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Drug Development and Industrial Pharmacy

Silvana A Barea, Cristiane B Mattos, Ariadne C C Cruz, Vitor C Chaves, Rafael N Pereira, Claudia M O Simões, Jadel M Kratz, Letícia S Koester
Thalidomide (THD) is a BCS class II drug with renewed and growing therapeutic applicability. Along with the low aqueous solubility, additional poor biopharmaceutical properties of the drug, i.e. chemical instability, high crystallinity and polymorphism, lead to a slow and variable oral absorption. In this view, we developed solid dispersions (SDs) containing THD dispersed in different self-emulsifying carriers aiming at an enhanced absorption profile for the drug. THD was dispersed in lauroyl macrogol-32 glycerides (Gelucire® 44/14) and α-tocopherol polyethylene glycol succinate (Kolliphor® TPGS),in the presence or absence of the precipitation inhibitor polyvinylpyrrolidone K30 (PVP K30), by means of the solvent method...
December 5, 2016: Drug Development and Industrial Pharmacy
Hailong Zhang, Xiaoyan Huang, Yongjing Zhang, Yang Gao
CONTEXT: Oral bioavailability of some hydrophilic therapeutic macromolecules was very poor, thus leading to their limited application in clinic. OBJECTIVE: To investigate the efficacy, safety and mechanism of HP-β-CD-PEI polymers on the intestinal absorption of some poorly absorbable drugs in rats. METHODS: Effects of HP-β-CD-PEI polymers on the intestinal absorptions of drugs were investigated by an in situ closed loop method in rats. The safety of HP-β-CD-PEI polymer was evaluated by measurement of lactate dehydrogenase (LDH) activity and amount of protein released from rat intestinal perfusate...
December 5, 2016: Drug Development and Industrial Pharmacy
Simona Dimchevska, Nikola Geskovski, Gjorgji Petruševski, Marina Chacorovska, Riste Popeski-Dimovski, Sonja Ugarkovic, Katerina Goracinova
One of the most important problems in nanoencapsulation of extremely hydrophobic drugs is poor drug loading due to rapid drug crystallization outside the polymer core. The effort to use nanoprecipitation, as a simple one-step procedure with good reproducibility and FDA approved polymers like Poly(lactic-co-glycolic acid) (PLGA) and Polycaprolactone (PCL), will only potentiate this issue. Considering that drug loading is one of the key defining characteristics, in this study we attempted to examine whether the nanoparticle core composed of two hydrophobic polymers will provide increased drug loading for 7-Ethyl-10-hydroxy-camptothecin (SN-38), relative to nanoparticles prepared using individual polymers...
December 2, 2016: Drug Development and Industrial Pharmacy
Mohammed H Elkomy, Shahira F El Menshawe, Hussein M Eid, Ahmed M A Ali
This study investigates potentials of solid lipid nanoparticles (SLN) based gel for transdermal delivery of tenoxicam (TNX) and describes a pharmacokinetics-pharmacodynamics (PK-PD) modeling approach for predicting concentration-time profile in skin. A 2(3) factorial design was adopted to study the effect of formulation factors on SLN properties and determine the optimal formulation. SLN-gel tolerability was investigated using rabbit skin irritation test. Its anti-inflammatory activity was assessed by carrageenan induced rat paw edema test...
December 2, 2016: Drug Development and Industrial Pharmacy
Duangkamon Sakloetsakun, Thaned Pongjanyakul
The aims of this study were to determine the potential of gellan gum (GG) and halloysite (HS) dispersions at different mixing ratios and investigate the potential of GG-HS dispersions in film formation. To this end, the dispersions and films were characterized. The dispersions formed films with large particles ranging from 3-4 µm in size, with a zeta potential of approximately -35 mV. The GG-HS films were fabricated using a solvent-casting technique, which generated films with a white opaque appearance and rough surface...
November 30, 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 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...
November 25, 2016: Drug Development and Industrial Pharmacy
Benchawan Chamsai, Sontaya Limmatvapirat, Srisagul Sungthongjeen, Pornsak Sriamornsak
CONTEXT: Manidipine (MDP) is generally used clinically as an antihypertensive agent; however, the bioavailability of orally administered MDP is limited very low due to their very low water solubility. OBJECTIVE: The objectives of this research were, therefore, to increase the solubility of MDP by the formation of ternary solid dispersions (tSD) with polyethylene glycol 4000 (PEG4000) and copovidone and to improve their stability. METHODS: Solid ternary phase diagram was constructed to find homogeneous solid dispersion region after melting and solidifying at low temperature with different quenching substances...
