检索结果-南通市图书馆

In vitro and in vivo evaluation of cubosomes containing 5-fluorouracil for liver targeting

在线全文

学校读者我要写书评

暂无评论

Acta Pharmaceutica Sinica B 2015年第1期5卷 79-88页

作者： Mohamed Nasr Mohamed K.Ghorab Ahmed Abdelazem Department of Pharmaceutics and Industrial Pharmacy Faculty of Pharmacy Helwan University department of Pharmaceutical Chemistry Faculty of Pharmacy Helwan University

The objective of this study was to prepare cubosomal nanoparticles containing a hydrophilic anticancer drug 5-fluorouracil(5-FU) for liver targeting. Cubosomal dispersions were prepared by disrupting a cubic gel phase of monoolein and water in the presence of Poloxamer 407 as a stabilizer.Cubosomes loaded with 5-FU were characterized in vitro and in vivo. In vitro, 5-FU-loaded cubosomes entrapped 31.21% drug and revealed nanometer-sized particles with a narrow particle size distribution. In vitro 5-FU release from cubosomes exhibited a phase of rapid release of about half of the entrapped drug during the first hour, followed by a relatively slower drug release as compared to 5-FU solution. In vivo biodistribution experiments indicated that the cubosomal formulation significantly(Po 0.05) increased5-FU liver concentration, a value approximately 5-fold greater than that observed with a 5-FU solution.However, serum serological results and histopathological findings revealed greater hepatocellular damage in rats treated with cubosomal formulation. These results demonstrate the successful development of cubosomal nanoparticles containing 5-FU for liver targeting. However, further studies are required to evaluate hepatotoxicity and in vivo antitumor activity of lower doses of 5-FU cubosomal formulation in treatment of liver cancer.

关键词： 5-Fluorouracil Hydrophilic drug Cubosomes Liver targeting Hepatotoxicity

Effect of thermal and chemical modifications on the mechanical and release properties of paracetamol tablet formulations containing corn, cassava and sweet potato starches as filler-binders

在线全文

学校读者我要写书评

暂无评论

Asian Pacific Journal of Tropical Biomedicine 2015年第7期5卷 576-580页

作者： Mariam Vbamiunomhene Lawal Michael Ayodele Odeniyi Oludele Adelanwa Itiola department of pharmaceutics & industrial pharmacy University of Ibadan

Objective: To investigate the effects of acetylation and pregelatinization of cassava and sweet potato starches on the mechanical and release properties of directly compressed paracetamol tablet formulations in comparison with official corn starch.Methods: The native starches were modified by acetylation and pregelatinization. The tablets were assessed using friability(Fr), crushing strength(Cs), disintegration time(Dt) and dissolution parameters. Results: Starch acetylation produced paracetamol tablets that were stronger and had the best balance of mechanical and disintegration properties, while pregelatinization produced tablets that were more friable but had a better overall strength in relation to disintegration than formulations made from natural starches. Correlations mainly existed between Dt and the dissolution parameters t80, t2 and k1 in the formulations. Conclusions: Modification of the experimental starches improved the mechanical and release properties of directly compressed paracetamol tablet formulations. Thus, they can be developed for use as pharmaceutical excipients in specific formulations.

关键词： Starch modification Direct compression Filler-binders Mechanical and release properties

Pulmonary delivery of siRNA against acute lung injury/acute respiratory distress syndrome

维普期刊数据库评论

在线全文

维普期刊数据库

学校读者我要写书评

暂无评论

Acta Pharmaceutica Sinica B 2022年第2期12卷 600-620页

作者： Makhloufi Zoulikha Qingqing Xiao George Frimpong Boafo Marwa A.Sallam Zhongjian Chen Wei He department of pharmaceutics School of PharmacyChina Pharmaceutical UniversityNanjing 211198China department of industrial pharmacy Faculty of PharmacyAlexandria UniversityAlexandria 21521Egypt Shanghai Skin Disease Hospital Tongji University School of MedicineShanghai 200443China

