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Drug Development and Industrial Pharmacy

Sarwar Beg, Sumant Saini, Shantanu Bandopadhyay, O P Katare, Bhupinder Singh
PURPOSE: The current research work entails Quality by Design (QbD)-based systematic development of nanostructured lipid carriers (NLCs) of olmesartan medoxomil (OLM) with improved biopharmaceutical attributes. METHODS: Quality target product profile (QTPP) was defined and critical quality attributes (CQAs) were earmarked. Solubility of drug was performed in various lipids for screening of them. NLCs were prepared by hot-microemulsion method using solid lipids, liquid lipids and surfactants with maximal solubility...
October 19, 2017: Drug Development and Industrial Pharmacy
Jaleh Varshosaz, Somayeh Taymouri, Mohsen Minaiyan, Fatemeh Rastegarnasab, Azar Baradaran
The aim of this study was to develop hydroxypropyl methyl cellulose (HPMC)/chitosan gel containing polymeric micelles loaded with simvastatin (Sim) and evaluates its wound healing properties in rats. An irregular full factorial design was employed to evaluate the effects of various formulation variables including polymer/drug ratio, hydration temperature, hydration time and organic solvent type on the physicochemical characteristics of pluronic F127-cholesterol nanomicelles prepared using the film hydration method...
October 18, 2017: Drug Development and Industrial Pharmacy
Berrin Küçüktürkmen, Asuman Bozkır
The practical use of solid lipid nanoparticles (SLNs) in research has been highlighted in the literature, but few reports have combined SLNs with miRNA-based therapy and chemotherapy. We aimed to prepare cationic SLNs (cSLNs) to load anti-miR-21 oligonucleotide and pemetrexed for glioblastoma therapy in vitro. cSLNs were employed to encapsulate both pemetrexed and anti-miR-21 by a high pressure homogenization method, and then the properties of cSLNs were characterized. We studied cellular uptake and cytotoxicity properties of cSLNs in U87MG cells...
October 12, 2017: Drug Development and Industrial Pharmacy
Theodoros Avgerinos, Nikolaos Kantiranis, Athanasia Panagopoulou, Stavros Malamataris, Kyriakos Kachrimanis, Ioannis Nikolakakis
Objective/Significance: To elucidate the role of plasticizers in different mini matrices and correlate mechanical properties with drug release. METHODS: Cylindrical pellets were prepared by hot-melt extrusion (HME) and mini tablets by hot (HC) and ambient compression (AC). Venlafaxine HCl was the model drug, Eudragit® RSPO the matrix former and citric acid or Lutrol® F127 the plasticizers. The matrices were characterised for morphology, crystallinity and mechanical properties. The influence of plasticizer's type and content on the extrusion pressure (Pe) during HME and ejection during tableting was examined and the mechanical properties were correlated with drug release parameters...
October 12, 2017: Drug Development and Industrial Pharmacy
Seyed Hesamoddin Hashemi, Majid Montazer, Nasser Naghdi, Tayebeh Toliyat
This research study aimed to develop a novel sustained release formulation of alprazolam that can also be used for transdermal delivery. This was carried out, for the first time, through encapsulation of alprazolam in nanoliposomes using ethanol injection. In order to obtain the best formulation, four process variables, including the solvent/nonsolvent volume ratio, phospholipid concentration, alprazolam concentration, and cholesterol content were considered as key factors. Response surface methodology (RSM) and a central composite design (CCD) model were used to investigate the effect of these factors on vesicle size (VS) and encapsulation efficiency (EE) as the major properties of nanoliposomes...
October 12, 2017: Drug Development and Industrial Pharmacy
Jake Irvine, Afrina Afrose, Nazrul Islam
Ibuprofen, a non-steroidal anti-inflammatory drug (NSAID) is mostly administered orally and topically to relieve acute pain and fever. Due to its mode of action this drug may be useful in the treatment regimens of other, more chronic conditions, like cystic fibrosis. This drug is poorly soluble in aqueous media and thus the rate of dissolution from the currently available solid dosage forms is limited. This leads to poor bioavailability at high doses after oral administration, thereby increasing the risk of unwanted adverse effects...
October 12, 2017: Drug Development and Industrial Pharmacy
Lei Wu, Yujie Bi, Hongfei Wu
OBJECTIVE: The aim of this study was to optimize baicalin nanoemulsion, clarify the absorption mechanisms of nanoemulsion improving the exposure of baicalin, and assess the potential of employing nanoemulsion as nanosystem for insoluble drugs. SIGNIFICANCE: A novel nanoemulsion formulation was successfully prepared to enhance oral exposure of baicalin. METHODS: Pseudo-ternary phase diagrams were utilized to evaluate nanoemulsion area. Physicochemical properties of optimal nanoemulsion formulation were investigated...
