drug interaction mediated by P-glycoprotein, the most predominant efflux transporter. In this study, we comprehensively evaluated the potential of the pharmacokinetic interaction of quercetin mediated by multidrug resistance-associated protein 2 (MRP2), another major efflux transporter. Read More

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http://dx.doi.org/10.1016/j.ajps.2018.12.003DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7032158PMC
November 2019

Investigation of molecular aggregation mechanism of glipizide/cyclodextrin complexation by combined experimental and molecular modeling approaches.

Asian J Pharm Sci 2019 Nov 8;14(6):609-620. Epub 2018 Dec 8.

State Key Laboratory of Quality Research in Chinese Medicine, Institute of Chinese Medical Sciences (ICMS), University of Macau, Macau, China.

Cyclodextrin complexation is a wise strategy to enhance aqueous solubility of water-insoluble drugs. However, the aggregation mechanism of drug-cyclodextrin complexes is still unclear. This research aimed to investigate the molecular aggregation mechanism of glipizide/cyclodextrin complexation by the combination of experimental and modeling methods. Read More

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http://dx.doi.org/10.1016/j.ajps.2018.10.008DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7032256PMC
November 2019

The functions and applications of A7R in anti-angiogenic therapy, imaging and drug delivery systems.

Asian J Pharm Sci 2019 Nov 25;14(6):595-608. Epub 2019 May 25.

Key Laboratory of Chemical Biology (Ministry of Education), Institute of Biochemical and Biotechnological Drug, School of Pharmaceutical Sciences, Shandong University, Jinan 250012, China.

Vascular endothelial growth factor receptor 2 (VEGFR-2) and neuropilin-1 (NRP-1) are two prominent antiangiogenic targets. They are highly expressed on vascular endothelial cells and some tumor cells. Therefore, targeting VEGFR-2 and NRP-1 may be a potential antiangiogenic and antitumor strategy. Read More

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http://dx.doi.org/10.1016/j.ajps.2019.04.004DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7032227PMC
November 2019

Cancer nanotechnology: Enhancing tumor cell response to chemotherapy for hepatocellular carcinoma therapy.

Asian J Pharm Sci 2019 Nov 12;14(6):581-594. Epub 2019 Jun 12.

School of Pharmaceutical Sciences, Southern Medical University, Guangzhou 510515, China.

Hepatocellular carcinoma (HCC) is one of the deadliest cancers due to its complexities, reoccurrence after surgical resection, metastasis and heterogeneity. In addition to sorafenib and lenvatinib for the treatment of HCC approved by FDA, various strategies including transarterial chemoembolization, radiotherapy, locoregional therapy and chemotherapy have been investigated in clinics. Recently, cancer nanotechnology has got great attention for the treatment of various cancers including HCC. Read More

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http://dx.doi.org/10.1016/j.ajps.2019.04.005DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7032247PMC
November 2019

Triphenylphosphonium-modified mitochondria-targeted paclitaxel nanocrystals for overcoming multidrug resistance.

Asian J Pharm Sci 2019 Sep 18;14(5):569-580. Epub 2018 Sep 18.

Shenyang Pharmaceutical University, Shenyang 110016, China.

Mitochondria are currently known as novel targets for treating cancer, especially for tumors displaying multidrug resistance (MDR). This present study aimed to develop a mitochondria-targeted delivery system by using triphenylphosphonium cation (TPP)-conjugated Brij 98 as the functional stabilizer to modify paclitaxel (PTX) nanocrystals (NCs) against drug-resistant cancer cells. Evaluations were performed on 2D monolayer and 3D multicellular spheroids (MCs) of MCF-7 cells and MCF-7/ADR cells. Read More

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http://dx.doi.org/10.1016/j.ajps.2018.06.006DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7032231PMC
September 2019

Preparation and evaluation of intestinal retention pellets of Berberine chloride to enhance hypoglycemic and lipid-lowing efficacy.

Asian J Pharm Sci 2019 Sep 25;14(5):559-568. Epub 2018 Oct 25.

Shengjing Hospital of China Medical University, Shenyang 110004, China.

