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Drug Development and Industrial Pharmacy

Viridiana Gisela Llera-Rojas, L Alicia Del Real, Néstor Mendoza-Muñoz, Luz María Melgoza-Contreras, David Quintanar-Guerrero
Nanocapsules (NCs) are submicron-sized core shell systems which present important advantages such as improvement of drug efficacy and bioavailability, prevention of drug degradation, and provision of controlled-release delivery. The available methods for NC production require expensive recovery and purification steps which compromised the morphology of nanocapsules. Industrial applications of NCs have been avoided due to the aforementioned issues. In this study, we developed a new method based on a modified self automicroemulsifying drug delivery system (SMEDDS) for in situ NCs production within the gastrointestinal tract...
January 20, 2017: Drug Development and Industrial Pharmacy
Satish Kumar Bedada, Ramgopal Appani, Praveen Kumar Boga
BACKGROUND AND OBJECTIVE: Capsaicin is the main pungent principle present in chilli peppers has been found to possess P-glycoprotein (P-gp) inhibition activity in vitro, which may have the potential to modulate bioavailability of P-gp substrates. Therefore, purpose of the present study was to evaluate the effect of capsaicin on intestinal absorption and bioavailability of fexofenadine, a P-gp substrate in rats. METHODS: The mechanistic evaluation was determined by non-everted sac and intestinal perfusion studies to explore the intestinal absorption of fexofenadine...
January 19, 2017: Drug Development and Industrial Pharmacy
Emil Joseph, Ranendra N Saha
The present study focuses on the effect of material used for the preparation of nanoparticulate (NP) systems and surface modification on the pharmacokinetics and biodistribution of atypical antipsychotic, olanzapine (OLN). NP carriers of OLN were prepared from two different materials such as polymer (polycaprolactone) and solid lipid (Glyceryl monostearate). These systems were further surface modified with surfactant, Polysorbate 80 and studied for pharmacokinetics-biodistribution in Wistar rats using in-house developed bioanalytical methods...
January 18, 2017: Drug Development and Industrial Pharmacy
Michał Teżyk, Emilia Jakubowska, Kasylda Milczewska, Bartłomiej Milanowski, Adam Voelkel, Janina Lulek
OBJECTIVE: The aim of this article is to compare the gravitational powder blend loading method to the tablet press and manual loading in terms of their influence on tablets' critical quality attributes (CQA). SIGNIFICANCE: The results of the study can be of practical relevance to the pharmaceutical industry in the area of direct compression of low-dose formulations, which could be prone to content uniformity (CU) issues. METHODS: In the preliminary study, particle size distribution (PSD) and surface energy of raw materials were determined using laser diffraction method and inverse gas chromatography, respectively...
January 17, 2017: Drug Development and Industrial Pharmacy
Vidhi J Parekh, Namita D Desai, Mushtaque S Shaikh, Ujwala A Shinde
Meloxicam, a BCS class II drug belonging to the class of NSAIDs is indicated in conditions of rheumatoid arthritis, ankylosing spondylitis and osteoarthritis in which rapid onset of drug action is desired to reduce inflammation and pain. The objective of the study was to thus develop Self Nanoemulsifying Granules (SNEGs) of Meloxicam (MLX) for enhancement of solubility; and subsequently dissolution rate, thus aiming for a faster onset of action. Preliminary studies along with molecular modeling studies were carried out for selection of appropriate lipids, surfactants and cosurfactants for the development of MLX-loaded Self Nanoemulsifying preconcentrate (SNEP)...
January 17, 2017: Drug Development and Industrial Pharmacy
Brunella Parodi, Eleonora Russo, Sara Baldassari, Guendalina Zuccari, Sara Pastorino, Mengying Yan, Karthik Neduri, Gabriele Caviglioli
OBJECTIVE: The aim of this work was the development of mucoadhesive sublingual films, prepared using a casting method, for the administration of oxycodone. MATERIALS AND METHODS: A solvent casting method was employed to prepare the mucoadhesive films. A calibrated pipette was used to deposit single aliquots of different polymeric solutions on a polystyrene plate lid. Among the various tested polymers, hydroxypropylcellulose at low and medium molecular weight (HPC) and pectin at two different degrees of esterification (PC) were chosen for preparing solutions with good casting properties, capable of producing films suitable for mucosal application...
January 11, 2017: Drug Development and Industrial Pharmacy
Stavros N Politis, Dimitrios M Rekkas
A novel hot melt direct pelletization method was developed, characterized and optimized, using statistical thinking and experimental design tools. Mixtures of carnauba wax (CW) and HPMC K100M were spheronized using melted gelucire 50-13 as a binding material (BM). Experimentation was performed sequentially; a fractional factorial design was set up initially to screen the factors affecting the process, namely spray rate, quantity of BM, rotor speed, type of rotor disk, lubricant-glidant presence, additional spheronization time, powder feeding rate and quantity...
