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AAPS PharmSciTech

Qingqing Zhai, Hailong Li, Yanlin Song, Ruijiao Wu, Chuanfang Tang, Xiaodong Ma, Zhihao Liu, Jinyong Peng, Jianbin Zhang, Zeyao Tang
This work aimed to develop and optimize several lipid nanocapsule formulations (LNCs) to encapsulate cisplatin (CDDP) for treatment of hepatocellular carcinoma. By comparing the effect of oil/surfactant ratio, lecithin content, and oil/surfactant type on LNC characteristics, two LNCs were selected as optimal formulations: HS15-LNC (Solutol HS 15/MCT/lecithin, 54.5:42.5:3%, w/w) and EL-LNC (Cremophor EL/MCT/lecithin, 54.5:42.5:3%, w/w). Both LNCs could effectively encapsulate CDDP with the encapsulation efficiency of 73...
April 20, 2018: AAPS PharmSciTech
Wenxiu Wei, Shida Li, Hongmei Xu, Feilong Zhou, Yi Wen, Zhimei Song, Sijia Feng, Runliang Feng
Macrolide antibiotics are lipophilic drugs with some limitations including low solubility, limited cellular permeation, patients discomfort, etc. With amphiphilic methoxy poly(ethylene glycol)-b-poly(ε-caprolactone) (MPEG-PCL) copolymer and azithromycin (AZT) as drug carrier and model drug, AZT-loaded micelles were prepared via thin-membrane hydration method in order to overcome these limitations. Encapsulation efficiency of AZT-loaded micelles was 94.40% with good storage stability for 28 days, and AZT's water solubility was enhanced to 944 μg/mL...
April 19, 2018: AAPS PharmSciTech
Ruhi V Ubale, Prathap Nagaraja Shastri, Carl Oettinger, Martin J D'Souza
Targeted delivery to the lung for controlling lung inflammation is an area that we have explored in this study. The purpose was to use microparticles containing an antisense oligonucleotide (ASO) to NF-κB to inhibit the production of proinflammatory cytokines. Microparticles were prepared using the B-290 Buchi Spray Dryer using albumin as the microparticle matrix. Physicochemical characterization of the microparticles showed the size ranged from 2 to 5 μm, the charge was - 38.4 mV, and they had a sustained release profile over 72 h...
April 16, 2018: AAPS PharmSciTech
Tejal Rawal, Neha Mishra, Abhishek Jha, Apurva Bhatt, Rajeev K Tyagi, Shital Panchal, Shital Butani
The elevated blood levels of cholesterol and low-density lipoproteins result in hyperlipidemia. The available expensive prophylactic treatments are kindred with severe side effects. Therefore, we fabricated the polymeric nanoparticles of gamma-oryzanol to achieving the improved efficacy of drug. The nanoparticles were prepared by ionic gelation method and optimized using 23 full factorial design taking drug/polymer ratio (X1 ), polymer/cross linking agent ratio (X2 ), and stirring speed (X3 ) as independent variables...
April 16, 2018: AAPS PharmSciTech
Zi-Qiang Li, Shuang Tian, Hui Gu, Zeng-Guang Wu, Makafui Nyagblordzro, Guo Feng, Xin He
Each of dissolution and permeation may be a rate-limiting factor in the absorption of oral drug delivery. But the current dissolution test rarely took into consideration of the permeation property. Drug dissolution/absorption simulating system (DDASS) valuably gave an insight into the combination of drug dissolution and permeation processes happening in human gastrointestinal tract. The simulated gastric/intestinal fluid of DDASS was improved in this study to realize the influence of dynamic pH change on the complete oral dosage form...
April 16, 2018: AAPS PharmSciTech
Divya Sunkara, Maxx Capece
This study investigated the effect of material properties, primarily particle size and surface energy, on the effectiveness of glidants used for the purpose of flowability enhancement. Three pharmaceutical grade glidants (Aerosil 200, Aerosil R972, and Cab-O-Sil M5P) were evaluated and blended with various pharmaceutical actives as well as cohesive excipients common to capsule and tablet formulation. Flowability enhancement was characterized by the flow function coefficient (ff c ). An industry-relevant mixer (Turbula mixer) and a highly efficient and effective mixer (LabRAM vibratory mixer) were used to further understand the effect of material properties on glidant effectiveness...
