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Drug Development and Industrial Pharmacy

Ibrahim El-Sherbiny, Islam Khalil, Isra Ali, Magdi Yacoub
Smart materials are those materials that are responsive to chemical (organic molecules, chemical agents or specific agents), biochemical (protein, enzymes, growth factors, substrates or ligands), physical (electric field, magnetic field, temperature, pH, ionic strength or radiation) or mechanical (pressure or mechanical stress) signals. These responsive materials interact with the stimuli by changing their properties or conformational structures in a predictable manner. Recently, smart polymers have been utilized in various biomedical applications...
June 21, 2017: Drug Development and Industrial Pharmacy
Paul M Young, Daniela Traini, Hui Xin Ong, Angelo Granieri, Bing Zhu, Santo Scalia, Jie Song, Patrick T Spicer
PURPOSE: Thickening polymers have been used as excipients in nasal formulations to avoid nasal run-off (nasal drip) post-administration. However, increasing the viscosity of the formulation can have a negative impact on the quality of the aerosols generated. Therefore, the study aims to investigate the use of a novel smart nano-cellulose excipient to generate suitable droplets for nasal drug delivery that simultaneously has only marginally increased viscosity while still reducing nasal drips...
June 21, 2017: Drug Development and Industrial Pharmacy
Ian Soulairol, Mohammad Chaheen, Nicolas Tarlier, Adrien Aubert, Bernard Bataille, Tahmer Sharkawi
OBJECTIVE: This work evaluates the functionalities of different superdisintegrants (SD) for manufacturing orodispersible mini tablets (ODMT) by direct compression. METHODS: Twenty-three formulations varying in SD type, concentration, and lubricant were used to manufacture ODMT. The ODMT were then characterized for the following properties: friability, porosity, tensile strength, in vivo and in vitro disintegration time (DT). RESULTS: The results show that the presence, type, and concentration of SD did not influence friability, porosity, or tablet tensile strength...
June 21, 2017: Drug Development and Industrial Pharmacy
Joana Marto, Cecilia Sangalli, Priscilla Capra, Paola Perugini, Andreia Ascenso, Lídia Gonçalves, Helena Ribeiro
N-Acetyl-d-glucosamine (NAG) has been recently considered for topical treatment of hyperpigmentation disorders due to its inhibitory effect on thyrosinase enzymes in melanocytes. NAG is a precursor of hyaluronic acid, increasing its amount in skin, and consequently, preserving the skin hydration and elasticity. It may also act as an emulsion stabilizer. Solid lipid nanoparticles (SLN) are advanced delivery systems successfully used in pharmaceutical and cosmetic formulations for the improvement of active molecules penetration into the skin...
June 21, 2017: Drug Development and Industrial Pharmacy
Mohamed A Safwat, Ghareb M Soliman, Douaa Sayed, Mohamed A Attia
OBJECTIVE: To enhance 5-fluorouracil (5-FU) permeability through the skin by loading onto gold nanoparticles (GNPs) capped with two cationic ligands, benzalkonium chloride (BC) or poly (ethylene imine) (PEI). Whereas 5-FU has excellent efficacy against many cancers, its poor permeability through biological membranes and several adverse effects limit its clinical benefits. BC and PEI were selected to stabilize GNPs and to load 5-FU through ionic interactions. METHODS: 5-FU/BC-GNPs and 5-FU/PEI-GNPs were prepared at different 5-FU/ligand molar ratios and different pH values and were evaluated using different techniques...
June 21, 2017: Drug Development and Industrial Pharmacy
Rutthapol Sritharadol, Titpawan Nakpheng, Paul Wan Sia Heng, Teerapol Srichana
OBJECTIVE: The aim of this study was to develop mupirocin topical spray using Eudragit E100 as a film-forming agent for the treatment of bacterial skin infections as well as to promote wound healing. MATERIALS AND METHODS: Twenty-seven of mupirocin formulations were formulated containing Eudragit E100 and other excipients. Mupirocin spray was prepared by aerosol crimping and filling machine using HFA-134a as a propellant. The formulations were evaluated for their stability and physicochemical properties...
June 18, 2017: Drug Development and Industrial Pharmacy
Chang Xing, Jin-Feng Xing, Zhi-Qiang Ge
α-Chymotrypsin (α-CT) and trypsin are important components of the enzymatic barrier. They could degrade the therapeutic proteins and peptides, inhibit their activity consequently, and thereby reduce their oral bioavailability. Acidic agents, as one type of indirect protease inhibitors, have shown proof of concept in clinical trials. We report here the inactivated proteases due to acid influence can be reactivated immediately by environmental pH recovery regardless of how long the inactivation last. To keep the inactivation time of proteases for 4-5 h, we designed and prepared a sustained-release tablet containing citric acid (CA) which can effectively reduce the pH below 5...
