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Pharmaceutical Development and Technology

Mouhamad Reslan, Veysel Kayser
Protein aggregation is a significant problem affecting the integrity of proteins, and is a major hindrance to the development of biopharmaceutical products. Deuterium Oxide (D2O), widely used in protein characterization studies, has been shown to promote protein aggregation when used as a substitute for water in most buffered protein solutions; however, a few studies have reported minor improvements in melting point temperatures for some proteins. Our study aims to investigate the effect of D2O on protein stability, using bovine serum albumin (BSA) as a model...
December 2, 2016: Pharmaceutical Development and Technology
Muhammad Tayyab Ansari, Muhammad Sohail Arshad, Altaf Hussain, Zeeshan Ahmad
The purpose of this study was to investigate changes in the water solubility of artemether; a poorly soluble drug used for the treatment of malaria. Different solid dispersions (SD) of artemether were prepared using; artemether and polyethyleneglycol 6000 at ratio 12:88 (Group 1), self-emulsified solid dispersions (SESD) containing artemether, polyethylene glycol 6000, cremophor-A-25, olive oil, hydroxypropylmethylcellulose and transcutol in the ratio 12:75:5:4:2:2, respectively (Group 2). SESD's were also prepared by substituting cremophor-A-25 in Group 2 with poloxamer 188 (noted as Group 3)...
November 25, 2016: Pharmaceutical Development and Technology
Tai Xia, Qin He, Kairong Shi, Yang Wang, Qianwen Yu, Li Zhang, Qianyu Zhang, Huile Gao, Lifang Ma, Ji Liu
The dense collagen network in tumors restricts the penetration of drugs into tumors. Free losartan could inhibit collagen, but it would cause hypotension at the dosage of 10 mg/kg/d. In this study, losartan was encapsulated in liposomes (LST-Lip) and the collagen inhibition ability of LST-Lip was investigated. Our results showed the blood pressure was not affected by LST-Lip at the dosage of 2.5 mg/kg every other day. The amount of Evans Blue in tumor in LST-Lip group was 1.98 times of that in control group...
November 25, 2016: Pharmaceutical Development and Technology
Xia Yu, Chun-Yang Shi, Jian-Guo Fang, Wang Wen-Qing
Microcrystalline cellulose (MCC) is widely regarded as the excellent choice to manufacture pellets via wet extrusion-spheronisation (ES) process due to its excellent water uptake capability, water holding capacity, desirable rheological properties, cohesiveness and plasticity etc. Nevertheless, in spite of all these advantages, limitations associated with the application of MCC also have been reported. The most prevailing limitation is prolonged or incomplete drug release profile due to the lack of disintegration as pellet contracts significantly during the drying process, especially when in combination with poorly soluble drug at a high level...
November 24, 2016: Pharmaceutical Development and Technology
Paweł Ramos, Barbara Pilawa
Free radicals in thermally treated chloramphenicol were examined by electron paramagnetic resonance (EPR) spectroscopy. The parameters and shape of EPR spectra were analysed and free radical concentrations were obtained in the tested drug samples. Chloramphenicol was thermally sterilised at pharmacopoeia conditions: 100°C (120 minutes). Sterilisation was also carried out at different conditions, 110°C (60 minutes) and 120°C (30 minutes), for comparison with pharmacopeia settings. Microbiological analysis was performed on the samples to confirm sterility...
November 24, 2016: Pharmaceutical Development and Technology
Min-Ho Park, Hye-Suk Jun, Jong-Woon Jeon, Jin-Kyu Park, Bong-Joo Lee, Guk-Hyun Suh, Jeong-Sook Park, Cheong-Weon Cho
Bee venom-loaded poly(lactic-co-glycolic acid) (PLGA) particles were prepared by double emulsion-solvent evaporation, and characterized for a sustained-release system. Factors such as the type of organic solvent, the amount of bee venom and PLGA, the type of PLGA, the type of polyvinyl alcohol, and the emulsification method were considered. Physicochemical properties, including the encapsulation efficiency, drug loading, particle size, zeta-potential, and surface morphology were examined by Fourier transform infrared (FT-IR) spectroscopy, differential scanning calorimetry (DSC), and X-ray diffraction (XRD)...
November 24, 2016: Pharmaceutical Development and Technology
Darjan Košir, Tadej Ojsteršek, Saša Baumgartner, Franc Vrečer
The drug release profile from hydrophilic matrix tablets can be crucially affected by the variability of physicochemical properties of the controlled release agent. This study investigates and seeks to understand the functionality-related characteristics (FRCs) of hydroxypropyl methylcellulose (HPMC) type 2208, K4M grade, that influence the release rate of the model drug carvedilol from hydrophilic matrix tablets during the entire dissolution profile. The following FRCs were examined: particle size distribution, degree of substitution, and viscosity...