Berberine chloride (BBR) is a pharmacokinetic profile of drug with poor bioavailability but good therapeutic efficacy, which is closely related to the discovery of BBR intestinal target. The major aim of this paper is to develop BBR intestinal retention type sustained-release pellets and evaluate their and behaviors base on the aspect of local action on intestinal tract. Here, wet milling technology is used to improve dissolution and dissolution rate of BBR by decreasing the particle size and increasing the wettability. Read More

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http://dx.doi.org/10.1016/j.ajps.2018.09.006DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7032169PMC
September 2019

Integration of phospholipid-drug complex into self-nanoemulsifying drug delivery system to facilitate oral delivery of paclitaxel.

Asian J Pharm Sci 2019 Sep 20;14(5):552-558. Epub 2018 Nov 20.

Wuya College of Innovation, Shenyang Pharmaceutical University, Shenyang 110016, China.

Self-nanoemulsifying drug delivery system (SNEDDS) has emerged as a promising platform to improve oral absorption of drugs with poor solubility and low permeability. However, large polarity molecules with insufficient lipid solubility, such as paclitaxel (PTX), would suffer from inferior formulation of SNEDDS due to poor compatibility. Herein, phospholipid-drug complex (PLDC) and SNEDDS were integrated into one system to facilitate oral delivery of PTX. Read More

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http://dx.doi.org/10.1016/j.ajps.2018.10.003DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7032203PMC
September 2019

Modulating intestinal mucus barrier for nanoparticles penetration by surfactants.

Asian J Pharm Sci 2019 Sep 12;14(5):543-551. Epub 2018 Oct 12.

School of Pharmacy, Shenyang Pharmaceutical University, Shenyang 110016, China.

Improving peroral delivery efficiency is always a persistent goal for both small-molecule and macromolecular drug development. However, intestinal mucus barrier which greatly impedes drug-loaded nanoparticles penetration is commonly overlooked. Therefore, in this study, taking fluorescent labeled PLGA (poly (lactic-co-glycolic acid)) nanoparticles as a tool, the influence of anionic and nonionic surfactants on mucus penetration ability of nanoparticles and their mucus barrier regulating ability were studied. Read More

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http://dx.doi.org/10.1016/j.ajps.2018.09.002DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7032225PMC
September 2019

Redox-sensitive micelles for targeted intracellular delivery and combination chemotherapy of paclitaxel and all-trans-retinoid acid.

Asian J Pharm Sci 2019 Sep 24;14(5):531-542. Epub 2018 Sep 24.

Department of Natural Medicinal Chemistry, China Pharmaceutical University, Nanjing 210009, China.

The application of paclitaxel (PTX) in clinic has been restricted due to its poor solubility. Several traditional nano-medicines have been developed to improve this defect, while they are still lack of tumor targeting ability and rapid drug release. In this work, an amphiphilic polymeric micelle of hyaluronic acid (HA) - all-trans-retinoid acid (ATRA) with a disulfide bond, was developed successfully for the co-delivery of PTX and ATRA. Read More

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http://dx.doi.org/10.1016/j.ajps.2018.08.009DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7032146PMC
September 2019

Exploring the relationship of hyaluronic acid molecular weight and active targeting efficiency for designing hyaluronic acid-modified nanoparticles.

Asian J Pharm Sci 2019 Sep 6;14(5):521-530. Epub 2018 Dec 6.

Wuya College of Innovation, Shenyang Pharmaceutical University, Shenyang 110016, China.

Although it is reported that the targeting ability of hyaluronic acid (HA)-based nanoparticles (NPs) is molecular weight (MW) dependent, the influence of HA MW on targeting efficiency of HA-functionalized NPs and the underlying mechanism remain elusive. In this study, we constituted three HA-functionalized Dox-loaded NPs (Dox/HCVs) different HA MWs (7, 63, and 102 kDa) and attempted to illustrate the effects of HA MW on the targeting efficiency. The three Dox/HCVs had similar physiochemical and pharmaceutical characteristics, but showed different affinity to CD44 receptor. Read More

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http://dx.doi.org/10.1016/j.ajps.2018.11.002DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7032078PMC
September 2019

Improving the protective effects of aFGF for peripheral nerve injury repair using sulfated chitooligosaccharides.