October 12, 2017: Drug Development and Industrial Pharmacy
Qionghua Wei, Cornelia M Keck, Rainer H Müller
OBJECTIVE: To accelerate the determination of optimal spray drying parameters, a "Design of Experiment" (DoE) software was applied to produce well redispersible hesperidin nanocrystals. SIGNIFICANCE: For final solid dosage forms, aqueous liquid nanosuspensions need to be solidified, whereas spray drying is a large-scale cost-effective industrial process. METHODS: A nanosuspension with 18% (w/w) of hesperidin stabilized by 1% (w/w) of poloxamer 188 was produced by wet bead milling...
October 11, 2017: Drug Development and Industrial Pharmacy
José M León Blanco, Pedro L González-R, Carmen Martina Arroyo García, María José Cózar-Bernal, Marcos Calle Suárez, David Canca Ortiz, Antonio María Rabasco Álvarez, María Luisa González Rodríguez
This work was aimed at determining the feasibility of Artificial Neural Networks (ANN) by implementing backpropagation algorithms with default settings to generate better predictive models than multiple linear regression (MLR) analysis. The study was hypothesized on timolol-loaded liposomes. As tutorial data for ANN, causal factors were used, which were fed into the computer program. The number of training cycles has been identified in order to optimize the performance of the ANN. The optimization was performed by minimizing the error between the predicted and real response values in the training step...
October 2, 2017: Drug Development and Industrial Pharmacy
Huan Zhang, Weimei Wang, Haoran Li, Yi Peng, Zhiqing Zhang
Insulin-loaded microspheres were prepared by alternating deposition film layers that were composed of insulin and poly(vinyl sulfate) potassium (PVSK) on the surface of poly(lactic acid) (PLA) microspheres. The preparation of the insulin-loaded microspheres was optimized by an orthogonal test design, and the relationship between drug loading (DL) and film layers was studied. The particle size, DL and encapsulation efficiency (EE) of the obtained insulin-loaded microspheres with ten films were 5.25±0.15 µm, 111...
September 28, 2017: Drug Development and Industrial Pharmacy
Abeer S Hassan, Ghareb M Soliman, Marwa F Ali, Mona M El-Mahdy, Gamal El-Din A El-Gindy
OBJECTIVE: To develop mucoadhesive tablets for the vaginal delivery of progesterone (P4) to overcome its low oral bioavailability resulting from drug hydrophobicity and extensive hepatic metabolism. METHODS: The tablets were prepared using mixtures of P4/Pluronic® F-127 solid dispersion and different mucoadhesive polymers. The tablets were evaluated for physical properties, swelling index, mucoadhesive properties and drug release kinetics. P4 pharmacokinetic and pharmacodynamic properties were evaluated in female rabbits and compared with vaginal micronized P4 tablets and intramuscular (IM) P4 injection, respectively...
September 28, 2017: Drug Development and Industrial Pharmacy
Xinyi Gao, Pooja Bakshi, Sindhu Sunkara Ganti, Mahima Manian, Andrew Korey, William Fowler, Ajay K Banga
CONTEXT: The improper disposal of unused prescription opioids has a potential for abuse as well as environmental contamination. Consequently, there is an imperative need for an environmentally safe, convenient and effective drug disposal system. OBJECTIVE: To analyze the deactivation efficiency of the disposal system employing four model opioid drugs of high abuse potential. METHODS: The deactivation system used in this investigation is an activated granular carbon based disposal system in the form of a pouch, which can be used to safely and effectively deactivate unused or expired medications...
September 28, 2017: Drug Development and Industrial Pharmacy
Kai Chen, Haoyang Wen, Feifei Yang, Yibin Yu, Xiumei Gai, Haiying Wang, Pingfei Li, Weisan Pan, Xinggang Yang
Dipyridamole (DIP), having a short biological half-life, has a narrow absorption window and is primarily absorbed in the stomach. So, the purpose of this study was to prepare controlled-release floating (CRF) tablets of Dipyridamole by the dry coated method. The influence of agents with different viscosity, Hydroxypropylmethylcellulose (HPMC) and Polyvinylpyrollidon K30 (PVP K30) in the core tablet and low viscosity HPMC and PVP K30 in the coating layer on drug release, were investigated. Then a study with a three-factor, three-level orthogonal experimental design was used to optimize the formulation of the CRF tablets...
September 28, 2017: Drug Development and Industrial Pharmacy
Mahmoud H Teaima, Sally A Abdelhalim, Mohamed A El-Nabarawi, Dalia A Attia, Doaa A Helal
Cellulite is a common topographical alteration where skin acquires an orange peel or mattress appearance with alterations in adipose tissue and microcirculation. This work aims to develop and evaluate a topical niosomal gel formulae with good permeation to reach the subcutaneous fat layer. Several caffeine niosomal dispersions were prepared and incorporated into gel formulae using Carbopol 940 polymer, chemical penetration enhancers and iontophoresis, then the prepared gels were applied onto the skin of rats and anticellulite activity of caffeine from the prepared gels compared to that of the commercial product Cellu Destock® was evaluated by histological study of the skin and measurement of plasma level of caffeine passing through the skin using liquid chromatography (LC/MS-MS)...