November 22, 2016: Drug Development and Industrial Pharmacy
Kai Dong, Hefeng Zhang, Yan Yan, Jinyao Sun, Yalin Dong, Ke Wang, Lu Zhang, Xianpeng Shi, Jianfeng Xing
CONTEXT: Extensive or long-time use of corticosteroids often causes many toxic side-effects. The ion exchange resins and the coating material, Eudragit, can be used in combination to form a new oral delivery system to deliver corticosteroids. OBJECTIVES: The resin microcapsule (DRM) composed by Amberlite 717 and Eudragit S100 was used to target hydrocortisone (HC) to the colon in order to improve its treatment effect on ulcerative colitis (UC) and reduce its toxic side-effects...
November 21, 2016: Drug Development and Industrial Pharmacy
Frank A Chrzanowski, Kaleem Ahmad
Salts of linogliride with reduced solubilities were prepared and evaluated as potential candidates for extended-release oral dosage forms. A once-daily dose of 300-800 mg was intended. Seven acids were selected: p-acetamidobenzoic, benzoic, p-hydroxybenzoic, 3-hydroxy-2-naphthoic, 1-napsylic, pamoic, and p-toluenesulfonic acids but only four salts were able to be prepared in suitable quantities for evaluation: linogliride pamoate, p-hydroxybenzoate, 3-hydroxy-2-naphthoate, and 1-napsylate. The pH-solubility profiles of the four new salts, free base, and fumarate salt were compared over the pH 1...
November 21, 2016: Drug Development and Industrial Pharmacy
Diána Hegyesi, Markus Thommes, Peter Kleinebudde, Tamás Sovány, Péter Kása, András Kelemen, Klára Pintye-Hódi, Géza Regdon
In this study a multiparticulate matrix system was produced, containing two different APIs: enalapril-maleate and hydrochlorothiazide. The critical control points of the process were investigated by means of factorial design. Besides the generally used microcrystalline cellulose, ethylcellulose was used as matrix former to achieve modified drug release ensured by diffusion. The matrix pellets were made by extrusion-spheronization using a twin-screw extruder. Some pellet properties (aspect ratio, 10% interval fraction, hardness, deformation process) were determined...
November 14, 2016: Drug Development and Industrial Pharmacy
Ghareb M Soliman, Gihan Fetih, Ahmed M Abbas
OBJECTIVE: The objective of this study is to develop and characterize in situ thermosensitive gels for the vaginal administration of sildenafil as a potential treatment of endometrial thinning occurring as a result of using clomiphene citrate for ovulation induction in women with type II eugonadotrophic anovulation. While sildenafil has shown promising results in the treatment of infertility in women, the lack of vaginal pharmaceutical preparation and the side effects associated with oral sildenafil limit its clinical effectiveness...
November 14, 2016: Drug Development and Industrial Pharmacy
Jianghui Xu, Vikramjeet Singh, Xianzhen Yin, Parbeen Singh, Li Wu, Xiaonan Xu, Tao Guo, Lixin Sun, Shuangying Gui, Jiwen Zhang
β-artemether (ARM) is a widely used anti-malarial drug isolated from the Chinese antimalarial plant, Artemisia annua. The solvent effects on crystal habits and dissolution of ARM were thoroughly investigated and discussed herein. The ARM was recrystallized in nine different solvents of varied polarity, namely, methanol, ethanol, isopropanol, tetrahydrofuran, dichloromethane, trichloromethane, ethyl acetate, acetone and hexane by solvent evaporation method. The obtained crystals were morphologically characterized using scanning electron microscope (SEM)...
November 14, 2016: Drug Development and Industrial Pharmacy
Sunghoon Park, Dong-Hwan Kim, Yoon Kim, Jeong Hwa Park, MinSeok Lee, Im-Sook Song, Chang-Koo Shim
A 3-month depot formulation of leuprolide acetate (Luphere 3M Depot) with a mean microsphere diameter of 22.3 μm was prepared aseptically by spray drying glacial acetic acid solution of the drug and polylactic acid, and lyophilization in a D-mannitol solution. The encapsulation efficiency and loading content of the drug in the Luphere 3M Depot were 94.7 and 9.92% (w/w), respectively. The in vitro release of leuprolide from the depot was substantially delayed and the release profile was similar to that of Lucrin Depot (Abbott Korea, Korea)...
