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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
Ksenia Kozhikhova, Maria Ivantsova, Maria Tokareva, Iliya Shulepov, Andrey Tretiyakov, Lev Shaidarov, Vladimir Rusinov, Maxim Mironov
Novel method for coating of positively charged liposomes with modified chitosan was elaborated. Liposomes were prepared by stepwise extrusion through inorganic membranes (Anotop) of 0.2 and 0.1 µm pore sizes. Chitosan derivatives were synthesized via the Ugi multicomponent reaction. Several series of liposomal compositions were produced and their properties were compared in terms of particle size, polydispersity index, zeta potential and stability. The effect of various additives was investigated and the optimal composition of the lipid film was determined...
September 28, 2016: Pharmaceutical Development and Technology
Mona F Arafa, Sanaa A El-Gizawy, Mohamed A Osman, Gamal M El Maghraby
Dissolution enhancement is a promising strategy for improving drug bioavailability. Co-crystallization of drugs with inert material can help in this direction. The benefit will become even greater if the inert material can form co-crystal while maintaining its main function as excipient. Accordingly, the objective of the current study was to investigate xylitol as a potential co-crystal co-former for felodipine with the goal of preparing felodipine sublingual tablets. Co-crystallization was achieved by wet co-grinding of the crystals deposited from methanolic solutions containing felodipine with increasing molar ratios of xylitol (1:1, 1:2 and 1:3)...
September 28, 2016: Pharmaceutical Development and Technology
Rohit Bisht, Ilva D Rupenthal
Frequent intravitreal injections are currently used to overcome the ocular barriers and provide sufficient drug to the posterior eye segment. However, intravitreal injections have been associated with a number of complications and high treatment costs. To overcome these limitations, peptide-loaded poly(d,l-lactic-co-glycolic acid) nanoparticles (PLGA NPs) were developed using the nanoprecipitation technique and were optimized via Box-Behnken Design (BBD) and Response Surface Methodology (RSM). Developed NPs were evaluated for potential toxicity and cell apoptosis using the zebrafish embryo toxicity (ZET) model with titanium dioxide NPs and ethanol (1% v/v) serving as positive controls...
September 27, 2016: Pharmaceutical Development and Technology
Ana Santoveña, Irma Charola, Javier Suárez-González, Nuria Teigell-Pérez, Susana García-van Nood, Mabel Soriano, José B Fariña
There is as yet no commercialized preparation for oral administration of flecainide acetate (FA) to children. In such cases, manipulation of commercial tablets is the usual practice in pharmacy services of hospitals and compounding pharmacies, to provide a suitable dosage form for this vulnerable pediatric population group. In this study we have formulated FA as an oral solution, as an alternative to the suspension elaborated from commercial tablets. Due to this sensitivity of young patients, we have used the pure active pharmaceutical ingredient (API) and the lowest permitted levels of pediatric excipients...
September 23, 2016: Pharmaceutical Development and Technology
Rongli Li, Rencai Chen, Weiwei Liu, Cuiying Qin, Jing Han
Astaxanthin oleoresin (AO) has a number of beneficial physiological functions. However, its sensitivity to light, heat, oxygen and gastric fluids has limited its application. In this paper, we describe the preparation of AO enteric microcapsules by coacervation to improve its stability and enteric solubility, and evaluate their efficacy by measuring the drug loading, encapsulation efficiency, optical microscopic appearance, stability, in vitro release and bioavailability. The results obtained showed that the AO enteric microcapsules possessed a high encapsulation efficiency (85...
September 19, 2016: Pharmaceutical Development and Technology
Swapnil Sharadkumar Chudiwal, Mohamed Hassan G Dehghan
The objective of the present study was to design and develop drug-device combination product in particular flunisolide nasal spray using quality by design (QbD) approach. Quality target product profile (QTPP) of flunisolide nasal spray was defined and critical quality attributes (CQAs) i.e. viscosity (cp) (Y1) and D50 DSD (µm) (Y2) were identified. Potential risk factors were identified using a fish bone diagram and failure mode effect analysis (FMEA) tools. Plackett Burman and Box Behnken design were used for screening the significant factors and optimizing the variables range respectively...
September 10, 2016: Pharmaceutical Development and Technology
Sajedeh Kioomars, Somayeh Heidari, Bizhan Malaekeh-Nikouei, Maryam Shayani Rad, Bahman Khameneh, Seyed Ahmad Mohajeri
In this study several Ciprofloxacin (CFX) imprinted and non-imprinted hydrogels were prepared and evaluated as ocular drug delivery systems in aqueous media. 2-hydroxyethyl methacrylate (HEMA) was used as a solvent and backbone monomer, ethylene glycol dimethacrylate (EGDMA) as a cross-linker, methacrylic acid (MAA) as a functional monomer and CFX as the template molecule. CFX imprinted hydrogels (MIPs) were prepared applying different CFX: MAA molar ratios (1:16, 1:20 and 1:32) in feed composition of monomer solutions...
