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Pharmaceutical Development and Technology

Ryo Araki, Takashi Matsuzaki, Ayumi Nakamura, Daisaku Nakatani, Shoji Sanada, Hai Ying Fu, Keiji Okuda, Masaki Yamato, Shota Tsuchida, Yasushi Sakata, Tetsuo Minamino
There are few methods available for injectable liposome production under good manufacturing practices (GMP). Injectable liposome production processes under GMP generally consist of liposome formation, size homogenization, organic solvent removal, liposome concentration control and sterilization. However, these complicated and separate processes make it difficult to maintain scalability, reproducibility and sterility. To overcome these limitations, we developed a novel one-step in-line closed liposome production system that integrated all production processes by combining the in-line thermal mixing device with modified counterflow dialysis...
March 20, 2017: Pharmaceutical Development and Technology
Ana I Prata, Patrícia Coimbra, M Eugénia Pina
Diseases affecting the posterior segment of the eye are the most common cause of visual disorders in industrialized countries. This scenario has encouraged the development of new treatment modalities for these diseases, such as drug loaded implants with prolonged drug release. The aim of the present work was to create a polymeric based biodegradable ophthalmic implant for the delivery of dexamethasone. For this purpose, we prepared and compared the in vitro release profiles of dexamethasone ophthalmic implants produced by two methods: melting casting and solvent casting...
March 16, 2017: Pharmaceutical Development and Technology
Samuel Pygall, Sarah Kujawinski, Peter Timmins, Colin Melia
The pH-dependent solubility of a drug can lead to pH-dependent drug release from hydrophilic matrix tablets. Adding buffer salts to the formulation to attempt to mitigate this can impair matrix hydration and negatively impact drug release. An evaluation of the buffering of hydrophilic matrix tablets containing a pH-dependent solubility weak acid drug (flurbiprofen), identified as possessing a deleterious effect on hydroxypropyl methylcellulose (HPMC) solubility, swelling and gelation, with respect to drug dissolution and the characteristics of the hydrophilic matrix gel layer in the presence of tromethamine as a buffer was undertaken...
March 16, 2017: 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...
March 16, 2017: Pharmaceutical Development and Technology
Manish Gupta, Adeyinka Aina, Yamina Boukari, Stephen Doughty, Andrew Morris, Nashiru Billa
Poly(lactic-co-glycolic acid) is a well-studied biodegradable polymer used in drug delivery and other medical applications such as in tissue regeneration. It is often necessary to impart porosity within the scaffold (microparticles) in order to promote the growth of tissue during the regeneration process. Sodium chloride and ammonium bicarbonate have been extensively used as porogens in the generation of porous microstructure. In this study we compared the effect of volumes (250 µl, 500 µl and 750 µl) of two porogens, sodium chloride (1...
March 14, 2017: Pharmaceutical Development and Technology
Yusuf A Haggag, Ahmed M Faheem, Murtaza M Tambuwala, Mohamed A Osman, Sanaa A El-Gizawy, Barry O'Hagan, Nigel Irwin, Paul A McCarron
CONTEXT: Size, encapsulation efficiency and stability affect the sustained release from nanoparticles containing protein-type drugs. OBJECTIVES: Insulin was used to evaluate effects of formulation parameters on minimizing diameter, maximizing encapsulation efficiency and preserving blood glucose control following intraperitoneal (IP) administration. METHODS: Homogenization or sonication was used to incorporate insulin into poly(D,L-lactic-co-glycolic acid) (PLGA) nanoparticles with increasing poly(ethylene glycol) (PEG) content...