June 8, 2017: Drug Development and Industrial Pharmacy
Ožbej Zupančič, Julia Rohrer, Hung Thanh Lam, Julia Anita Grießinger, Andreas Bernkop-Schnürch
AIM: In this study SEDDS for oral delivery of opioid peptide dalargin were developed and characterized in vitro. METHODS: Dalargin lipophilicity was increased by O-esterification of tyrosine OH group, hydrophobic ion pairing or a combination thereof. Distribution coefficients (log D) of lipidized dalargin derivatives were determined. Then, dalargin was incorporated in chosen SEDDS, namely SEDDS-1, composed of 50% Capmul 907, 40% Cremophor EL and 10% propylene glycol and comparatively more lipophilic SEDDS-2 composed of 30% Captex 8000, 30% Capmul MCM, 30% Cremophor EL and 10% propylene glycol...
June 7, 2017: Drug Development and Industrial Pharmacy
Yan Zhou, Shiqing Liu, Jianghua Ming, Yaming Li, Ming Deng, Bin He
The low bioavailability and short biological half-life of berberine chloride (BBR) negatively affect the protective role of this compound against osteoarthritis (OA). The present study was performed to evaluate the effectiveness of sustained BBR release system. Novel BBR-loaded chitosan microspheres (BBR-loaded CMs) were successfully synthesized using an ionic cross-linking method for sustained release. The basic characteristics of the prepared microspheres were subsequently evaluated by scanning electron microscopy (SEM), fourier transform infrared spectroscopy (FT-IR), X-ray diffraction (XRD) techniques, encapsulation efficiency (EE), and in vitro release experiments...
June 6, 2017: Drug Development and Industrial Pharmacy
Shaozhi Zhang, Jiwei Liu, Baojian Ge, Meiling Du, Li Fu, Yushan Fu, Qiu Yan
OBJECTIVE: The objective of this study is to investigate the encapsulation of 20(R)-ginsenoside Rg3 (20(R)-Rg3) using PLGA and promotion for its antitumor activity. SIGNIFICANCE: Preparation and evaluation of the antitumor efficacy of 20(R)-Rg3-loaded PLGA nanoparticles were the first reported. The data will be helpful to apply 20(R)-Rg3 efficiently and broadly in new drug form development and clinical cancer treatment. METHODS: The nanoparticles were prepared using emulsion and solvent evaporation methods...
June 5, 2017: Drug Development and Industrial Pharmacy
Braj Gaurav Sharma, Kushagra Khanna, Neeraj Kumar, Dhruv K Nishad, Mitra Basu, Aseem Bhatnagar
Calcium chloride is an essential calcium channel agonist which plays an important role in the contraction of muscles by triggering calcium channel. First time hypothesized about its role in the treatment of GER (gastro-oesophageal reflux) and vomiting disorder due to its local action. There are two objectives covered in the present study as first, the development & optimization of floating formulation of calcium chloride and another objective was to evaluated optimized formulation through gamma scintigraphy in human subjects...
June 5, 2017: Drug Development and Industrial Pharmacy
Saurabh Sarkar, Bruna Minatovicz, Kyrre Thalberg, Bodhisattwa Chaudhuri
Pulmonary delivery of cohesive and micronized drugs through Dry Powder Inhalers (DPIs) is traditionally achieved through the formation of ordered mixtures. In order to improve the mechanistic understanding of formation of ordered mixtures, the system consisting of micronized lactose (AZFL, representative of an active pharmaceutical ingredient) and a coarse particle carrier (LH100) is investigated as a function of different process and material variables in a high shear mixer (HSM) and in a low shear double cone (DCN) blender, using both experimental and numerical methods...
June 2, 2017: Drug Development and Industrial Pharmacy
Mayuri Ahirrao, Shilpa Shrotriya
The aim of this study was to enhance the delivery of resveratrol to the brain through the transnasal route by cubosomes. Cubosomes were prepared using glycerol monooleate and Lutrol F127 by probe sonication method. A 3(2) full factorial design was used for optimization of cubosomes and batch containing 4% w/v glycerol monooleate and 1.5% w/v of Lutrol F 127 was optimized. The selected cubosomal batch was cubical in shape, having mean particle size 161.5±0.12 nm. Entrapment efficiency was found to be 83.08% with zeta potential of - 20...
June 2, 2017: Drug Development and Industrial Pharmacy
Kyung Mi Yang, In Chul Shin, Joo Won Park, Kab-Sig Kim, Dae Kyong Kim, Kyungmoon Park, Kunhong Kim
OBJECTIVES: Nanoparticulation using fat and supercritical fluid (NUFS(TM)) is a drug delivery platform technology enabling efficient and effective formulation of poorly soluble drugs. We performed experiments to examine whether NUFS™ could improve poor bioavailability and reduce fed-fasted bioavailability variances of erlotinib (Ert). METHODS: NUFS-Ert was prepared using NUFS™ technology; its physical properties were characterized, and drug release was measured...
