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Branched module-modified SN38 prodrug nanoassemblies for improved colorectal cancer therapy:Effectively balance efficacy and safety

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Nano Research 2025年第1期18卷 572-585页

作者： Qing Wang Shiyi Zuo Shufang Zheng Cuiyun Liu Yaqiao Li Jiayu Guo Danping Wang Shuo Wang Wenjing Wang Bowen Zhang Minglong Huang Xianbao Shi Jin Sun Zhonggui He Bingjun Sun department of pharmaceutics Wuya College of InnovationShenyang Pharmaceutical UniversityShenyang 110016China Joint International Research Laboratory of Intelligent Drug Delivery Systems Ministry of EducationShenyang Pharmaceutical UniversityShenyang 110016China School of Chemical Engineering The University of AdelaideAdelaideSA 5005Australia department of Pharmacy The First Affiliated Hospital of Jinzhou Medical UniversityJinzhou 121001China

The clinical utility of irinotecan is restricted by individual variability in carboxylesterase *** administration of its active metabolite,7-ethyl-10-hydroxycamptothecin(SN38),presents an appealing alternative due to its potent anti-tumor ***,the undesirable properties of SN38,such as poor water solubility and nontarget toxicity,present significant hurdles to its clinical *** nanoassemblies based on modular design strategy show promise in overcoming these challenges by enhancing drug delivery and selective *** modular design,the modification module plays a crucial role in improving the self-assembly capability of *** current studies mainly focus on using straight aliphatic chains for prodrug design,branched aliphatic chains emerge as superior alternatives warranting further *** this study,we selected 2-heptylundecanol(BAlc18)as modification module to construct an SN38 *** exquisite design,SN38-SS-BAlc18 NPs integrated prominent properties in selfassembly capability,specific activation and biocompatibility,resolving the challenges of irinotecan and SN38,ultimately demonstrating excellent anti-tumor *** exploration enriched the design theory of prodrug nanoassemblies that can effectively balance safety and colorectal anti-tumor efficacy.

关键词： irinotecan SN38 prodrug nanoassemblies disulfide bonds branched aliphatic chains

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Effect of isopropyl myristate on the viscoelasticity and drug release of a drug-in-adhesive transdermal patch containing blonanserin

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Acta Pharmaceutica Sinica B 2016年第6期6卷 623-628页

作者： Chunyi Zhao Peng Quan Chao Liu Qiaoyun Li Liang Fang department of pharmaceutics Shenyang Pharmaceutical University

The purpose of this study was to investigate the effect of isopropyl myristate (IPM), a penetration enhancer, on the viscoelasticity and drug release of a drug-in-adhesive transdermal patch containing blonanserin. The patches were prepared with DURO-TAK (R) 87-2287 as a pressure-sensitive adhesive (PSA) containing 5% (w/w) of blonanserin and different concentrations of IPM. An in vitro release experiment was performed and the adhesive performance of the drug-in-adhesive patches with different concentrations of IPM was evaluated by a rolling ball tack test and a shear-adhesion test. The glass transition temperature (T-g) and rheological parameters of the drug-in-adhesive layers were determined to study the effect of IPM on the mechanical properties of the PSA. The results of the in vitro release experiment showed that the release rate of blonanserin increased with an increasing concentration of IPM. The rolling ball tack test and shear-adhesion test showed decreasing values with increasing IPM concentration. The results were interpreted on the basis of the IPM-induced plasticization of the PSA, as evidenced by a depression of the glass transition temperature and a decrease in the elastic modulus. In conclusion, IPM acted as a plasticizer on DURO-TAK (R) 87-2287, and it increased the release of blonanserin and affected the adhesive properties of the PSA. (C) 2016 Chinese pharmaceutical Association and Institute of Materia Medica, Chinese Academy of Medical Sciences. Production and hosting by Elsevier B.V. This is an open access article under the CC BY-NC-ND

关键词： Isopropyl myristate Drug-in-adhesive patch Viscoelasticity Dnag release Blonanserin

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Hypoglycemic efficacy of chitosan-coated insulin liposomes after oral administration in mice

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Acta Pharmacologica Sinica 2004年第7期25卷 120-126页

作者： Zheng-hong WU, Qi-neng PING2, Yi WEI, Jia-ming LAI department of pharmaceutics, China pharmaceutical University, Nanjing 210009, China department of pharmaceutics China Pharmaceutical University Nanjing 210009

AIM: To evaluate the hypoglycemic efficacy of insulin liposomes coated by chitosan with different molecular weights and concentrations after oral administration in mice. METHODS: Insulin-liposomes were prepared by reversed-phase evaporation. Chitosan coating was carried out by incubation of the liposomal suspensions with the chitosan solution. The hypoglycemic efficacies of chitosan-coated insulin liposomes were investigated by monitor- ing the blood glucose level using the glucose oxidase method after oral administration to healthy mice. RESULTS: In all the insulin liposomes, the insulin liposomes coated by 0.2 % chitosan (Mr 1000 kDa) showed a better hypogly- cemic efficacy as compared with the other liposomes coated by chitosan. The minimum blood glucose level was 15.1 %±6.0 % of the initial (n=6). The hypoglycemic efficacy lasted for 4 h after oral administration to mice. CONCLUSION: Chitosan-coated liposomes could reduce tryptic digestion on insulin, and enhance enteral absorp- tion of insulin. The molecular weights and concentrations of chitosan had significant effects on hypoglycemic efficacy of chitosan-coated insulin liposomes after oral administration to healthy mice.