November 8, 2016: Drug Development and Industrial Pharmacy
Saipon Chanburee, Waree Tiyaboonchai
PURPOSE: To examine effects of polymer types on the mucoadhesive properties of polymer coated NLCs Experiment: Curcumin-loaded NLCs were prepared using a warm microemulsion technique followed by coating particle surface with mucoadhesive polymers; polyethylene glycol400 (PEG400), polyvinyl alcohol (PVA) and chitosan (CS). The physicochemical properties and entrapment efficacy were examined. In vitro mucoadhesive studies were assessed by wash-off test. In addition, the stability of mucoadhesive NLCs in gastrointestinal fluids and the pattern of drug release were also investigated...
November 3, 2016: Drug Development and Industrial Pharmacy
Muhammad Tahir Haseeb, Muhammad Ajaz Hussain, Sajid Bashir, Muhammad Umer Ashraf, Naveed Ahmad
CONTEXT: Advancement in technology has transformed the conventional dosage forms to intelligent drug delivery systems. Such systems are helpful for targeted and efficient drug delivery with minimum side effects. Drug release from these systems are governed and controlled by external stimuli (pH, enzymes, ions, glucose, etc.). Polymeric biomaterial having stimuli responsive properties has opened a new area in drug delivery approach. OBJECTIVE: Potential of a polysaccharide (rhamnogalacturonan) based hydrogel from Linseeds (Linum usitatissimum L...
November 3, 2016: Drug Development and Industrial Pharmacy
Marjan Motiei, Soheila Kashanian, Avat Arman Taherpour
OBJECTIVE: To develop a novel biocompatible amphiphilic drug delivery for hydrophobic drugs, chitosan (CS) was grafted to a series of hydrophobic amino acids including L-alanine (A), L-proline (P) and L-tryptophan (W) by carbodiimide mediated coupling reaction. MATERIALS AND METHODS: Chemical characteristics of the modified polymers were determined and confirmed by FT-IR, (1)H-NMR, and UV-vis spectroscopy and the degree of substitution was quantified by elemental analysis...
November 2, 2016: Drug Development and Industrial Pharmacy
Mohit Dwivedi, Vijay Sharma, Kamla Pathak
CONTEXT: Eosinophilic pustular folliculitis is a secondary symptom associated with HIV infection appears as levels of CD4 lymphocyte cells and T4 lymphocyte cell. Isotretinoin, an analog of vitamin A (retinoid) alters the DNA transcription mechanism and interferes in the process of DNA formation. It also inhibits the eosinophilic chemotactic factors present in sebaceous lipids and in the stratum corneum of patients suffering from this ailment. OBJECTIVE: The present research was aimed to formulate isotretenoin-loaded invasomal gel to deliver and target the drug to pilosebaceous follicular unit...
November 2, 2016: Drug Development and Industrial Pharmacy
Pouya Dehghankelishadi, Ebrahim Saadat, Fatemeh Ravar, Maliheh Safavi, Mahboobeh Pordeli, Mehdi Gholami, Farid A Dorkoosh
The aim of this study was to evaluate the in vitro and in vivo efficacy of Paclitaxel-Lapatinib loaded Pluronic micelles. Lapatinib and pluronic sensitize the cancerous cells to Paclitaxel via efflux pump inhibition. In addition, pluronic polymers can trigger intrinsic apoptosis pathways. Furthermore, micellar system can passively target the chemotherapeutic agents by enhanced permeability and retention effect. The paclitaxel-lapatinib loaded micelles were characterized in means of encapsulation efficacy and size...
October 31, 2016: Drug Development and Industrial Pharmacy
Ashkan K Yazdi, Hugh D C Smyth
OBJECTIVE: To optimize air-jet milling conditions of ibuprofen (IBU) using design of experiment (DoE) method, and to test the generalizability of the optimized conditions for the processing of another non-steroidal anti-inflammatory drug (NSAID). METHODS: Bulk IBU was micronized using an Aljet mill according to a circumscribed central composite (CCC) design with grinding and pushing nozzle pressures (GrindP, PushP) varying from 20 to 110 psi. Output variables included yield and particle diameters at the 50(th) and 90(th) percentile (D50, D90)...
October 28, 2016: Drug Development and Industrial Pharmacy
Snežana Marković, Janez Kerč, Matej Horvat
We are presenting a new approach of identifying sources of variability within a manufacturing process by NIR measurements of samples of intermediate material after each consecutive unit operation (interprocess NIR sampling technique). In addition we summarize the development of a multivariate statistical process control (MSPC) model for the production of enteric-coated pellet product of the proton-pump inhibitor class. By developing provisional NIR calibration models, the identification of critical process points yields comparable results to the established MSPC modeling procedure...
October 26, 2016: Drug Development and Industrial Pharmacy
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