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AAPS PharmSciTech

Ying Gao, Guo Chen, Xiaojiao Luan, Meijuan Zou, Hongyu Piao, Gang Cheng
In this study, borneol, a natural active compound was applied to improve the bioavailability of curcumin (CUR). In order to increase CUR solubility and dissolution, solid dispersions (SDs) were prepared with the matrix of polyvinylpyrrolidone (PVP) at various ratios by solvent evaporation method. CUR was evidenced to exist as amorphous state in solid dispersion by differential scanning calorimetry (DSC) and powder X-ray diffraction (PXRD). Fourier-transform infrared spectroscopy (FT-IR) was utilized to confirm intermolecular hydrogen bonding...
March 22, 2019: AAPS PharmSciTech
Manoj Kumar Gautam, Mousumi Besan, Divya Pandit, Sanjay Mandal, Renu Chadha
To prepare the cocrystals of 5-fluorouracil (5-FU) with GRAS status coformers via a cocrystallization technique with an aim to improve physicochemical properties as well as bioavailability for colon cancer, breast cancer, and prostate cancer. The mechanochemical method was used in the preparations of three crystals of 5-FU with gentisic acid (5-FUGA), 3,4-dihydroxybenzoic acid (5-FUBA), and 4-aminopyridine (5-FUPN). A thermoanalytical and spectroscopic technique was used for their characterization. Their biological evaluation was done in different cancer cell lines...
March 22, 2019: AAPS PharmSciTech
Shohei Nakamura, Chisato Tanaka, Hiroshi Yuasa, Takatoshi Sakamoto
Direct powder compression is the simplest tablet manufacturing method. However, segregation occurs when the drug content is low. It is difficult to assure drug content uniformity in these cases. In this study, we evaluated microcrystalline cellulose (MCC) as a segregation inhibitor in pharmaceutical powders. We assessed the influence of MCC concentration and mixing time on the physical properties of tablets. The tablet formulation comprised acetaminophen, lactose hydrate, cornstarch, MCC (0%, 10%, or 20%), croscarmellose sodium, and magnesium stearate (Mg-St)...
March 22, 2019: AAPS PharmSciTech
Alexander Kalies, Hüseyin Özcoban, Claudia S Leopold
The aim of this study was to investigate the concept of lower punch vibration as a possible approach to densify the powder bed within the die of a rotary tablet press. Therefore, a laboratory vibration equipment was developed to obtain a better understanding of the performance characteristics and effects of a pneumatically generated vibration system on pharmaceutical powders. For this purpose, two widely used pharmaceutical powders, basic magnesium carbonate (Pharmagnesia MC Type F) and microcrystalline cellulose (Ceolus® KG1000), both with different physical properties, were investigated...
March 20, 2019: AAPS PharmSciTech
Damrongsak Faroongsarng, Somkiat Sunpaweravong, Achara Raksawong
Cancerous invasion yields unusual metabolisms providing a significant amount of peptide albuminomes that modulate albumin stability via binding. The study aimed at the investigation of the thermal stability of human plasma albumin with breast cancer of various stages by means of differential scanning calorimetry (DSC). Blood plasma was drawn from 11 female breast cancer patients and 50 healthy volunteers of homogeneous demographics. Plasma samples and their albumin-enriched fractions were subjected to DSC scanning between 37 and 90°C at 5°C/min rate...
March 18, 2019: AAPS PharmSciTech
Xiangjun Shi, Tiantian Xu, Wan Huang, Baibai Fan, Xiaoxia Sheng
The purpose of this study was to investigate the synergistic effect of polymers and drug-polymer(s) interactions on the improved stability and bioavailability of telmisartan (TEL) ternary solid dispersions. As a water-insoluble drug, 40 and 160 mg doses of TEL tablets exhibited bioavailabilities of 42% and 58%, respectively. Through polymer screening, PVP K30 and/or Soluplus were selected and used at different concentrations to prepare TEL amorphous solid dispersions by solvent evaporation. Compared to pure TEL and TEL-PVP K30/Soluplus binary solid dispersions, TEL-PVP K30-Soluplus ternary solid dispersions demonstrated significant advantages, including higher dissolution (over 90% release at 60 min), better amorphous stability (physically stable in 90 days), and improved oral bioavailability (Cmax of 5535...
March 18, 2019: AAPS PharmSciTech
Jorge Cruz-Angeles, Marcelo Videa, Luz María Martínez
One-third of the population of the USA suffers from metabolic syndrome (MetS). Treatment of patients with MetS regularly includes drugs prescribed simultaneously to treat diabetes and cardiovascular diseases. Therefore, the development of novel multidrug formulations is recommended. However, the main problem with these drugs is their low solubility. The use of binary co-amorphous systems emerges as a promising strategy to increase drug solubility. In the present study, irbesartan (IBS) and glimepiride (GMP), class II active pharmaceutical ingredients (API), widely used in the treatment of arterial hypertension and diabetes, were selected to develop a novel binary co-amorphous system with remarkable enhancement in the dissolution of both APIs...