May 30, 2017: Drug Development and Industrial Pharmacy
Natália Noronha Ferreira, Taciane Alvarenga Perez, Liliane Neves Pedreiro, Fabíola Garavello Prezotti, Fernanda Isadora Boni, Valéria Maria de Oliveira Cardoso, Tiago Venâncio, Maria Palmira Daflon Gremião
This work aimed to develop a calcium alginate hydrogel as a pH responsive delivery system for polymyxin B (PMX) sustained-release through the vaginal route. Two samples of sodium alginate from different suppliers were characterized. The molecular weight and M/G ratio determined were, approximately, 107 KDa and 1.93 for alginate_S and 32 KDa and 1.36 for alginate_V. Polymer rheological investigations were further performed through the preparation of hydrogels. Alginate_V was selected for subsequent incorporation of PMX due to the acquisition of pseudoplastic viscous system able to acquiring a differential structure in simulated vaginal microenvironment (pH 4...
May 25, 2017: Drug Development and Industrial Pharmacy
Leonie Wagner-Hattler, Joachim Schoelkopf, Jörg Huwyler, Maxim Puchkov
A new mineral-polymer composite (FCC-PCL) performance was assessed to produce complex geometries to aid in development of controlled release tablet formulations. The mechanical characteristics of a developed material such as compactibility, compressibility and elastoplastic deformation were measured. The results and comparative analysis versus other common excipients suggest efficient formation of a complex, stable and impermeable geometries for constrained drug release modifications under compression. The performance of the proposed composite material has been tested by compacting it into a geometrically altered tablet (Tablet-In-Cup, TIC) and the drug release was compared to commercially available product...
May 23, 2017: Drug Development and Industrial Pharmacy
Michał Teżyk, Emilia Jakubowska, Bartłomiej Milanowski, Janina Lulek
The aim of this study was to optimize the process of tablets compression and identification of film-coating critical process parameters (CPPs) affecting critical quality attributes (CQAs) using quality by design (QbD) approach. Design of experiment (DOE) and regression methods were employed to investigate hardness, disintegration time, and thickness of uncoated tablets depending on slugging and tableting compression force (CPPs). Plackett-Burman experimental design was applied to identify critical coating process parameters among selected ones that is: drying and preheating time, atomization air pressure, spray rate, air volume, inlet air temperature, and drum pressure that may influence the hardness and disintegration time of coated tablets...
May 23, 2017: Drug Development and Industrial Pharmacy
Anish Babu, Anupama Munshi, Rajagopal Ramesh
RNA interference (RNAi) is emerging as a powerful approach in cancer treatment. siRNA is an important RNAi tool that can be designed to specifically silence the expression of genes involved in drug resistance and chemotherapeutic inactivity. Combining siRNA and other therapeutic agents can overcome the multidrug resistance (MDR) phenomenon by simultaneously silencing genes and enhancing chemotherapeutic activity. Moreover, the therapeutic efficiency of anticancer drugs can be significantly improved by additive or synergistic effects induced by siRNA and combined therapies...
May 19, 2017: Drug Development and Industrial Pharmacy
Shiva Golmohammadzadeh, Nafiseh Farhadian, Amir Biriaee, Faranak Dehghani, Bahman Khameneh
Raloxifene hydrochloride (RLX) is a selective estrogen receptor modulator which is orally used for treatment of osteoporosis and prevention of breast cancer. The drug has low aqueous solubility and bioavailability. The aim of the present study is to formulate and characterize oil-in-water microemulsion systems for oral delivery of RLX. To enhance the drug aqueous solubility, microemulsion based on sesame oil was prepared. Sesame oil and Tween 80 were selected as the drug solvent oil and surfactant, respectively...
May 19, 2017: Drug Development and Industrial Pharmacy
Xin Jin, Sajid Asghar, Xieting Zhu, Zhipeng Chen, Junhong Liu, Yibo Li, Hongying Li, Qineng Ping, Yanyu Xiao
The article describes the preparation, physicochemical characterization, drug release, and in vivo behavior of 10-hydroxycamptothecin-loaded poly (n-butyl cyanoacrylate) (PBCA) nanospheres (HCPT-PBCA-NSs). HCPT-PBCA-NSs were successfully prepared via emulsion polymerization of n-butyl cyanoacrylate (BCA) monomer in acidic medium with the aid of two colloidal stabilizers (Poloxamer 188 and Dextran 70). The influence of pH, the time of polymerization, and the dosage of the drug on particle size and encapsulation efficiency (EE) were studied...
May 19, 2017: Drug Development and Industrial Pharmacy
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