Asian J Pharm Sci 2019 Sep 1;14(5):511-520. Epub 2018 Nov 1.

Department of Stomatology, Jinan University Medical College, Guangzhou 510632, China.

Injury to the peripheral nerves can result in temporary or life-long neuronal dysfunction and subsequent economic or social disability. Acidic fibroblast growth factor (aFGF) promotes the growth and survival of neurons and is a possible treatment for peripheral nerve injury. Yet, the actual therapeutic utility of aFGF is limited by its short half-life and instability . Read More

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http://dx.doi.org/10.1016/j.ajps.2018.09.007DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7032102PMC
September 2019

Design, mechanism, delivery and therapeutics of canonical and Dicer-substrate siRNA.

Asian J Pharm Sci 2019 Sep 13;14(5):497-510. Epub 2019 Feb 13.

Department of Pharmaceutics, Faculty of Pharmacy, Northern Border University, Rafha 73211, Saudi Arabia.

Upon the discovery of RNA interference (RNAi), canonical small interfering RNA (siRNA) has been recognized to trigger sequence-specific gene silencing. Despite the benefits of siRNAs as potential new drugs, there are obstacles still to be overcome, including off-target effects and immune stimulation. More recently, Dicer substrate siRNA (DsiRNA) has been introduced as an alternative to siRNA. Read More

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http://dx.doi.org/10.1016/j.ajps.2018.12.005DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7032099PMC
September 2019

Nanocarriers as a powerful vehicle to overcome blood-brain barrier in treating neurodegenerative diseases: Focus on recent advances.

Asian J Pharm Sci 2019 Sep 22;14(5):480-496. Epub 2018 Oct 22.

Institute of Pharmaceutics, College of Pharmaceutical Sciences, Zhejiang University, Hangzhou 310058, China.

Neurodegenerative diseases including Alzheimer's disease, Parkinson's disease, Huntington disease and amyotrophic lateral sclerosis throw a heavy burden on families and society. Related scientific researches make tardy progress. One reason is that the known pathogeny is just the tip of the iceberg. Read More

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http://dx.doi.org/10.1016/j.ajps.2018.09.005DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7032222PMC
September 2019

Complex formulations, simple techniques: Can 3D printing technology be the Midas touch in pharmaceutical industry?

Asian J Pharm Sci 2019 Sep 14;14(5):465-479. Epub 2019 Feb 14.

College of Pharmacy, Keimyung University, Daegu 42601, Republic of Korea.

3D printing is a method of rapid prototyping and manufacturing in which materials are deposited onto one another in layers to produce a three-dimensional object. Although 3D printing was developed in the 1980s and the technology has found widespread industrial applications for production from automotive parts to machine tools, its application in pharmaceutical area is still limited. However, the potential of 3D printing in the pharmaceutical industry is now being recognized. Read More

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http://dx.doi.org/10.1016/j.ajps.2018.11.008DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7032174PMC
September 2019

Effect of Kupffer cells depletion on ABC phenomenon induced by Kupffer cells-targeted liposomes.

Asian J Pharm Sci 2019 Jul 4;14(4):455-464. Epub 2018 Sep 4.

Shenyang Pharmaceutical University, Shenyang 110016, China.

Accelerated blood clearance (ABC) phenomenon is common in many PEGylated nanocarriers, whose mechanism has not been completely elucidated yet. In this study, the correlation between Kupffer cells (KCs) and ABC phenomenon has been studied by KCs-targeted liposomes inducing ABC phenomenon and KCs depletion. In other words, the 4-aminophenyl-α-D-mannopyranoside (APM) lipid derivative DSPE-PEG-APM (DPM), and 4-aminophenyl-β-L-fucopyranoside (APF) lipid derivative DSPE-PEG-APF (DPF) were conjugated and modified on alendronate sodium (AD) liposomes to specifically target and deplete KCs. Read More

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http://dx.doi.org/10.1016/j.ajps.2018.07.004DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7032111PMC

Extended tacrolimus release via the combination of lipid-based solid dispersion and HPMC hydrogel matrix tablets.

Asian J Pharm Sci 2019 Jul 8;14(4):445-454. Epub 2018 Sep 8.