March 6, 2017: Pharmaceutical Development and Technology
Vinícius Raphael de Almeida Borges, Marina R Tavares, Julianna Henriques da Silva, Lidia Tajber, Fabio Boylan, Ana Ferreira Ribeiro, Luiz Eurico Nasciutti, Lucio Mendes Cabral, Valeria Pereira de Sousa
Copaiba oleoresin (CPO) obtained from Copaifera landgroffii, is described as active to a large number of diseases and more recently in the endometriosis treatment. In this work poly(lactic-co-glycolic acid) (PLGA) nanoparticles containing CPO were obtained using the design of experiments (DOE) as a tool to optimize the production process. The nanoparticles optimized by means of DOE presented an activity in relation to the cellular viability of endometrial cells. The DOE showed that higher amounts of CPO combined with higher surfactant concentrations resulted in better encapsulation efficiency and size distribution along with good stability after freeze drying...
February 1, 2017: Pharmaceutical Development and Technology
Somchai Sawatdee, Apichart Atipairin, Attawadee Sae Yoon, Teerapol Srichana, Narumon Changsan
Dry foam formulation technology is alternative approach to enhance dissolution of the drug. Sildenafil citrate was suspended in sodium dodecyl sulfate solution and adding a mixture of maltodextrin and mannitol as diluent to form a paste. Sildenafil citrate paste was passed through a nozzle spray bottle to obtain smooth foam. The homogeneous foam was dried in a vacuum oven and sieved to obtain dry foam granules. The granules were mixed with croscarmellose sodium, magnesium stearate and compressed into tablet...
January 30, 2017: Pharmaceutical Development and Technology
A Bonaccorso, T Musumeci, C Carbone, L Vicari, M Rosaria Lauro, G Puglisi
The efficient design of nanocarriers is a major challenge and must be correlated to the route of administration. Intranasal route is studied for local, systemic or cerebral treatments. In order to develop nanocarriers with suitable properties for intranasal delivery, to achieve brain, and to market the product, it is extremely important the simplification of the formulation in terms of raw materials. Surfactants and cryoprotectants are often added to improve structuration and/or storage of polymeric nanoparticles...
January 27, 2017: Pharmaceutical Development and Technology
Peng Cheng, Darren Svirskis, Sung Je Lee, Indrawati Oey, Hae-Soo Kwak, Guanyu Chen, Craig Bunt, Jingyuan Wen
Beta-carotene is a potent antioxidant for maintaining human health. However, its oral absorption is low due to poor aqueous solubility of less than 1 µg/ml. A microemulsion delivery system was designed to solubilize beta-carotene towards enhancing its oral bioavailability. From seven pseudo-ternary diagrams constructed, three systems were selected with large microemulsion areas suitable for oral administration and dilution in the predominately aqueous gastrointestinal fluids. Conductivity and rheology characterization were conducted along four dilution lines within the selected systems...
January 27, 2017: Pharmaceutical Development and Technology
P Barmpalexis, P Syllignaki, K Kachrimanis
Water diffusion through the matrix of three superdisintegrants, namely sodium starch glycolate (SSG), croscarmellose sodium (cCMC-Na) and crospovidone (cPVP), was studied at the sub-molecular level using Attenuated Total Reflectance (ATR)-FTIR spectroscopy and molecular dynamics simulations, and the results were correlated to water uptake studies conducted at the particulate level using Parallel Exponential Kinetics (PEK) modeling in dynamic moisture sorption studies and optical microscopy. ATR-FTIR studies indicated that water diffuses inside cPVP by a single fast acting process, while in SSG and cCMC-Na, a slow and a fast process acting simultaneously, were identified...
January 26, 2017: Pharmaceutical Development and Technology
Venkata R Naidu, Rucha S Deshpande, Moinuddin R Syed, Pravin S Wakte
A direct imaging system (Eyecon™) was used as a Process Analytical Technology (PAT) tool to monitor fluid bed coating process. Eyecon™ generated real-time onscreen images, particle size and shape information of two identically manufactured lab-scale batches. Eyecon™ has accuracy of measuring the particle size increase of ± 1 μm on particles in the size range of 50-3000 μm. Eyecon™ captured data every 2 seconds during the entire process. The moving average of D90 particle size values recorded by Eyecon™ were calculated for every 30 minutes to calculate the radial coating thickness of coated particles...