关键词： chitin chitosan insulin liposomes blood glucose oral administration

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Supersaturation induced by Itraconazole/Soluplus micelles provided high GI absorption in vivo

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Asian Journal of pharmaceutical Sciences 2016年第2期11卷 255-264页

作者： Yue Zhong Guanghui Jing Bin Tian Hao Huang Yuanyuan Zhang Jingxin Gou Xing Tang Haibing He Yanjiao Wang department of pharmaceutics Shenyang Pharmaceutical University

To investigate the effect of supersaturation induced by micelle formation during dissolution on the bioavailability of itraconazole(ITZ)/Soluplus~? solid dispersion. Solid dispersions prepared by hot melt extrusion (HME) were compressed into tablets directly with other excipients. Dissolution behavior of ITZ tablets was studied by dissolution testing and the morphology of micelles in dissolution media was studied using transmission electron microscopy (TEM). Drug transferring from stomach into intestine was simulated to obtain a supersaturated drug solution. Bioavailability studies were performed on the ITZ tablets and Sporanox~? in beagle dogs. The morphology of micelles in the dissolution media was observed to be spherical in shape, with an average size smaller than 100 nm. The supersaturated solutions formed by Soluplus~? micelles were stable and no precipitation took place over a period of 180 min. Compared with Sporanox~?, ITZ tablets exhibited a 2.50-fold increase in the AUC (0–96) of ITZ and a 1.95-fold increase in its active metabolite hydroxyitraconazole (OHITZ) in the plasma of beagle dogs. The results obtained provided clear evidence that not only the increase in the dissolution rate in the stomach, but also the supersaturation produced by micelles in the small intestine may be of great assistance in the successful development of poorly water-soluble drugs. The micelles formed by Soluplus~? enwrapped the molecular ITZ inside the core which promoted the amount of free drug in the intestinal cavity and carried ITZ through the aqueous boundary layer(ABL), resulting in high absorption by passive transportation across biological membranes. The uptake of intact micelles through pinocytosis together with the inhibition of P-glycoprotein-mediated drug efflux in intestinal epithelia contributed to the absorption of ITZ in the gastrointestinal tract. These results indicate that HME with Soluplus~?, which can induce supersaturation by micelleformation, may be of gre

关键词： Solid dispersion Itraconazole tablets Hot melt extrusion Supersaturation Micelles Bioavailability

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Development of cryptotanshinone-loaded pellets for angina chronotherapy:In vitro/in vivo prediction and evaluation

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Asian Journal of pharmaceutical Sciences 2018年第4期13卷 310-316页

作者： Zhenghua Li Shuangshuang Zhang Hongxiang Yan Jianping Liu department of pharmaceutics China Pharmaceutical University

The clinical manifestations of variant angina is unevenly distributed during the 24 h, thusthe in vivo performance of drugs should be tailored according to the angina circadianrhythm. Cryptotanshinone(CTN) is one of the representative bioactive lipid-soluble com-ponents of Danshen which has been commonly used for cardiovascular diseases such asangina pectoris. The aim of this study was to develop a novel CTN sustained-released pel-lets(CTN-SRPs) to precisely synchronize the CTN plasma concentrations with predictedoccurrence of angina pectoris for angina chronotherapy. A deconvolution-based methodwas applied to develop and optimize the CTN-SRPs. The plasma concentration-time curveof CTN immediate-released formulation after oral administration in rats was used as theweight function. The predicted plasma concentration-time curve of CTN-SRPs simulatedaccording to the incidence of variant angina during 24 h was used as the response func-tion. Then the desired drug release profile of CTN-SRPs was calculated based on deconvo-lution using weight function and response function, and subsequently used for guiding theformulation optimization. CTN-SRPs were prepared with the combinations of PVP, polox-amer 127 and EC as matrix using fluidized bed technology. An orthogonal design was em-ployed to obtain the optimal formulation with its release profile similar with the desiredone. Pharmacokinetic studies validated that the actual plasma concentration-time curve ofthese optimized CTN-SRPs was similar with the predicted one. In addition, the percent er-rors(%PE) of CTN plasma concentrations in 8–12 h were less than 10%. In conclusion, thisdeconvolution-based method could be applied to adjust the in vivo performance of drugs forangina chronotherapy.

