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Drug Development and Industrial Pharmacy

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https://www.readbyqxmd.com/read/28330377/enhanced-oral-bioavailability-and-sustained-delivery-of-glimepiride-via-niosomal-encapsulation-in-vitro-characterization-and-in-vivo-evaluation
#1
Amira Mohamed Mohsen, Mona Mahmoud AbouSamra, Shaimaa Ahmed ElShebiney
This study was designed to investigate the potency of niosomes, for glimepiride (GLM) encapsulation, aiming at enhancing its oral bioavailability and hypoglycemic efficacy. Niosomes containing non-ionic surfactants (NIS) were prepared by thin film hydration technique and characterized. In-vitro release study was performed using a dialysis technique. In-vivo pharmacodynamic studies, as well as pharmacokinetic evaluation were performed on alloxan induced diabetic rats. GLM niosomes exhibited high entrapment efficiency percentages (E...
March 23, 2017: Drug Development and Industrial Pharmacy
https://www.readbyqxmd.com/read/28323493/microparticles-containing-erlotinib-loaded-solid-lipid-nanoparticles-for-treatment-of-non-small-cell-lung-cancer
#2
Zahra Bakhtiary, Jaleh Barar, Ayuob Aghanejad, Amir Ata Saei, Elhameh Nemati, Jafar Ezzati Nazhad Dolatabadi, Yadollah Omidi
Non-small cell lung cancer (NSCLC) patients with sensitizing mutations in the exons 18-21 of the epithelial growth factor receptor (EGFR) geneshowincreased kinase activity of EGFR. Hence, tyrosine kinase inhibitors (TKIs) such as erlotinib (ETB) havecommonly been used as the second line therapeutic option in metastatic NSCLC. While the ETB is available as an oral dosage form, the local delivery of this TKI to the diseased cells of the lung may ameliorate its therapeutic impacts. In the current study, we report on the development of ETB-loaded solid lipid nanoparticle (SLN) based formulation of dry powder inhaler (ETB-SLN DPI)...
March 21, 2017: Drug Development and Industrial Pharmacy
https://www.readbyqxmd.com/read/28301952/correction-to-karimzadeh-mahmonir-rashidi-ladan-ganji-fariba-mesoporous-silica-nanoparticles-for-efficient-rivastigmine-hydrogen-tartrate-delivery-into-sy5y-cells
#3
(no author information available yet)
No abstract text is available yet for this article.
March 16, 2017: Drug Development and Industrial Pharmacy
https://www.readbyqxmd.com/read/28300426/soluplus%C3%A2-tpgs-mixed-micelles-for-dioscin-delivery-in-cancer-therapy
#4
Jing Zhao, Youwei Xv, Changyuan Wang, Yanfang Ding, Manyu Chen, Yifei Wang, Jinyong Peng, Lei Li, Li Lv
BACKGROUND: Dioscin has shown cytotoxicity against cancer cells, but its poor solubility and stability have limited its clinical application. In this study, we designed mixed micelles composed of TPGS and Soluplus(®) copolymers entrapping the poorly soluble anticancer drug dioscin. METHOD: In order to improve the aqueous solubility and bioactivity of dioscin, TPGS/Soluplus® mixed micelles with an optimal ratio were prepared using a thin-film hydration method, and their physicochemical properties were characterized...
March 16, 2017: Drug Development and Industrial Pharmacy
https://www.readbyqxmd.com/read/28279078/nano-carrier-mediated-co-delivery-of-methyl-prednisolone-and-minocycline-for-improved-post-traumatic-spinal-cord-injury-conditions-in-rats
#5
Xiao-Feng Wu, Zi-Hui Zhou
OBJECTIVE: To investigate the fate of albumin coupled nanoparticulate system over non-targeted drug carrier in the treatment of hemisectioned spinal cord injury (SCI). SIGNIFICANCE: Targeted delivery of methyl prednisolone (MP) and minocycline (MC) portrayed improved therapeutic efficacy as compared to non-targeted nanoparticles. METHODS: Albumin coupled, Chitosan stabilized, and cationic nanoparticles (albumin-MP + MC-NPS) of poly-(lactide-co-glycolic acid) were prepared using the emulsion solvent evaporation method...