September 1, 2016: Pharmaceutical Development and Technology
Joël Schlatter, Elodie Bourguignon, Elyes Majoul, Sofiane Kabiche, Issa-Bella Balde, Salvatore Cisternino, Jean-Eudes Fontan
Adapted forms for administration to infants are limited. The proposed study was performed to propose oral liquid formulations of idebenone in Ora-Plus and either Ora-Sweet or Ora-Sweet SF, Ora-Blend, Ora-Blend SF, and Inorpha. Each formulation was stored in 30-ml amber glass bottle at 5 or 25°C for 90 days. Idebenone content in these suspensions, determined by a stability-indicating high-performance liquid chromatography method, remained stable at least 90 days in Inorpha when stored at the two temperatures...
September 1, 2016: 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...
September 1, 2016: 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(-)...
August 30, 2016: 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 with using anti-Contactin2 or anti-Neurofascin, two axo-glial-glycoprotein antigens located in node of Ranvier, were prepared...
August 30, 2016: Pharmaceutical Development and Technology
Seiichi Hori, Tsubasa Kawada, Sanae Kogure, Shinako Yabu, Kenji Mori, Masayuki Akimoto
The release characteristics of lipophilic suppositories containing acetaminophen (AAP) were examined using four types of dissolution methods: the basket, paddle, dialysis tubing (DT), and flow-through cell (FTC) methods. The suitability of each apparatus for quality control in AAP compounded suppositories was evaluated using statistical procedures. More than 80% of the drug was released over 60 min in all the release methods studied, with the exception of the basket method. Reproducible and faster release was achieved using the paddle method at 100 and 200 rpm, whereas poor release occurred with the basket method...
August 30, 2016: Pharmaceutical Development and Technology
Babita Kumari, Karthikeyan Kesavan
Clotrimazole (CTZ) is a broad spectrum antimycotic agent known to be very effective locally for the treatment of fungal skin infections. The aim of this study was to study the effect of chitosan-coated microemulsion (CME) for topical delivery of CTZ and also evaluate its in-vitro antifungal efficacy, Ex-vivo permeation and retention ability on the skin surface. The pseudo-ternary phase diagrams were developed using clove oil as oil phase, Tween 80 and propylene glycol as surfactant and co-surfactant, respectively and distilled water as aqueous phase...
August 30, 2016: Pharmaceutical Development and Technology
Muhammad H E ElHansy, Marina E Boules, Heba Farid, Henry Chrystyn, Sameh Kamal El-Maraghi, Mohamed Bakry Al-Kholy, Assem Fouad Mohamed El-Essawy, Maha M Abdelrahman, Amira S A Said, Raghda R S Hussein, Hoda Rabea, Mohamed E A Abdelrahim
Aerodynamic characteristics of aerosol delivery during invasive mechanical ventilation (IMV) are mostly determined by inserting cascade impactor in the circuit. Impactor might have some effect on airflow within IMV. Hence, the aim of the present study was to develop and evaluate new in vitro aerodynamic characterization methodology without affecting airflow in IMV. Breathing simulator was set in standard adult IMV circuit with inspiratory and expiratory pressures of 20 and 5 cm H2O, 1:3 inspiratory-expiratory ratio, 15 breaths min(-1), and tidal volume of 500 ml...
August 30, 2016: Pharmaceutical Development and Technology
Worranan Rangsimawong, Praneet Opanasopit, Theerasak Rojanarata, Suwannee Panomsuk, Tanasait Ngawhirunpat
The effect of sonophoresis on the transdermal drug delivery of sodium fluorescein (NaFI)-loaded lipid nanocarriers such as liposomes (LI), niosomes (NI) and solid lipid nanoparticles (SLN) was investigated by confocal laser scanning microscopy (CLSM), fourier transform infrared spectroscopy (FTIR) and scanning electron microscopy (SEM). The results showed that SN decreased the skin penetration of NaFI-loaded SLN (6.32-fold) and NI (1.79-fold), while it increased the penetration of NaFI-loaded LI (5.36-fold)...
August 30, 2016: Pharmaceutical Development and Technology
Wenshi Lai, Qiuhong Kang, Chengjuan Zou, Qingrui Li, Huiting Sun, Wen Tan
An intravenously injectable liquid formulation of the poorly water-soluble isosteviol sodium (ISVNa) that has a great clinical potential for cardiovascular diseases was developed using the co-solvent technology. The pH and composition of the co-solvent were optimized to obtain a stable liquid formulation (termed as STVNa) based on saline at pH 10.0 containing 25% (v/v) of ethanol and 20% (v/v) of propylene glycol. STVNa was physicochemically stable upon storage for more than three months under various conditions...
August 24, 2016: Pharmaceutical Development and Technology
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