January 5, 2017: Drug Development and Industrial Pharmacy
Yanan Cui, Ping Cui, Binlong Chen, Suxin Li, Hua Guan
Monoclonal antibodies (mAbs) are extensively employed for disease diagnosis and treatment because of their high homogeneity and antigen specificity. In recent years, important outcomes have been achieved with mAbs due to their admirable therapeutic efficacy and relatively rare side effects. In clinical practice, several mAb products have been approved by regulatory entities, but their formulations have been highly specific given the complex structure and proteinaceous nature of mAbs. Thus, a great deal of attention has focused on formulations...
January 4, 2017: Drug Development and Industrial Pharmacy
Gladys Rosario Ramos Yacasi, Ana Cristina Calpena Capmany, María Antonia Egea Gras, Marta Espina García, María Luisa García López
CONTEXT: The stabilization of flurbiprofen loaded poly-Ɛ-caprolactone nanoparticles (FB-PƐCL-NPs) for ocular delivery under accurate freeze-drying (FD) process provide the basis for a large-scale production and its commercial development. OBJECTIVE: Optimization of the FD to improve long term stability of ocular administration's FB-PƐCL-NPs Methods: FB-PƐCL-NPs were prepared by solvent displacement method with poloxamer 188 (P188) as stabilizer. Freezing and primary dying (PD) were studied and optimized through freeze-thawing test and freeze-drying microscopy...
January 3, 2017: Drug Development and Industrial Pharmacy
Xuan Gao, Jun Zhang, Qiang Xu, Zun Huang, Yiyue Wang, Qi Shen
The goal of this research is to structure a hyaluronic acid modified nanostructured lipid carrier (HA-NLCs) for vincristine sulfate (VCR) delivery, and detect its efficiency to improve the oral bioavailability. Emulsion solvent evaporation method was used to prepare the HA-NLCs nanoparticles. The particle size, zeta potential and entrapment efficiency of VCR-NLCs and HA-NLCs were 187 ± 3.52 nm, -8.61 ± 1.29 mV, 33.12 ± 1.16% and 192 ± 4.41 nm, -32.82 ± 2.64 mV, 34.41 ± 2.21%, respectively. HA-NLCs could significantly improve the cellular uptake efficiency and cytotoxicity in MCF-7 cells than other VCR formulations...
January 3, 2017: Drug Development and Industrial Pharmacy
Mahmonir Karimzadeh, Ladan Rashidi, Fariba Ganji
Rivastigmine hydrogen tartrate (RT) is a molecule with both hydrophilic and hydrophobic properties used for the treatment of the Alzheimer's disease. In this work, the larger pore size of mesoporous silica nanoparticles (P1-MSN) was synthesized and then, P1-MSN were functionalized by succinic anhydride (S-P1-MSN) and 3-aminopropyltriethoxysilane (APTES) (AP-CO-P1-MSN) using the grafting and co-condensation methods, respectively. A new method was used for the functionalization of P1-MSN by succinic anhydride at room temperature...
January 3, 2017: Drug Development and Industrial Pharmacy
Mei Hu, Jinjie Zhang, Rui Ding, Yao Fu, Tao Gong, Zhirong Zhang
The clinical use of dabigatran etexilate (DABE) is limited by its poor absorption and relatively low bioavailability. Our study aimed to explore the potential of a mixed micelle system composed of Soluplus(®) and D-alpha tocopheryl polyethylene glycol 1000 succinate (TPGS) to improve the oral absorption and bioavailability of DBAE. DBAE was first encapsulated into Soluplus/TPGS mixed micelles by a simple thin film hydration method. The DBAE loaded micelles displayed an average size distribution of around 83...
December 29, 2016: Drug Development and Industrial Pharmacy
Naseem A Charoo, Rodrigo Cristofoletti, Sun K Kim
OBJECTIVE: Clinically relevant critical quality attributes (CQA's) were identified for the development of generic drug products containing fluconazole and potential design spaces relevant to the clinical application of the drug candidate was explored. SIGNIFICANCE: A simplified scoring system for the biopharmaceutics risk assessment roadmap (BioRAM) is proposed to guide product development. METHODS: Factorial design of experiments was employed to study the effect of formulation and process variables on CQA's...