The use of small interfering RNAs(si RNAs)has been under investigation for the treatment of several unmet medical needs,including acute lung injury/acute respiratory distress syndrome(ALI/ARDS)wherein si RNA may be implemented to modify the expression of pro-inflammatory cytokines and chemokines at the m RNA level.The properties such as clear anatomy,accessibility,and relatively low enzyme activity make the lung a good target for local si RNA therapy.However,the translation of si RNA is restricted by the inefficient delivery of si RNA therapeutics to the target cells due to the properties of naked si RNA.Thus,this review will focus on the various delivery systems that can be used and the different barriers that need to be surmounted for the development of stable inhalable si RNA formulations for human use before si RNA therapeutics for ALI/ARDS become available in the clinic.

关键词： Pulmonary administration Drug delivery Nanoparticles siRNA Cellular uptake Endosomal escape Inflammatory diseases ALI/ARDS

Comparison of drug release from liquid crystalline monoolein dispersions and solid lipid nanoparticles using a flow cytometric technique

在线全文

学校读者我要写书评

暂无评论

Acta Pharmaceutica Sinica B 2016年第2期6卷 163-169页

作者： Mohamed Z.Dawoud Mohamed Nasr Department of Pharmaceutics and Industrial Pharmacy Faculty of Pharmacy Helwan University

Colloidal lipid particles such as solid lipid nanoparticles and liquid crystalline nanoparticles have great opportunities as drug carriers especially for lipophilic drugs intended for intravenous administration. In order to evaluate drug release from these nanoparticles and determine their behavior after administration, emulsion droplets were used as a lipophilic compartment to which the transfer of a model drug was measured. The detection of the model drug transferred from monoolein cubic particles and trimyristin solid lipid nanoparticles into emulsion droplets was performed using a flow cytometric technique. A higher rate and amount of porphyrin transfer from the solid lipid nanoparticles compared to the monoolein cubic particles was observed. This difference might be attributed to the formation of a highly ordered particle which leads to the expulsion of drug to the surface of the crystalline particle.Furthermore, the sponge-like structure of the monoolein cubic particles decreases the rate and amount of drug transferred. In conclusion, the flow cytometric technique is a suitable technique to study drug transfer from these carriers to large lipophilic acceptors. Monoolein cubic particles with their unique structure can be used successfully as a drug carrier with slow drug release compared with trimyristin nanoparticles.

关键词： Cubic particles Drug release Drug transfer Flow cytometric technique Emulsion droplets Solid lipid nanoparticles Porphyrin

Development of carrier-free nanocrystals of poorly water-soluble drugs by exploring metastable zone of nucleation

在线全文

学校读者我要写书评

暂无评论

Acta Pharmaceutica Sinica B 2019年第1期9卷 118-127页

作者： Xiaoting Ren Jianping Qi Wei Wu Zongning Yin Tonglri Li Yi Lu Key Laboratory of Drug Targeting and Drug Delivery Systems West China School of Pharmacy Sichuan University department of pharmaceutics School of Pharmacy Fudan University department of industrial and Physical pharmacy College of Pharmacy Purdue University

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. A solution may stay supersaturated without forming any nuclei and become metastable. The maximal degree of supersaturation is known as the metastable zone width. When nucleation is triggered directly from the metastable zone, it helps to produce homogeneous nuclei leading to uniform nanocrystals. Herein, we report a study in which the solubility and metastable limit of paclitaxel(PTX) in ethanol aqueous solution were measured at 40 °C. A wide range of metastable compositions were studied to prepare carrier-free PTX nanocrystals with particle size smaller than250 nm and PDI less than 0.25. Compared with the raw material, dissolution rate of PTX nanocrystals was significantly increased. The study enables production of high-quality drug nanocrystals for treating patients.