April 16, 2018: AAPS PharmSciTech
Rabia Gul, Naveed Ahmed, Naseem Ullah, Muhammad Ijaz Khan, Abdelhamid Elaissari, Asim Ur Rehman
Biodegradable materials are extensively employed to design nanocarriers that mimic extracellular environment in arthritis. The aim of this study was to formulate and characterize biocompatible, biodegradable ketoprofen-loaded chitosan-chondroitin sulfate (CHS-CS) nanoparticles with natural ingredients for transdermal applications. Polymers used in the design of nanocarriers are biodegradable and produce synergistic anti-inflammatory effect for the treatment of arthritis. For transdermal application, argan oil-based emulgel is utilized to impart viscosity to the formulation...
April 12, 2018: AAPS PharmSciTech
Shiqi Hong, Steven A Nowak, Chan Lai Wah
The precipitation inhibitory effect of cellulosic polymers in relation to their physicochemical properties was studied. Using a poorly water-soluble model drug, griseofulvin, the precipitation inhibitory effect of a series of hydroxypropyl methylcellulose (HPMC) and methylcellulose polymers was studied using solvent-shift method. The extent of supersaturation maintenance of each polymer was then quantified by the parameter, supersaturation factor (SF). Partial least square (PLS) regression analysis was employed to understand the relative contribution from viscosity, hydroxypropyl content (HC), methoxyl content, methoxyl/hydroxypropyl ratio, and drug-polymer interaction parameter (χ) on SF...
April 10, 2018: AAPS PharmSciTech
Maria Alice Maciel Tabosa, Ana Rosa Brissant de Andrade, Ana Amélia Moreira Lira, Victor Hugo Vitorino Sarmento, Davi Pereira de Santana, Leila Bastos Leal
This project was carried out to investigate the feasibility of using microemulsions for transdermal delivery of lapachol. From the screening of surfactants and oils, a range of microemulsions were developed using oleic acid, a mixture of Cremophor EL and Tween 20 and water. The solubility of lapachol was determined in these ingredients and in the formulated microemulsions. The microemulsions were characterised using cross-polarising light microscopy, their electrical conductivity, pH, zeta potential and rheology were analysed, and they were also investigated using small-angle X-ray scattering and differential scanning calorimetry...
April 10, 2018: AAPS PharmSciTech
Xu Xue, Mengyuan Cao, Lili Ren, Yiwen Qian, Guoguang Chen
In this paper, a novel self-nanoemulsifying drug delivery system (SNEDDS) was used to improve the oral bioavailability in fasted state and diminish the food effect for rivaroxaban. Oil, surfactant, and co-surfactant were selected by saturated solubility study. IPM, Tween80, and 1,2-propanediol were finally selected as oil, surfactant, and co-surfactant, respectively. The pseudo-ternary-phase diagram was utilized to optimize the preliminary composition of SNEDDS formulation. The optimized rivaroxaban-SNEDDS formulation was selected by central composite design (CCD) of response surface methodology...
April 10, 2018: AAPS PharmSciTech
Galen H Shi, Xia Dong, Michelle Lytle, Craig A J Kemp, Robert J Behme, Jeremy Hinds, Zhicheng Xiao
This study aimed to elucidate the mechanisms and kinetics of coating failure for enteric coated beads exposed to high-humidity conditions at different storage temperatures. Enteric coated beads were placed on high-humidity conditions (75 to 98% relative humidity (RH)) in the temperature range of 5 to 40°C. These stability samples of beads were tested for acid dissolution and water activity and also analyzed with SEM, X-ray CT, and DMA. Exposure of enteric coated beads to high humidity led to increased gastric release of drug which eventually failed the dissolution specification...
April 9, 2018: AAPS PharmSciTech
Lindsay A Wegiel, Steven J Ferris, Steven L Nail
One of the current methods for cycle optimization in primary drying to is develop a graphical design space based on quality by design (QbD). In order to construct the design space, the vial heat transfer coefficient (Kv ) is needed. This paper investigated experimental factors that can affect the Kv result, examined the relationship between the batch average Kv and Kv values for individual vials, and recommended best practices for measuring Kv . Factors investigated included the technique for measuring ice temperature, shelf temperature, the use of a radiation shield on the door of the freeze-dry chamber, and shelf spacing...
April 3, 2018: AAPS PharmSciTech
Shubhmita Bhatnagar, Pooja Kumari, Srijanaki Paravastu Pattarabhiran, Venkata Vamsi Krishna Venuganti
Localized delivery of chemotherapeutic agents to treat breast cancer could limit their adverse drug reactions. The aim of this study was to investigate the influence of physico-chemical properties of chemotherapeutic agents in their loading, release behavior, and skin permeation using microneedles. Zein microneedles were fabricated using the micromolding technique containing 36 microneedles in a 1-cm2 area. These microneedles were loaded with two anti-breast cancer drugs, tamoxifen and gemcitabine, having different water solubilities...