March 10, 2017: Drug Development and Industrial Pharmacy
https://www.readbyqxmd.com/read/28276282/stability-of-pharmaceutical-salts-in-solid-oral-dosage-forms
#6
Haichen Nie, Stephen R Byrn, Qi Tony Zhou
Using pharmaceutical salts in solid dosage forms can raise stability concerns, especially salt dissociation which can adversely affect the product performance. Therefore, a thorough understanding of the salt instability encountered in solid state formulations is imperative to ensure the product quality. The present article uses the fundamental theory of acid base, ionic equilibrium, relationship of pH and solubility as a starting point to illustrate and interpret the salt formation and salt disproportionation in pharmaceutical systems...
March 9, 2017: Drug Development and Industrial Pharmacy
https://www.readbyqxmd.com/read/28276277/a-novel-design-for-stable-self-assembly-cubosome-precursor-microparticles-enhancing-dissolution-of-insoluble-drugs
#7
Liling Mei, Yecheng Xie, Hui Jing, Ying Huang, Jintian Chen, Hao Ran, Xin Pan, Chuanbin Wu
Cubosomes have been presented to enhance dissolution of insoluble drugs, but their applications are limited by the practical hurdles associated with both preparation and storage instability, resulting in drug delivery failure. In the present study, an innovative cubosome precursor-microparticles (CPMs) spray dried from an aqua-free precursor solution was developed to improve cubosome stability during both preparation and storage as well as to enhance the dissolution of insoluble drugs. These CPMs spontaneously self-assembled in situ forming homogeneous cubosome dispersion by hydration and disintegration after exposure to the aqueous medium...
March 9, 2017: Drug Development and Industrial Pharmacy
https://www.readbyqxmd.com/read/28274147/lipid-nanoparticles-of-zaleplon-for-improved-oral-delivery-by-box-behnken-design-optimization-in-vitro-and-in-vivoevaluation
#8
Narendar Dudhipala, Karthik Yadav Janga
PURPOSE: Zaleplon (ZL) is a hypnotic drug prescribed for the management of insomnia and convulsions. The oral bioavailability of ZL was low (∼30%) owing to poor water solubility and hepatic first-pass metabolism. The cornerstone of this investigation is to develop and optimize solid lipid nanoparticles (SLNs) of ZL with the aid of Box-Behnken design (BBD) to improve the oral bioavailability. METHODS: A design space with three formulation variables at three levels were evaluated in BBD...
March 9, 2017: Drug Development and Industrial Pharmacy
https://www.readbyqxmd.com/read/28274133/oral-bioavailability-enhancement-of-flubendazole-by-developing-nanofibrous-solid-dosage-forms
#9
Tamás Vigh, Balázs Démuth, Attila Balogh, Dorián L Galata, Ivo Van Assche, Claire Mackie, Monica Vialpando, Ben Van Hove, Petros Psathas, Enikő Borbás, Hajnalka Pataki, Peter Boeykens, György Marosi, Geert Verreck, Zsombor K Nagy
The bioavailability of the anthelminthic flubendazole was remarkably enhanced in comparison with the pure crystalline drug by developing completely amorphous electrospun nanofibres with a matrix consisting of hydroxypropyl-β-cyclodextrin and polyvinylpyrrolidone. The thus produced formulations can potentially be active against macrofilariae parasites causing tropical diseases, for example, river blindness and elephantiasis, which affect altogether more than a hundred million people worldwide. The bioavailability enhancement was based on the considerably improved dissolution...
March 8, 2017: Drug Development and Industrial Pharmacy
https://www.readbyqxmd.com/read/28271908/development-of-olmesartan-medoxomil-optimized-nanosuspension-using-box-behnken-design-to-improve-oral-bioavailability
#10
Nagaraj K, Narendar D, Kishan V
The aim of present investigation was to enhance the oral bioavailability of olmesartan medoxomil by improving its solubility and dissolution rate by preparing nanosuspension (OM-NS), using Box-Behnken design. In this, four factors were evaluated at three levels. Independent variables include: concentration of drug (X1), concentration of surfactant (X2), concentration of polymer (X3) and number of homogenization cycles (X4). Based on preliminary studies the size (Y1), zeta potential (Y2) and % drug release at 5min (Y3) were chosen as dependent responses...