关键词： Chronotherapy Deconvolution Angina pectoris Cryptotanshinone In vitro/in vivo performance Control release

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Recognition and quality mapping of traditional herbal drugs:way forward towards artificial intelligence

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Traditional Medicine Research 2025年第1期10卷 12-26页

作者： Sanyam Sharma Subh Naman Ashish Baldi Faculty of Pharmacy Pacific Academy of Higher Education and Research UniversityUdaipur 313024India Pharma Innovation Lab Department of Pharmaceutical Sciences and TechnologyMaharaja Ranjit Singh Punjab Technical UniversityBathinda 151001India Faculty of pharmaceutical Sciences The ICFAI UniversityBaddi 174103India.

The use of traditional herbal drugs derived from natural sources is on the rise due to their minimal side effects and numerous health ***,a major limitation is the lack of standardized knowledge for identifying and mapping the quality of these herbal *** article aims to provide practical insights into the application of artificial intelligence for quality-based commercialization of raw herbal *** focuses on feature extraction methods,image processing techniques,and the preparation of herbal images for compatibility with machine learning *** article discusses commonly used image processing tools such as normalization,slicing,cropping,and augmentation to prepare images for artificial intelligence-based *** also provides an overview of global herbal image databases and the models employed for herbal plant/drug *** will gain a comprehensive understanding of the potential application of various machine learning models,including artificial neural networks and convolutional neural *** article delves into suitable validation parameters like true positive rates,accuracy,precision,and more for the development of artificial intelligence-based identification and authentication techniques for herbal *** article offers valuable insights and a conclusive platform for the further exploration of artificial intelligence in the field of herbal drugs,paving the way for smarter identification and authentication methods.

关键词： artificial intelligence Ayurveda machine learning models herbal drugs image pre-processing medicinal plants

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The antiplasmodial effect of the extracts and formulated capsules of Phyllanthus amarus on Plasmodium yoelii infection in mice

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Asian Pacific Journal of Tropical Medicine 2011年第4期4卷 283-287页

作者： Tolulope O Ajala Cecilia I Igwilo Ibrahim A Oreagba Oluwatoyin A Odeku department of pharmaceutics & pharmaceutical technology Faculty of PharmacyOlabisi Onabanjo University department of pharmaceutics and pharmaceutical technology Faculty of PharmacyUniversity of Lagos department of Pharmacology College of MedicineUniversity of Lagos department of pharmaceutics and Industrial Pharmacy Faculty of PharmacyUniversity of Ibadan

Objective:To investigate the antiplasmodial activity of the extracts of Phyllanthus amarus(P. amarus) on Plasmodium yoelii(***)(a resistant malaria parasite strain used in animal stuthes) infection in ***:The aqueous and ethanol extracts of the whole plant of Phyllanthus amarus was administered to Swiss albino mice at doses of 200 mg/kg/day,400 mg/ kg/day,800 mg/kg/day and 1 600 mg/kg/day and the prophylactic and chemotherapeutic effect of the extracts against *** infection in mice was investigated and compared with those of standard antimalaria drugs used in the treatment of malaria parasite *** toxicity test was carried out in mice to determine the safety of the plant extract when administered orally. Results:The results showed that the extracts demonstrated a dose-dependent prophylactic and chemotherapeutic activity with the aqueous extracts showing slightly higher effect than the ethanol *** antiplasmodial effects of the extracts were comparable to the standard prophylactic and chemotherapeutic drugs used in chloroquine resistant Plasmodium infection although the activity depended on the dose of the extract *** extracts showed prophylactic effect by significantly delaying the onset of infection with the suppression of 79% at a dose of 1 600 mg/kg/***:The results obtained indicate that the extracts of the whole plant of *** possess repository and chemotherapeutic effects against resistant strains of *** in Swiss albino *** findings justify the use of the extract of *** in traditional medicine practice,for the treatment of malaria infections.

关键词： Antiplasmodial activity Phyllanthus amarus Plasmodium yoelli Artesunate/amodiaquine Pyrimethamine

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Effects of some common additives on the antimicrobial activities of alcohol-based hand sanitizers

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Asian Pacific Journal of Tropical Medicine 2018年第3期11卷 222-226页

作者： Nzekwe Ifeanyi Thaddeus Egbuna Chukwuemeka Francis Okpara Ogonna Jane Agubata Chukwuma Obumneme Esimone Charles Okechukwu department of pharmaceutics & pharmaceutical technology Nnamdi Azikiwe University department of pharmaceutical technology & Industrial Pharmacy University of Nigeria department of pharmaceutical Microbiology and Biotechnology Nnamdi Azikiwe University