January 25, 2017: Pharmaceutical Development and Technology
Guolian Ren, Mengjuan Jiang, Weiling Guo, Bingjun Sun, He Lian, Yongjun Wang, Zhonggui He
A redox-responsive docetaxel (DTX) prodrug consisting of a disulfide linkage between DTX and vitamin E (DTX-SS-VE) was synthesized in our laboratory and was successfully formulated into liposomes. The aim of this study was to optimize the formulation and investigate the cellular uptake of DTX prodrug-loaded liposomes (DPLs). The content of DTX-SS-VE was determined by ultra high performance liquid chromatography (UPLC). The formulation and process were optimized using entrapment efficiency (EE), drug-loading (DL), particle size and polydispersity index (PDI) as the evaluation indices...
January 25, 2017: Pharmaceutical Development and Technology
Raid Alany
No abstract text is available yet for this article.
May 2017: Pharmaceutical Development and Technology
Hugo Almeida, Paulo Lobão, Christian Frigerio, Joel Fonseca, Renata Silva, José Manuel Sousa Lobo, Maria Helena Amaral
CONTEXT: Nanostructured lipid carrier (NLC) dispersions present low viscosity and poor mucoadhesive properties, which reduce the pre-corneal residence time and consequently, the bioavailability of ocular drugs. OBJECTIVE: The aim of this study was to prepare thermoresponsive eyedrops based on the combination of lipid nanoparticles and a thermoresponsive polymer with mucomimetic properties (Pluronic® F-127). MATERIALS AND METHODS: NLCi dispersions were prepared based on the melt-emulsification and ultrasonication technique...
May 2017: 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...
May 2017: 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...
May 2017: Pharmaceutical Development and Technology
Amira Motawea, Thanaa Borg, Manal Tarshoby, Abd El-Gawad H Abd El-Gawad
OBJECTIVE: The aim of this study is to develop and characterize self-nanoemulsifying drug delivery system (SNEDDS) of piroxicam in liquid and solid forms to improve its dissolution, absorption and therapeutic efficacy. MATERIALS AND METHODS: The generation of liquid SNEDDS (L-SNEDDS) was composed of soybean or coconut oil/Tween 80/Transcutol HP (12/80/8%w/w) and it was selected as the optimized formulation based on the solubility study and pseudo-ternary phase diagram...
May 2017: Pharmaceutical Development and Technology
Yang Li, Chengcheng Tang, Enbo Zhang, Li Yang
The potential use of liposomes for the pulmonary delivery of colistin has been hindered by their phospholipid membrane permeability resulting in a very low entrapment of colistin in the liposomes. To increase the entrapment capacity of colistin in liposomes, the anionic lipid sodium cholesteryl sulfate (Chol-SO4(-)) was used to enhance the electrostatic attraction between colistin and the lipid membrane. The resulting colistin-entrapped liposomes of Chol-SO4(-) (CCL) showed significantly greater entrapment efficiency in comparison with liposomes without Chol-SO4(-)...
May 2017: Pharmaceutical Development and Technology
Nargess Gandomi, Reyhaneh Varshochian, Fatemeh Atyabi, Mohammad Hossein Ghahremani, Mohammad Sharifzadeh, Mohsen Amini, Rassoul Dinarvand
Multiple sclerosis (MS) is a chronic central nervous system (CNS) inflammation. Efficient drug delivery to brain is however hampered by blood-brain barrier (BBB). In order to have highly efficient and safe delivery of drugs to brain, solid lipid nanoparticles (SLNs) have indicated promising potentials as smart carriers that can pass the blood-brain barrier and deliver therapeutic biomolecules to the brain. In this study, PEGylated SLNs surface modified using anti-Contactin-2 or anti-Neurofascin, two axo-glial-glycoprotein antigens located in node of Ranvier, were prepared...
May 2017: Pharmaceutical Development and Technology
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