March 8, 2017: Drug Development and Industrial Pharmacy
https://www.readbyqxmd.com/read/28270008/gene-delivery-to-the-lungs-pulmonary-gene-therapy-for-cystic-fibrosis
#11
Ilia Villate-Beitia, Jon Zarate, Gustavo Puras, José Luis Pedraz
Cystic fibrosis (CF) is a monogenic autosomal recessive disorder where the defective gene, the cystic fibrosis transmembrane conductance regulator (CFTR), is well identified. Moreover, the respiratory tract can be targeted through noninvasive aerosolized formulations for inhalation. Therefore, gene therapy is considered a plausible strategy to address this disease. Conventional gene therapy strategies rely on the addition of a correct copy of the CFTR gene into affected cells in order to restore the channel activity...
March 7, 2017: Drug Development and Industrial Pharmacy
https://www.readbyqxmd.com/read/28277845/topical-safety-and-vasoconstrictive-assay-based-bioequivalence-of-a-new-reformulated-mometasone-cream
#12
Rajesh Krishna, Ann Horowitz, Patrick Larson, James Bolognese, Eugene E Marcantonio
OBJECTIVES: A new improved mometasone furoate (Elocon) cream with an emulsification system that produces a stable emulsion has been developed. In order to register the product in various markets, it was essential to ensure the cream was topically well tolerated and that it was bioequivalent to the reference product. METHODS: Phase I clinical studies were performed to assess the local safety and tolerability upon multiple dosing of this new cream as well as to assess the single dose bioequivalence relative to the marketed product...
March 3, 2017: Drug Development and Industrial Pharmacy
https://www.readbyqxmd.com/read/28277844/effects-of-surface-charge-of-low-molecular-weight-heparin-modified-cationic-liposomes-on-drug-efficacy-and-toxicity
#13
Haohuan Li, Yi Chen, Yueyang Deng, Yue Wang, Xue Ke, Tianyuan Ci
Cationic liposome is a potential nanocarrier to deliver drugs to solid tumor with proven efficiency in targeting of tumor tissues. However, the major limitation is their charge-related instability and blood toxicity via intravenous injection. In order to overcome these problems and to maintain tumor targeting potency, we modified the cationic liposomes with low molecular weight heparin (LMWH) to obtain series of liposomes with different surface charges. Both in vitro and in vivo studies including serum stability, blood hemolysis, cellular uptake, cytotoxicity and in vivo biodistribution were evaluated...
March 3, 2017: Drug Development and Industrial Pharmacy
https://www.readbyqxmd.com/read/28277843/nanoethosomal-formulation-of-gammaoryzanol-for-skin-aging-protection-and-wrinkle-improvement-a-histopathological-study
#14
Saman Heydari, Saeed Ghanbarzadeh, Behzad Anoosh, Mohammad Reza Ranjkesh, Yousef Javadzadeh, Maryam Kouhsoltani, Hamed Hamishehkar
BACKGROUND: Free radical scavengers and antioxidants, with the main focus on enhanced targeting to the skin layers, can provide protection against skin ageing. OBJECTIVE: The aim of the present study was to prepare nanoethosomal formulation of Gammaoryzanol (GO), a water insoluble antioxidant, for its dermal delivery to prevent skin aging. METHODS: Nanoethosomal formulation was prepared by a modified ethanol injection method and characterized by using laser light scattering, scanning electronic microscope (SEM) and X-ray diffraction (XRD) techniques...
March 3, 2017: Drug Development and Industrial Pharmacy
https://www.readbyqxmd.com/read/28277846/study-of-a-novel-disintegrable-oleanolic-acid-polyvinylpolypyrrolidone-solid-dispersion
#15
Weiqin Wang, Changchang Cui, Mengying Li, Zhenhai Zhang, Huixia Lv
Novel solid dispersions of oleanolic acid-Polyvinylpolypyrrolidone (OLA-PVPP SDs) were designed and prepared to improve the apparent solubility of drug, as well as to improve the stability, fluidity and compressibility of SDs. Disintegrable OLA-PVPP SDs were then evaluated both in vitro and in vivo. DSC, XRD, IR and SEM analysis proved the formation of OLA-PVPP SD and its amorphous state. The results of fluidity study, moisture absorption test and stability test showed that OLA-PVPP SD with good fluidity and qualified stability was successfully obtained...