School of Pharmaceutical Engineering, Shenyang Pharmaceutical University, Benxi 117004, China.

The objective of this study is to evaluate the feasibility of obtaining extended release of tacrolimus by a novel combination of lipid-based solid dispersion and matrix-type extended release tablet techniques. Tacrolimus solid dispersion was prepared using glycerylbehenate (Compritol ATO888) and Pluronic F127 as the carrier materials with hot-melt method, which was then blended with hydrogel matrix materials, such as HPMC and lactose, the powders were directly compressed into tablets. drug release tests were carried out to evaluate the performance of the solid dispersions and the tablets. Read More

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http://dx.doi.org/10.1016/j.ajps.2018.08.001DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7032121PMC

A thorough analysis of the effect of surfactant/s on the solubility and pharmacokinetics of (S)-zaltoprofen.

Asian J Pharm Sci 2019 Jul 2;14(4):435-444. Epub 2018 Nov 2.

College of Pharmacy and Institute of Drug Research and Development, Chungnam National University, Daejeon 34134, Republic of Korea.

Until now, there are no publications about the preformulation studies on (S)-zaltoprofen ((S)-ZPF). Hence, we first investigated the solubility of (S)-ZPF, screened solubilizers and performed the pharmacokinetic study of (S)-ZPF in the presence of the solubilizers. The measurement of the solubility of (S)-ZPF in 26 different solvents was carried out, including d-alpha tocopheryl polyethylene glycol 1000 succinate (TPGS), 2-hydroxypropyl-β-cyclodextrin (HPCD), and mixtures of individual solvent. Read More

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http://dx.doi.org/10.1016/j.ajps.2018.10.002DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7032178PMC

A hybrid genipin-crosslinked dual-sensitive hydrogel/nanostructured lipid carrier ocular drug delivery platform.

Asian J Pharm Sci 2019 Jul 10;14(4):423-434. Epub 2018 Sep 10.

Shenyang Pharmaceutical University, Shenyang 110016, China.

The objective of this study was to develop a novel hybrid genipin-crosslinked dual-sensitive hydrogel/nanostructured lipid carrier (NLC) drug delivery platform. An ophthalmic anti-inflammatory drug, baicalin (BN) was chosen as the model drug. BN-NLC was prepared using melt-emulsification combined with ultra-sonication technique. Read More

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http://dx.doi.org/10.1016/j.ajps.2018.08.002DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7032125PMC

Optimizing pH-sensitive and time-dependent polymer formula of colonic pH-responsive pellets to achieve precise drug release.

Asian J Pharm Sci 2019 Jul 28;14(4):413-422. Epub 2018 Aug 28.

School of Pharmacy, Guangdong Medical University, No.1, Xincheng Road, Dongguan 523808, China.

Time-sensitive and pH-dependent polymers are generally employed to prepare colon-site delivery system, and their coating thickness and order are very important in controlling the drug release. The traditional colon-site delivery systems consist of time-dependent polymers as inner layer and pH-sensitive polymers as outer layer. However, they suffer from low drug-loading rate and immature drug release. Read More

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http://dx.doi.org/10.1016/j.ajps.2018.05.012DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7032081PMC

Amino functionalized chiral mesoporous silica nanoparticles for improved loading and release of poorly water-soluble drug.

Asian J Pharm Sci 2019 Jul 1;14(4):405-412. Epub 2018 Jul 1.

Wuya college of Innovation, Shenyang Pharmaceutical University, No.103, Wenhua Road, Shenyang 110016, China.

In the present paper, chiral mesoporous silica nano-cocoon (A-CMSN) functionalized with amino group was synthesized, and its loading and release of indomethacin (IMC), a poorly soluble drug, was studied. Due to the use of chiral anionic surfactants as a template, A-CMSN possessed 2D hexagonal nano-cocoon morphology with curled channels on its surface, which was quite different from another 2D hexagonal mesoporous silica nanoparticles (MCM-41) with straightway channels. After being loaded into the two silica carriers by hydrogen bond, crystalline IMC converted to amorphous form, leading to the improved drug dissolution. Read More

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http://dx.doi.org/10.1016/j.ajps.2018.04.002DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7032221PMC