April 3, 2018: AAPS PharmSciTech
Javier Rueda Arregui, Surya Prakasarao Kovvasu, Guru V Betageri
The aim of this study was to develop a proliposomal formulation of lipopeptide antibiotic drug daptomycin (DAP) for oral delivery. Thin film hydration was the selected method for preparation of proliposomes. Different phospholipids including soy-phosphatidylcholine (SPC), hydrogenated egg-phosphatidylcholine (HEPC), and distearoyl-phosphatidylcholine (DSPC) were evaluated in combination with cholesterol. The inclusion of surface charge modifiers in the formulation such as dicetyl phosphate (DCP) and stearylamine (SA) to enhance drug encapsulation was also evaluated...
April 3, 2018: AAPS PharmSciTech
M Li, P Alvarez, P Orbe, E Bilgili
Characterization of wet-milled drug suspensions containing neutral polymer-anionic surfactant as stabilizers poses unique challenges in terms of assessing the aggregation state and examining the stabilization mechanisms. Using a multi-faceted characterization method, this study aims to assess the aggregation state of wet-milled griseofulvin (GF) nanosuspensions and elucidate the stabilization mechanisms and impact of stabilizers. Two grades, SSL and L, of hydroxypropyl cellulose (HPC) with molecular weights of 40 and 140 kg/mol, respectively, were used as a neutral stabilizer at concentrations varying from 0 to 7...
March 30, 2018: AAPS PharmSciTech
Mauro Morri, Patricia Castellano, Darío Leonardi, Silvana Vignaduzzo
Liquid formulations can be used in children of different ages by varying the volume of the administered dose in order to ensure an exact dosage. The aim of this work was to develop and to optimize a safe liquid atenolol formulation and to carry out the corresponding chemical and microbiological stability studies. A Plackett-Burman design was used to determine the factors that could be critical in the development of the formulations, and a central composite design was used to determine the optimal working conditions...
March 30, 2018: AAPS PharmSciTech
Thalita Marcílio Cândido, Camila Areias De Oliveira, Maíra Bueno Ariede, Maria Valéria Robles Velasco, Catarina Rosado, André Rolim Baby
Topical application of dermocosmetics containing antioxidant and/or the intake of antioxidants through diet or supplementation are remarkable tools in an attempt to slow down some of the harmful effects of free radicals. Rutin is a strong antioxidant compound used in food and pharmaceutical industries. It was established that rutin presents a low skin permeation rate, a property that could be considered an inconvenience to the satisfactory action for a dermocosmetic formulation to perform its antioxidant activity onto the skin...
March 29, 2018: AAPS PharmSciTech
Kailash C Petkar, Sandip Chavhan, N Kunda, I Saleem, S Somavarapu, Kevin M G Taylor, Krutika K Sawant
A novel hydrophobic chitosan derivative, octanoyl chitosan (OC) with improved organic solubility was synthesized, characterized, and employed for the preparation of rifampicin (Rif) encapsulated nanoparticle formulations for pulmonary delivery. OC was characterized to confirm acyl group substitution and cytotoxicity in A549 epithelial lung cells. OC nanoparticles were produced by the double emulsion solvent evaporation technique without cross-linking and characterized for particle size distribution, morphology, crystallinity, thermal stability, aerosol delivery, and drug release rate...
March 27, 2018: AAPS PharmSciTech
Heather Boyce, Dan Smith, Steve Byrn, Bhawana Saluja, Wen Qu, Vadim J Gurvich, Stephen W Hoag
In vitro evaluation of abuse deterrent formulations (ADFs) is a challenge since real abuse situations are variable and ADF technology is evolving. Specifically, an assessment of an ADF to deter nasal insufflation would be valuable. In this study, a vertical diffusion cell (VDC) was used to evaluate polyethylene oxide (PEO)-based tablets manipulated by three different forces. The commercially available products Oxycontin®, an ADF, Opana®, and metoprolol tartrate tablet formulations made in our laboratory were studied...
March 26, 2018: AAPS PharmSciTech
Hina Javed, Syed Nisar Hussain Shah, Furqan Muhammad Iqbal
The aim of present study is to formulate diphenhydramine nasal nano-emulgels, having lipophilic nano-sized interior droplets, with better penetration for targeted controlled delivery to mucous membrane. Different diphenhydramine (DPH) nasal nano-emulgels were developed having propylene glycol and olive oil (as permeation enhancers) by using RSM for optimization and then evaluated for physico-chemical characteristics and thermal stability. In-vitro drug release through cellophane membrane was conducted and results were analyzed statistically...
March 22, 2018: AAPS PharmSciTech
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