December 29, 2016: Drug Development and Industrial Pharmacy
Francesca Sacchetti, Domenico D'Arca, Filippo Genovese, Salvatore Pacifico, Eleonora Maretti, Miriam Hanuskova, Valentina Iannuccelli, Maria Paola Costi, Eliana Leo
CONTEXT: LR-peptide, a novel hydrophilic peptide synthetized and characterized in previous work, is able to reduce the multi-drug resistance response in cisplatin (cDPP) resistant cancer cells by inhibiting human thymidylate synthase (hTS) overexpressed in several tumors, including ovarian and colon-rectal cancers, but it is unable to enter the cells spontaneously. OBJECTIVE: The aim of this work was to design and characterize liposomal vesicles as drug delivery systems for the LR peptide, evaluating the possible benefits of the pH-responsive feature in improving intracellular delivery...
December 26, 2016: Drug Development and Industrial Pharmacy
A J P van Heugten, M Versluijs-Helder, H Vromans
The Pharmacopoeia monograph for petrolatum poorly defines the materials physical properties. Indeed, differences between petrolatum grades can be substantial; yield stress varies between 65 and 280 Pa which can be compared to the consistency of respectively thin cream or thick ointment. This variation is not only due to differences in composition or refining process but also as a result of different processing; for example, thermal history influences petrolatum structure considerably. Slow cooling of petrolatum resulted in a yield stress of 26 Pa and fast cooling in 79 Pa...
December 23, 2016: Drug Development and Industrial Pharmacy
E Sawicki, J H M Schellens, J H Beijnen, B Nuijen
OBJECTIVE: A novel tablet formulation containing an amorphous solid dispersion (ASD) of elacridar hydrochloride was developed with the purpose to resolve the drug's low solubility in water and to conduct proof-of-concept clinical studies. SIGNIFICANCE: Elacridar is highly demanded for proof-of-concept clinical trials that study the drug's suitability to boost brain penetration and bioavailability of numerous anticancer agents. Previously, clinical trials with elacridar were performed with a tablet containing elacridar hydrochloride...
December 23, 2016: Drug Development and Industrial Pharmacy
Min Yang, Zhonghua Dong, Yongchun Zhang, Fang Zhang, Yongjie Wang, Zhongxi Zhao
Objectives Posaconazole (POS) is an antifungal compound which has a low oral bioavailability. The aim of this study was to prepare POS enteric microparticles to enhance its oral bioavailability. Methods POS enteric microparticles were prepared with hypromellose acetate succinate (HPMCAS) via the spray drying method. The solvent mixtures of acetone and ethanol used in the preparation of the microparticles were optimized to produce the ideal POS enteric microparticles. Multivariate data analysis using a principal component analysis was used to find the relationship among the HPMCAS molecular characteristics, particle properties and drug release kinetics from the spray dried microparticles...
December 22, 2016: Drug Development and Industrial Pharmacy
Dong Liu, Jing Xing, Fei Xiong, Fang Yang, Ning Gu
In order to improve the in vivo safety and specific delivery efficiency of the antileukemic homoharringtonine (HHT) at the targets, the long-circulating PEGylated liposomes loaded with HHT (LCLipo-HHT) were prepared. Their physical characteristics, in vitro drug release, in vivo pharmacokinetic properties and elementary toxicity were evaluated. The mean diameter of the prepared LCLipo-HHT is 75.6 ± 3.2 nm and the zeta potential is -16.9 ± 2.5 mV. The entrapment efficiency (EE) of HHT in the liposomes is 69...
December 22, 2016: Drug Development and Industrial Pharmacy
Mounika Nooli, Chella Naveen, Hitesh Kulhari, Nalini R Shastri, Ramakrishna Sistla
OBJECTIVE: Olmesartan medoxomil (OLM) is an antihypertensive drug with low oral bioavailability (28%) resulting from poor aqueous solubility, presystemic metabolism and P-glycoprotein (P-gp) mediated efflux. The present investigation studies the role of lipid nanocarriers in enhancing the OLM bioavailability through oral delivery. MATERIALS AND METHODS: Solid lipid nanoparticles were prepared by solvent emulsion-evaporation method. Statistical tools like regression analysis and Pareto charts were used to detect the important factors effecting the formulations...
December 22, 2016: Drug Development and Industrial Pharmacy
Vivek S Dave, Deepak Gupta, Monica Yu, Phuong Nguyen, Sheeba Varghese Gupta
The Biopharmaceutics Classification System (BCS) classifies pharmaceutical compounds based on their aqueous solubility and intestinal permeability. The BCS Class III compounds are hydrophilic molecules (high aqueous solubility) with low permeability across the biological membranes. While these compounds are pharmacologically effective, poor absorption due to low permeability becomes the rate-limiting step in achieving adequate bioavailability. Several approaches have been explored and utilized for improving the permeability profiles of these compounds...
December 20, 2016: Drug Development and Industrial Pharmacy
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