November 23, 2016: Pharmaceutical Development and Technology
Preetanshu Pandey, Christopher Levins, Steve Pafiakis, Brian Zacour, Dilbir S Bindra, Jade Trinh, David Buckley, Shruti Gour, Shasad Sharif, Howard Stamato
The objective of this study was to improve the disintegration and dissolution characteristics of a highly water-soluble tablet matrix by altering the manufacturing process. A high disintegration time along with high dependence of the disintegration time on tablet hardness was observed for a high drug loading (70% w/w) API when formulated using a high-shear wet granulation process. Keeping the formulation composition mostly constant, a fluid bed granulation process was explored as an alternate granulation method...
November 23, 2016: Pharmaceutical Development and Technology
Nimra Iqbal, Carla Vitorino, Kevin M G Taylor
The development of a transdermal nanocarrier drug delivery system with potential for the treatment of psychiatric disorders, such as schizophrenia and bipolar disorder, is described. Lipid nanocarriers (LN), encompassing various solid:liquid lipid compositions were formulated and assessed as potential nanosystems for transdermal delivery of olanzapine. A previously optimized method of hot high pressure homogenization (HPH) was adopted for the production of the LN, which comprised solid lipid nanoparticles (SLN), nanostructured lipid carriers (NLC) and nanoemulsions (NE)...
November 23, 2016: Pharmaceutical Development and Technology
Ahmad Ainurofiq, Syaiful Choiri
The purpose of this research was to develop an inclusion complex of meloxicam (MEL)/β-cyclodextrin (β-CD) incorporated into an orally disintegrating tablet (ODT), using statistical analysis to optimize the ODT formulation based on a quality by design (QbD) approach. MEL/β-CD complexation was performed by kneading, co-precipitation, and spray drying methods under different molar ratios. Fourier transform infrared spectroscopy, X-Ray diffraction, and thermal analysis were utilized to evaluate the complexes...
November 22, 2016: Pharmaceutical Development and Technology
Azar Kajbafvala, Alireza Salabat, Anayatollah Salimi
The aim of this study was to develop a new microemulsion formulation for topical application of poorly soluble drug named quercetin. In order to design suitable microemulsion system, the pseudo-ternary phase diagrams of microemulsion systems were constructed at different surfactant/co-surfactant ratios using tween 80 as surfactant, transcutol® P as co-surfactant and oleic acid as oil phase. Some physicochemical properties such as droplet size, density, refractive index, electrical conductivity, pH, surface tension and viscosity of the microemulsion systems were measured at 298...
November 22, 2016: Pharmaceutical Development and Technology
Nian-Qiu Shi, Hong-Wei Lai, Yong Zhang, Bo Feng, Xiao Xiao, Hong-Mei Zhang, Zheng-Qiang Li, Xian-Rong Qi
Polyvinyl caprolactam-polyvinyl acetate-polyethylene glycol graft copolymer, or Soluplus(®), is a relatively new copolymer and a promising carrier of amorphous solid dispersions. Knowledge on the inherent properties of Soluplus(®) (e.g. cloud points, critical micelle concentrations, and viscosity) in different conditions is relatively inadequate, and the application characteristics of Soluplus(®)-based solid dispersions made by microwave methods still need to be clarified. In the present investigation, the inherent properties of a Soluplus(®) carrier, including cloud points, critical micelle concentrations, and viscosity, were explored in different media and in altered conditions...
November 16, 2016: Pharmaceutical Development and Technology
Rania Hamed, Tamadur Al Baraghthi, Suhair Sunoqrot
Drug release from hydroxypropyl methylcellulose (HPMC) hydrophilic matrix tablets is controlled by drug diffusion through the gel layer of the matrix-forming polymer upon hydration, matrix erosion, or combination of diffusion and erosion mechanisms. In this study, the relationship between viscoelastic properties of the gel layer of swollen intact matrix tablets and drug release was investigated. Two sets of quetiapine fumarate (QF) matrix tablets were prepared using the high viscosity grade HPMC K4M at low (70 mg/tablet) and high (170 mg/tablet) polymer concentrations...