March 18, 2019: AAPS PharmSciTech
Jeremy Robertson, Marie Squire, Sid Becker
During skin sonoporation and sonophoresis, time-consuming duty cycles or fluid replacement is often required to mitigate coupling fluid temperature increases. This study demonstrates an alternative method for temperature regulation: a circulating, thermoelectric system. Porcine skin samples were sonoporated continuously for 10 min at one of three intensities (23.8, 34.2, 39.4 W/m2 ). A caffeine solution was then applied to the skin and left to diffuse for 20 h. During sonoporation, the system was able to maintain the temperature between 10 and 16°C regardless of the intensity...
March 18, 2019: AAPS PharmSciTech
Ashwini Gumireddy, Ryann Christman, Dunesh Kumari, Amit Tiwari, E Jeffrey North, Harsh Chauhan
Curcumin and resveratrol are natural compounds with significant anticancer activity; however, their bioavailability is limited due to poor solubility. This study aimed to overcome the solubility problem by means of solid lipid nanoparticles (SLN). 2-Hydroxypropyl β-cyclodextrin (HPβCD) was selected from a range of polymers based on miscibility and molecular interactions. SLNs were obtained by probe sonication and freeze-drying curcumin-resveratrol with/without HPβCD incorporated in gelucire 50/13. SLNs were characterized by dynamic light scattering (DLS), zeta potential, powder X-ray diffractometry (PXRD), differential scanning calorimetry (DSC), thermogravimetric analysis (TGA), scanning electron microscopy (SEM), and physical stability...
March 18, 2019: AAPS PharmSciTech
Anis Y Chaerunisaa, Rebaz Ali, Andriy Dashevskiy
The objective of this study was to modify the release of two drugs having different solubility in a combined matrix tablet as a fixed-dose combination for extended release. Propranolol HCl (freely soluble) and carbamazepine (very slightly soluble) were used as model drugs, water-soluble hydroxypropyl methylcellulose (HPMC) and water-insoluble ethylcellulose (EC) were used as matrix-forming polymers. Tablets were prepared by direct compression of powder blends, or propranolol HCl was first granulated with one of the matrix-forming polymers (1:1) followed by compression with carbamazepine and matrix former...
March 14, 2019: AAPS PharmSciTech
Sarika Wairkar, Ram Gaud
In the present work, co-amorphous mixture (COAM) of poorly soluble nateglinide (NT) and highly soluble Metformin hydrochloride (MT) was prepared by spray drying method to improve the dissolution rate of NT and the processability of COAM. Binary spray-dried COAM of NT and MT (120 mg: 500 mg) was prepared in its clinical dose ratio whereas 20% Neusilin®US2 (NS) was added to prepare non-sticky, free flowing ternary COAM. Solubility studies of binary and ternary COAM exhibited sevenfold and tenfold rise in the solubility of NT...
March 13, 2019: AAPS PharmSciTech
Ajaz S Hussain, Vadim J Gurvich, Kenneth Morris
Facilitating utility of prior knowledge to accelerate evidence-based new drug development is a focus of several communities of knowledge, such as clinical pharmacology. For example, progress has been made via modeling and simulation of pharmacokinetic and pharmacodynamic relationships in the more effective use of "End of Phase 2" regulatory meetings for a New Drug Application (NDA). Facilitating utility of prior "Chemistry, Manufacturing, and Controls" (CMC) knowledge to accelerate new drug development and regulatory review process is also a topic of significant interest...
March 12, 2019: AAPS PharmSciTech
Maryam Maghsoodi, Ali Nokhodchi, Mahzad Azhdarzadeh Oskuei, Saman Heidari
Physiologically generated supersaturation and subsequent crystallization of a weakly basic drug in the small intestine leads to compromised bioavailability. In this study, the pH-induced crystallization of cinnarizine (CNZ) in the presence of different polymers was investigated. Inhibitory effect of Eudragit L100 (Eu) on crystallization of CNZ at varying supersaturation ratios was examined. The effect of Eu on the dissolution behavior of CNZ from CNZ/Eu physical mixtures (PMs) and solid dispersions (SDs) was assessed...
March 11, 2019: AAPS PharmSciTech
Ramy N Elsergany, Lai Wah Chan, Paul Wan Sia Heng
Coating of fine primary drug particles by a fluidized bed processor has been reported to be potentially challenging. This work aimed to develop a spray layering process to produce nonpareils by a side spray fluid bed with swirling air flow. The first part examined the effects of various parameters for producing lactose nonpareils by using Box-Behnken design. The factors considered were atomizing air pressure, spray rate, and fluidizing air temperature. This was followed by an in-depth investigation on the effects of inlet airflow rate, air temperature, and spray rate on properties of the product, in addition to process optimization...