Objective: To study the effects of some common additives on the antimicrobial activities of alcohol-based hand sanitizers. Methods: The antibacterial activities of varying aqueous concentrations of ethanol and isopropyl alcohol were tested by the agar well diffusion method. The influences of different concentrations of glycerin was similarly tested. Finally, isopropyl alcohol and benzalkonium chloride were combined in different ratios within the sate use concentrations of each, and the effects of these combinations were compared with values obtained for the two agents used alone. Statistical methods, such as student t test and one-way ANOVA were used when appropriate to evaluate the differences in activity. Results: The activities of the alcohols showed marked concentration dependence, and both showed peak activity at 85%-95% concentration range. Over the concentration range of 60%-100%, isopropyl alcohol inhibited more bacterial and fungal organisms than ethanol, though the inhibition zone diameters it produced were not statistically different from those of ethanol for organisms which were sensitive to both of *** of glycerin reduced the antimicrobial activities of the isopropyl alcohol, as shown by reduction in the inhibition zone diameters produced in vitro, which may be due to reduced drug diffusion with increase in viscosity. Addition of benzalkonium to isopropyl alcohol systems improved the activity of the alcohol, but the overall activity of the combination was not superior to that seen in the use of benzalkonium alone. Conclusion: Alcohol-based hand sanitizers should not be used outside the concentration range of 85%-95% and isopropyl alcohol inhibits more bacterial and fungal organisms than ethanol for most concentrations. Inclusion of benzalkonium improves the antimicrobial spectrum and activity of isopropyl alcohol, and the combination may justifiably be used to achieve both immediate and long lasting effect. Glycerin may adversely affect the an

关键词： Infection control Disinfection Hand sanitizer Alcohol Optimization

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Parenteral nanosuspensions:a brief review from solubility enhancement to more novel and specific applications

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Acta Pharmaceutica Sinica B 2018年第5期8卷 733-755页

作者： Eknath Ahire Shreya Thakkar Mahesh Darshanwad Manju Misra department of pharmaceutics National Institute of Pharmaceutical Education and Research (NIPER)

Advancements in in silico techniques of lead molecule selection have resulted in the failure of around 70% of new chemical entities(NCEs). Some of these molecules are getting rejected at final developmental stage resulting in wastage of money and resources. Unfavourable physicochemical properties affect ADME profile of any efficacious and potent molecule, which may ultimately lead to killing of NCE at final stage. Numerous techniques are being explored including nanocrystals for solubility enhancement purposes. Nanocrystals are the most successful and the ones which had a shorter gap between invention and subsequent commercialization of the first marketed product. Several nanocrystal-based products are commercially available and there is a paradigm shift in using approach from simply being solubility enhancement technique to more novel and specific applications. Some other aspects in relation to parenteral nanosuspensions are concentrations of surfactant to be used, scalability and in vivo fate. At present, there exists a wide gap due to poor understanding of these critical factors,which we have tried to address in this review. This review will focus on parenteral nanosuspensions,covering varied aspects especially stabilizers used, GRAS(Generally Recognized as Safe) status of stabilizers, scalability challenges, issues of physical and chemical stability, solidification techniques to combat stability problems and in vivo fate.

关键词： Parenteral Nanosuspension Stabilizer In vivo fate Solidification Scalability

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Hot-melt sub-and outercoating combined with enteric aqueous coating to improve the stability of aspirin tablets

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Asian Journal of pharmaceutical Sciences 2017年第3期12卷 266-278页

作者： Xiuzhi Wang Puxiu Wang Chenglong Huang Xiaoyang Lin Haoyu Gong Haibing He Cuifang Cai department of pharmaceutics Science Shenyang Pharmaceutical University

Aspirin is apt to hydrolyze. In order to improve its stability, a new method has been developed involving the application of hot-melt sub-and outercoating combined with enteric aqueous coating. The main aim was to investigate the influence of these factors on the stability of ASA and understand how they work. Satisfactory storage stability were obtained when the aspirin tablet core coated with Eudragit L30D55 film was combined with glycerin monostearate(GMS) as an outercoat. Hygroscopicity testing indicated that the moisture penetrating into the tablet may result in a significant change in the physical properties of the coating film observed by scanning electron microscopy. Investigation of the compatibility between the drug and film excipients shows that the talc and methacrylic acid had a significant catalytic effect on ASA. A hypothesis was proposed that the hydrolysis of ASA enteric coated tablets(ASA-ECT) was mostly concentrated in the internal film and the interfaces between the film and tablet core. In conclusion, hot-melt coating technology is an alternative to subcoating or outercoating. Also, GMS sub-coating was a better choice for forming a stable barrier between the tablet core and the polymer coating layer, and increases the structure and chemical stability.

关键词： Acetylsalicylic acid Hot-melt coating Glycerin monostearate Storage stability Drug/excipient compatibility

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