关键词： Nanocrystals Metastable zone Nucleation Sonication Dissolution Paclitaxel

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

在线全文

学校读者我要写书评

暂无评论

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(P.yoelii)(a resistant malaria parasite strain used in animal stuthes) infection in mice.Methods: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 P.yoelii infection in mice was investigated and compared with those of standard antimalaria drugs used in the treatment of malaria parasite infection.Acute 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 extract.The 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 administered.The extracts showed prophylactic effect by significantly delaying the onset of infection with the suppression of 79% at a dose of 1 600 mg/kg/day.Conclusions:The results obtained indicate that the extracts of the whole plant of P.amarus possess repository and chemotherapeutic effects against resistant strains of P.yoelii in Swiss albino mice.The findings justify the use of the extract of P.amarus in traditional medicine practice,for the treatment of malaria infections.

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

Flavonoids kaempferide and 4,2’-dihydroxy-4’,5’,6’-trimethoxychalcone inhibit mitotic clonal expansion and induce apoptosis during the early phase of adipogenesis in 3T3-L1 cells

维普期刊数据库评论

在线全文

维普期刊数据库

学校读者我要写书评

暂无评论

Journal of Integrative Medicine 2019年第4期17卷 288-295页

作者： Supakanya Kumkarnjana Rutt Suttisri Ubonthip Nimmannit Apirada Sucontphunt Mattaka Khongkow Thongchai Koobkokkruad Nontima Vardhanabhuti Department of Pharmaceutics and Industrial Pharmacy Faculty of Pharmaceutical SciencesChulalongkorn University Nano-Cosmeceuticals Laboratory National Nanotechnology CenterNational Science and Technology Development Agency

Objective: Kaempferide and 4,2'-dihydroxy-4',5',6'-trimethoxychalcone (DTMC) are two major flavonoids found in Chromolaena odoraia Linn, leaf extract. The aim of this study was to elucidate the mechanism by which these two flavonoids exerted their effect on adipogenesis. The inhibitory effect of kaempferide and DTMC on adipocyte differentiation and their mechanisms involving mitotic clonal expansion (MCE) and apoptosis during the early stage of adipogenesis were investigated. Methods: Confluent 3T3-L1 preadipocytes were induced to differentiate and exposed to the flavonoids during various phases of difTerentiaiion. Intracellular lipid accumulation, cell density and expression of the transcription factors peroxisome proliferator-activated receptor γ and CCAAT/enhancer-binding pro-teins a were assessed using AdipoRed, Oil red 0 and Western blot assays. Effects of both flavonoids on cell proliferation and apoptosis were also determined by carboxyfluorescein diacetate succinimidyl ester and annexin V-fluorescein isothiocyanate/propidium iodide-staining assays, respectively. Results: Kaempferide and DTMC showed significant, concentration-dependent anti-adipogenic activity and effect on cell density in the early phase of adipogenesis. The expression of the transcription factors seemed to be reduced when the treatment was prolonged or in the early phase of adipogenesis. These flavonoids interrupted MCE via inhibition of preadipocyte proliferation and induction of apoptosis. DTMC was nearly three times more potent than kaempferide in inducing apoptosis. Conclusion: Kaempferide and DTMC exerted their anti-adipogenic activity through inhibition of MCE, either by suppressing cell proliferation or by inducing apoptosis during the early phase of differentiation.

关键词： Kaempferide 4,2'-Dihydroxy-4',5',6'-trimethoxychalcone Mitotic clonal expansion Apoptosis Anti-adipogenic 3T3-L1 adipocytes

Formulation development of nifedipine controlled-release coated tablets

在线全文

学校读者我要写书评

暂无评论

Asian Journal of Pharmaceutical Sciences 2016年第1期11卷 118-119页

作者： Ananya Ubonratana Sirachaya Choosakul Nara Nilnakara Chaisan Sriwichupong Garnpimol Ritthidej Department of Pharmaceutics and Industrial Pharmacy Faculty of Pharmaceutical Sciences Chulalongkorn University

Due to frequent administration of oral nifedipine tablet, controlled or sustained release of the drug will improve patient compliance, stable blood level and side effect decrement [1,2].Various extended release nifedipine products have been commercially available. In this study, extended release tablets of this drug were formulated using sodium alginate,hydroxypropylmethylcellulose (HPMC) as controlled release matrix materials.