March 11, 2019: AAPS PharmSciTech
Donglei Leng, Eric Ofosu Kissi, Korbinian Löbmann, Kaushik Thanki, Elias Fattal, Thomas Rades, Camilla Foged, Mingshi Yang
Corticosteroid resistance poses a major challenge to effective treatment of chronic obstructive pulmonary diseases. However, corticosteroid resistance can be overcome by co-administration of theophylline. The aim of this study was to formulate the corticosteroid budesonide with theophylline into inhalable dry powders intended for pulmonary combination therapy. Four types of spray-dried powders were prepared: (i) budesonide and theophylline co-dissolved and processed using a 2-fluid nozzle spray drier, (ii) budesonide nanocrystals and dissolved theophylline co-dispersed and processed using a 2-fluid nozzle spray drier, (iii) dissolved budesonide and dissolved theophylline processed using a 3-fluid nozzle spray drier, and (iv) budesonide nanocrystals and dissolved theophylline processed using a 3-fluid nozzle spray drier...
March 7, 2019: AAPS PharmSciTech
Janet Tan Sui Ling, Clive J Roberts, Nashiru Billa
Surface-modified nanostructured lipid carriers (NLC) represent a promising mode of drug delivery used to enhance retention of drugs at absorption site. Formulated chitosan-coated amphotericin-B-loaded NLC (ChiAmp NLC) had a size of 394.4 ± 6.4 nm, encapsulation and loading efficiencies of 86.0 ± 3% and 11.0 ± 0.1% respectively. Amphotericin-B release from NLCs was biphasic with no changes in physical properties upon exposure to simulated gastrointestinal conditions. Antifungal properties of Amphotericin-B and ChiAmpB NLC were comparable but ChiAmpB NLC was twice less toxic to red blood cells and ten times safer on HT-29 cell lines...
March 5, 2019: AAPS PharmSciTech
Ketan Patel, Ravi Doddapaneni, Manali Patki, Vasanthkumar Sekar, Arvind Bagde, Mandip Singh
Lung cancer patients develop acquired resistance to tyrosine kinase inhibitors including erlotinib (ERL) after few months of primary treatment. Evidently, new chemotherapy strategies to delay or overcome the resistance are urgently needed to improve the clinical outcome in non-small cell lung cancer (NSCLC) patients. In this paper, we have investigated the cytotoxic interaction of ERL and valproic acid (VA) in ERL-resistant NSCLC cells and developed a liquisolid formulation of ERL-VA for improving oral bioavailability of ERL...
March 4, 2019: AAPS PharmSciTech
Dina M Abdelnabi, Marwa H Abdallah, Hanaa A Elghamry
Nasal nanovesicular gels of buspirone hydrochloride (BH) were prepared and characterized aiming for sustained delivery and enhancing bioavailability. Buspirone hydrochloride has low bioavailability of about 4% after oral administration due to first pass metabolism. Buspirone hydrochloride nanovesicles were formulated by thin film hydration method (TFH). The selected nanovesicular formulation was incorporated into two types of in situ gels (pH-induced and thermoreversible) using carbopol 974P and poloxamer 407 (P407), respectively, together with different mucoadhesive polymers...
March 4, 2019: AAPS PharmSciTech
João Panão Costa, Sofia Carvalho, Sandra Jesus, Edna Soares, Ana Patrícia Marques, Olga Borges
Among non-viral vectors, the cationic polymer chitosan has gained attention as a gene delivery system. We hypothesized that the addition of casein into the nanoparticle's structure would facilitate a proper gene transfer. The work herein presented aimed to optimize the production method of chitosan-casein nanoparticles (ChiCas NPs) and to test their ability as a gene delivery system. ChiCas NPs formulation optimization was carried out by analyzing several characteristics such as NP size, zeta potential, and chitosan and casein incorporation efficacy...
February 28, 2019: AAPS PharmSciTech
Xuehua Yang, Ying Yang, Qingwen Jia, Yanyun Hao, Jingjing Liu, Guihua Huang
Irinotecan (IRT), the pro-drug of SN-38, has exhibited potent cytotoxicity against various tumors. In order to enhance the anti-tumor effect of IRT, we prepared IRT-loaded PLGA nanoparticles (IRT-PLGA-NPs) by emulsion-solvent evaporation method. Firstly, IRT-PLGA-NPs were characterized through drug loading (DL), entrapment efficiency (EE), particle size, zeta potential, transmission electron microscopy (TEM), and differential scanning calorimetry (DSC). We next studied the in vitro release characteristics of IRT-PLGA-NPs...
February 28, 2019: AAPS PharmSciTech
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