September 28, 2017: Drug Development and Industrial Pharmacy
Atefeh Ebrahimi, Komail Sadrjavadi, Marziyeh Hajialyani, Yalda Shokoohinia, Ali Fattahi
The principal objective of the present study is to achieve a depot formulation of Risperidone by gelation of silk fibroin (SF). For this purpose, hydrochloric acid (HCl)/acetone based and methanol based hydrogels were prepared with different drug/polymer ratios (1:3, 1:6 and 1:15). For all the drug-loaded methanol based hydrogels, gel transition of SF solutions occurred immediately and gelation time was 1 min, while the gelation time of HCL/acetone based hydrogels was around 360 min. From Fourier transform infrared spectroscopy (FT-IR), and X-ray diffraction (XRD) spectra, solvent systems, and Risperidone could induce β-sheet structure, but HCL/acetone system had the lowest effect on induction of β-sheets...
September 28, 2017: Drug Development and Industrial Pharmacy
Giovanna Bruni, Vittorio Berbenni, Lauretta Maggi, Piercarlo Mustarelli, Valeria Friuli, Chiara Ferrara, Francesca Pardi, Federica Castagna, Alessandro Girella, Chiara Milanese, Amedeo Marini
OBJECTIVE: To improve the pharmaceutical behaviour of the oral antidiabetic agent gliclazide through the synthesis of multicomponent crystals with tromethamine. METHODS: Multicomponent crystals were prepared by solvent evaporation method, kneading and combining mechanical and thermal activation. DSC, FT-IR spectroscopy, X-ray diffraction, SEM-EDS and SSNMR were used to investigate their formation. Measurements of solubility and dissolution rate were carried out for the pharmaceutical characterization...
September 28, 2017: Drug Development and Industrial Pharmacy
Tao Liu, Rainer H Müller, Jan P Möschwitzer
Objective Drug nanosuspension is one of the established methods to improve the bioavailability of poorly soluble drugs. Drug physical properties aspect (morphology, solid state, starting size et al) is a critical parameter determining the production efficiency. Some drug modification approaches such as spray-drying were proved to improve the millability of drug powders. However, the mechanism behind those improved performances is unclear. This study is to systematically investigate the influence of those physical properties...
September 28, 2017: Drug Development and Industrial Pharmacy
Elham Masoudipour, Soheila Kashanian, Nasim Maleki, Ali Karamyan, Kobra Omidfar
OBJECTIVE: This study was performed to investigate a novel pH-responsive nanocarrier based on modified nano graphene oxide (nGO) to promote the acid-triggered intracellular release of a poorly soluble drug, FTY720. METHODS: To synthesize a drug conjugated to modified nGO, firstly the polyethylene glycol (PEG) was conjugated to nGO, then the produced PEG-nGO was functionalized with the anticancer drug, FTY720, through amide bonding. It was characterized by the scanning electron microscopy (SEM), the atomic force microscopy (AFM), the Fourier transform infrared (FTIR) spectroscopy and the UV-vis spectroscopy...
September 28, 2017: Drug Development and Industrial Pharmacy
Marianne Lilletvedt Tovsen, Ingunn Tho, Hanne Hjorth Tønnesen
Meso-tetraphenyl chlorin disulphonate (TPCS2a) is a photosensitizer (PS) particularly developed and patented for use in the technology of photochemical internalization (PCI) against cancer. TPCS2a is known to aggregate in aqueous media even at low concentrations (≥ 0.1 µM) and to form a high viscosity network at clinically relevant concentrations (mM). The aim of this work was to evaluate the effect of two hydroxypropylated cyclodextrin derivatives of beta and gamma type, respectively i.e., HPβCD and HPγCD, on the aggregation and solubilization of TPCS2a in isotonic solutions...
September 28, 2017: Drug Development and Industrial Pharmacy
Amira Motawea, Thanaa Borg, Abd El-Gawad H Abd El-Gawad
Phenytoin (PHT) is an antiepileptic drug that was reported to exhibit high wound healing activity. Nevertheless, its limited solubility, bioavailability, and inefficient distribution during topical administration limit its use. Therefore, this study aims to develop, characterize nanostructured lipid carriers (NLCs) and evaluate their potential in topical delivery of PHT to improve the drug entrapment efficiency and sustained release. The NLCs were prepared by hot homogenization followed by ultrasonication method using 2(3) factorial design...
September 28, 2017: Drug Development and Industrial Pharmacy
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