关键词： Nifedipine Extended release tablet Matrix Sodium alginate HPMC

The safety,efficacy and pharmaceutical quality of male enhancement nutraceuticals bought online:Truth versus claim

在线全文

学校读者我要写书评

暂无评论

Journal of Integrative Medicine 2021年第3期19卷 232-242页

作者： Mohamed Ismail Nounou Heba AEassa Nada AHelal Khaled Aboul Fotouh Ihab Mansoor Isabel KLatz Cindy Zheng Hadeer AEassa Dina Mohamed Diana MHuynh Abigail RWiss Jessica Sweeney Monica TOakes Mark MMikhail Nadine Amine Harshvir Kaur Natalia Echeverry Kamila Orzechowski Doreen Szollosi department of Pharmaceutical Sciences School of Pharmacy&Physician Assistant Studies(SOPPAS)University of Saint Joseph(USJ)HartfordConnecticut 06103USA Department of Pharmaceutics and Industrial Pharmacy Faculty of PharmacyAL-Azhar UniversityCairo 11651Egypt Pharmaceutical Sciences department Irma Lerma Rangel College of PharmacyTexas A&M Health Science CenterTexas A&M UniversityCollege StationTexas 77843USA Division of Molecular pharmaceutics and Drug Delivery College of PharmacyThe University of Texas at AustinTexas 78712USA department of pharmaceutics Faculty of PharmacyAssiut UniversityAssiut 71526Egypt department of pharmaceutics Faculty of PharmacyAlexandria UniversityAlexandria 21521Egypt department of Public Health Sciences College of Health SciencesThe University of Texas at El PasoTX 79968USA Genetic Engineering and Biotechnology Research Institute University of Sadat CitySadat 32897Egypt department of industrial pharmacy Faculty of PharmacyAlexandria UniversityAlexandria 21521Egypt

Objective:Nutraceutical products are widely used for their claimed therapeutic benefits.However,falsified or adulterated nutraceuticals present a major health threat to consumers.This study investigates the pharmaceutical quality,safety and anti-inflammatory effects of six male enhancement nutraceuticals that claim to be 100%natural.Methods:Three batches of six male enhancement products were tested to detect the presence and levels of adulterants via high-performance liquid chromatography(HPLC).The pharmaceutical quality of the selected nutraceuticals was tested with near infrared spectroscopy(NIR)and Se De M.The cytotoxic effects of these products on HepG2 cells were determined through cell proliferation(XTT)and lactate dehydrogenase(LDH)cytotoxicity assays.Lastly,the in vitro inflammatory effects of these products were investigated using murine J774 macrophages through cytokine release analysis.Results:HPLC analysis detected the presence of sildenafil citrate,a vasodilator,and the active ingredient in Viagra and Revatio,in all batches of the products we analyzed.Amount of sildenafil citrate ranged from 0.45 mg to 51.85 mg among different batches.NIR assessment showed inter-and intra-batch heterogeneity in product composition.Results of the XTT and LDH assays showed significant cytotoxic effects of the analyzed products.XTT analysis revealed that the viability of HepG2 treated with tested products varied from 27.57%to 41.43%.Interestingly,the male enhancement products also showed anti-inflammatory effects.Conclusion:Despite their labeling as 100%natural,all products tested in this study contained levels of sildenafil citrate,which was not reported on the packaging.There was a lack of pharmaceutical uniformity among products of the same batch and across different batches.Additionally,the products we tested had cytotoxic effects.These study findings highlight the adulteration,poor quality and hazard of these nutraceuticals.Therefore,strict regulation of these products and standardization of the definition of nutra

关键词： Nutraceuticals Adulteration Erectile dysfunction Sildenafil citrate Online market