March 2, 2017: Drug Development and Industrial Pharmacy
https://www.readbyqxmd.com/read/28277848/kozeny-carman-permeability-relationship-with-disintegration-process-predicted-from-early-dissolution-profiles-of-immediate-release-tablets
#16
Parveen Kumari, Pooja Rathi, Virender Kumar, Jatin Lal, Harmeet Kaur, Jasbir Singh
This study was oriented towards the disintegration profiling of the diclofenac sodium (DS) immediate-release (IR) tablets and development of its relationship with medium permeability kperm based on Kozeny-Carman equation. Batches (L1-L9) of DS IR tablets with different porosities and specific surface area were prepared at different compression forces and evaluated for porosity, in vitro dissolution and particle-size analysis of the disintegrated mass. The kperm was calculated from porosities and specific surface area, and disintegration profiles were predicted from the dissolution profiles of IR tablets by stripping/residual method...
March 1, 2017: Drug Development and Industrial Pharmacy
https://www.readbyqxmd.com/read/28277847/development-of-electrosprayed-artesunate-loaded-core-shell-nanoparticles
#17
Hoang Nhan Ho, Ivo Laidmäe, Karin Kogermann, Andres Lust, Andres Meos, Chien Ngoc Nguyen, Jyrki Heinämäki
OBJECTIVE: Artesunate (ART) is proven to have potential anti-proliferative activities, but its instability and poor aqueous solubility limit its application as an anti-cancer drug. The present study was undertaken to develop coaxial electrospraying as a novel technique for fabricating nanoscale drug delivery systems of ART as the core-shell nanostructures. METHODS: The core-shell nanoparticles (NPs) were fabricated with coaxial electrospraying and the formation mechanisms of NPs were examined...
March 1, 2017: Drug Development and Industrial Pharmacy
https://www.readbyqxmd.com/read/28276785/a-critical-review-about-methodologies-for-the-analysis-of-mucoadhesive-properties-of-drug-delivery-systems
#18
Jéssica Bassi da Silva, Sabrina Barbosa de Souza Ferreira, Osvaldo de Freitas, Marcos Luciano Bruschi
Mucoadhesion is a useful strategy for drug delivery systems, such as tablets, patches, gels, liposomes, micro/nanoparticles, nanosuspensions, microemulsions and colloidal dispersions. Moreover, it has contributed to many benefits like increased residence time at application sites, drug protection, increased drug permeation and improved drug availability. In this context, investigation into the mucoadhesive properties of pharmaceutical dosage forms is fundamental, in order to characterize, understand and simulate the in vivo interaction between the formulation and the biological substrate, contributing to the development of new mucoadhesive systems with effectiveness, safety and quality...
March 1, 2017: Drug Development and Industrial Pharmacy
https://www.readbyqxmd.com/read/28276784/nanostructured-lipid-carriers-loaded-with-simvastatin-effect-of-peg-glycerides-on-characterization-stability-cellular-uptake-efficiency-and-in-vitro-cytotoxicity
#19
Sally Safwat, Rania A H Ishak, Rania M Hathout, Nahed D Mortada
OBJECTIVE: The aim of this study is to evaluate the use of PEG/glycerides of different HLB; oleoyl macrogol-6-glycerides (Labrafil(®) M 1944 CS) and caprylocaproylmacrogol-8-glycerides (Labrasol(®)), compared to Labrafac lipophile(®) as PEG-free glyceride in the preparation of nanostructured lipid carriers (NLCs). PEG/glycerides are suggested to perform a dual function; as the oily component, and as the PEG-containing substrate required for producing the PEGylated carriers without physical or chemical synthesis...
March 1, 2017: Drug Development and Industrial Pharmacy
https://www.readbyqxmd.com/read/28276783/application-of-cyclodextrins-in-antibody-microparticles-potentials-for-antibody-protection-in-spray-drying
#20
Vahid Ramezani, Alireza Vatanara, Mohammad Seyedabadi, Mohsen Nabi Meibodi, Hamed Fanaei
OBJECTIVES: Dry powder formulations are extensively used to improve the stability of antibodies. Spray drying is one of important methods for protein drying. This study investigated the effects of trehalose, hydroxypropyl beta cyclodextrin (HPBCD) and beta cyclodextrin (BCD) on the stability and particle properties of spray-dried IgG. METHODS: D-optimal design was employed for both experimental design and analysis and optimization of the variables. The size and aerodynamic behavior of particles were determined using laser light scattering and glass twin impinger, respectively...
March 1, 2017: Drug Development and Industrial Pharmacy
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