November 3, 2016: Pharmaceutical Development and Technology
Jing Fu, Xiaoxv Dong, Xinbing Yin, Chunjing Yang, Wenping Wang, Xueying Du, Xin Zhang, Jian Ni
Isoimperatorin is a naturally occurring furocoumarin and is being considered as a potential chemoprevention. Only one crystal form of isoimperatorin (Form I) was reported during previous research so that an investigation of polymorphism of isoimperatorin was successfully undertaken. A new polymorph of isoimperatorin was discovered through comprehensive polymorph screening experiments. Their structures were elucidated by single-crystal structure analysis and extensively characterized by XRPD, DSC, FT-IR and SEM...
November 3, 2016: Pharmaceutical Development and Technology
Rana Obaidat, Nizar Al-Shar'i, Bassam Tashtoush, Tamara Athamneh
Levodopa is a promising candidate for administration via the transdermal route because it exhibits a short plasma half-life and has a small window of absorption in the upper section of the small intestine. The aim of this study was to prepare stable levodopa transdermal patches. Both xanthan gum and Carbopol 971 polymers were selected with ethylcellulose constituting the backing layer of the prepared patches. The effect of adding β-cyclodextrin on the prepared patches was investigated. The uniformity in thickness, weight and content of the studied patches was acceptable...
November 3, 2016: Pharmaceutical Development and Technology
Negar Seyedhassantehrani, Roya Karimi, Gholamreza Tavoosidana, Amir Amani
Problems commonly associated with using nanoemulsions are their cytotoxic effects and low stability profiles. Here, for the first time, concentrations of ingredients of a nanoemulsion system were investigated to obtain the most stable nanoemulsion system with the least cytotoxic effect on MCF7 cell line. Artificial neural networks (ANNs) were used to model the experimentally obtained data. Surfactant concentration was found to be the dominant factor in determining the stability - surfactant concentration above a critical point made the preparation unstable, while it appeared not to be influencing the cytotoxicity...
October 25, 2016: Pharmaceutical Development and Technology
Kyu-Mok Hwang, Woojin Byun, Cheol-Hee Cho, Eun-Seok Park
The aim of this study was to prepare a highly porous multiparticulate dosage form containing cilostazol for gastroretentive drug delivery. The floating pellets were prepared with glyceryl behenate as a matrix former and camphor as a sublimating agent by extrusion-spheronization and sublimation under vacuum. Granules prepared with sublimation at 60°C displayed a slower dissolution rate and smoother surface morphology than those prepared at lower temperatures. This was unexpected as the reported melting point of glyceryl behenate is higher than 69°C...
October 10, 2016: Pharmaceutical Development and Technology
Talitha Caldas Dos Santos, Mariana Alves Battisti, Caroline Flach Ortmann, Flávio Henrique Reginatto, Cláudia Maria Oliveira Simões, Angela Machado de Campos
Studies employing Cecropia glaziovii Snethl leaves have shown great potential in regard to their antiviral activity, mainly related to the phenolic compounds present in this species. The main goal of this work is to combine the therapeutic potential of this species with new technological strategies targeted at the development of an herbal nanoparticulate system for prepare a phytotherapeutic formulation. Poly (lactic-co-glycolic acid) nanoparticles containing the enriched flavonoid fraction of Cecropia glaziovii Snethl were developed through a study for the choice of preparation technique, amount of drug and surfactants used...
October 6, 2016: Pharmaceutical Development and Technology
Jaya Malladi, Kurex Sidik, Sutan Wu, Ryan McCann, Jeffrey Dougherty, Prakash Parab, Thomas Carragher
Tablet hardness, a measure of the breaking force of a tablet, is based on numerous factors. These include the shape of the tablet and the mode of the application of force. For instance, when a pentagonal-shaped tablet was tested with a traditional hardness tester with flat platens, there was a large variation in hardness measurements. This was due to the propensity of vertices of the tablet to crush, referred to as an "improper break". This article describes a novel approach to measure the hardness of pentagonal-shaped tablets using modified platens...
October 4, 2016: Pharmaceutical Development and Technology
Jaber Emami, Mahboubeh Rezazadeh, Hojjat Sadeghi, Khashayar Khadivar
The treatment of brain cancer remains one of the most difficult challenges in oncology. The purpose of this study was to develop transferrin-conjugated nanostructured lipid carriers (Tf-NLCs) for brain delivery of paclitaxel (PTX). PTX-loaded NLCs (PTX-NLCs) were prepared using solvent evaporation method and the impact of various formulation variables were assessed using Box-Behnken design. Optimized PTX-NLC was coupled with transferrin as targeting ligand and in vitro cytotoxicity of it was investigated against U-87 brain cancer cell line...
September 30, 2016: Pharmaceutical Development and Technology
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