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International Journal of Pharmaceutics

Arianna Fallacara, Laura Busato, Michele Pozzoli, Maliheh Ghadiri, Hui Xin Ong, Paul M Young, Stefano Manfredini, Daniela Traini
An innovative lyophilized dry powder formulation consisting of urea-crosslinked hyaluronic acid (HA-CL) and sodium ascorbyl phosphate (SAP) -LYO HA-CL - SAP- was prepared and characterized in vitro for physico-chemical and biological properties. The aim was to understand if LYO HA-CL - SAP could be used as adjuvant treatment for nasal inflammatory diseases. LYO HA-CL - SAP was suitable for nasal delivery and showed to be not toxic on human nasal septum carcinoma-derived cells (RPMI 2650 cells) at the investigated concentrations...
January 16, 2019: International Journal of Pharmaceutics
Evert Fuenmayor, Martin Forde, Andrew V Healy, Declan M Devine, John G Lyons, Christopher McConville, Ian Major
Oral tablets are a convenient form to deliver active pharmaceutical ingredients (API) and have a high level of acceptance from clinicians and patients. There is a wide range of excipients available for the fabrication of tablets thereby offering a versatile platform for the delivery of therapeutic agents to the gastrointestinal tract. However, the geometry of tablets is limited by conventional manufacturing processes. This study aimed to compare three manufacturing processes in the production of flat-faced oral tablets using the same formulation composed of a polymer blend and caffeine as a model drug: fused-filament fabrication (FFF), direct compression (DC) and injection molding (IM)...
January 16, 2019: International Journal of Pharmaceutics
Ala' Salem, Sándor Nagy, Szilárd Pál, Aleksandar Széchenyi
Pharmaceutical co-crystals present an opportunity to improve the solubility of conventional active pharmaceutical ingredients (APIs). Despite advances in co-crystal screening, the rational design of even the chemically simplest co-crystals remains challenging. Hansen solubility parameters (HSPs) have previously been used as a tool to predict co-crystal formation using only the chemical structure. The aim of this study was to validate the use of HSPs as a tool to predict co-crystal formation, analyse its limitations and examine the previously set Δδ inclusion cut-off value...
January 14, 2019: International Journal of Pharmaceutics
Jean-Pierre Gomez, Guillaume Tresset, Chantal Pichon, Patrick Midoux
Linear Polyethylenimine (lPEI) is an efficient cationic polymer for transfecting cells, both in vitro and in vivo, but poses concerns regarding cytotoxicity. Histidinylated lPEI (His-lPEI) exhibits also high transfection efficiency but lower cytotoxicity than lPEI. For the first time, we tested polyfection efficiency of polyplexes comprising both lPEI and His-lPEI. A series of pDNA polyplexes was prepared with mixtures of lPEI and His-lPEI and the amount of each polymer within His-lPEI/lPEI polyplexes was determined by flow cytometry...
January 14, 2019: International Journal of Pharmaceutics
Huangliang Zheng, Jiaqi Li, Mengjing Wang, Xiang Luo, Qiujun Qiu, Ling Hu, Cong Li, Yanzhi Song, Yihui Deng
To overstep the dilemma of chemical drug degradation within powerful lysosomes of tumor associated macrophages (TAMs), a sialic acid-polyethylenimine-cholesterol (SA-PEI-CH) modified liposomal doxorubicin (DOX-SPCL) was designed with both TAMs targeting and smart lysosomal trafficking. The modified liposome DOX-SPCL performed particle size as 103.2 ± 3.1 nm and zeta potential as -4.5 ± 0.9 mV with encapsulation efficiency as 95.8 ± 0.5%. In in vitro cell experiments, compared with conventional liposomal doxorubicin (DOX-CL) and PEGylated liposomal doxorubicin (DOX-PL), DOX-SPCL showed a selective binding on TAMs and a mere lysosomal concentration...
January 14, 2019: International Journal of Pharmaceutics
Masaaki Imono, Hiromasa Uchiyama, Hiroshi Ueda, Kazunori Kadota, Yuichi Tozuka
One of the most difficult challenges in developing nanocrystal formulations is to determine the dissolution behavior of nanocrystal suspensions (nanosuspensions), which occurs within seconds. Mefenamic acid (MFA) is a poorly soluble drug thought to limit the dissolution rate for membrane permeation. In this study, in-situ dissolution-permeation studies of a nanosuspension of mefenamic acid (MFA) were carried out using second-derivative UV spectroscopy. This method enabled us to distinguish between the concentrations of dissolved MFA and nano-suspended MFA via in-situ measurement and showed an improved dissolution rate of the nanosuspension compared to that of the microsuspension...
January 14, 2019: International Journal of Pharmaceutics
Amir Shamloo, Ali Amani, Mohamadamin Forouzandehmehr, Ibrahim Ghoytasi
Coronary artery disease is the first cause of death across the world. Targeted delivery of therapeutics through controlled release of micro- and nano-particles remains a very capable approach to develop new strategies in treating restenosis and atherosclerotic plaques. In this research, to produce the arterial geometry, an image-processing was done using CT-scan images of a LAD coronary artery. After implementing the finite element mesh, the Fluid-Structure Interaction (FSI) simulation based on physiological boundary conditions was performed...
January 14, 2019: International Journal of Pharmaceutics
Masazumi Iwashita, Kohjiro Hashizume, Masahiro Umehara, Takaaki Ishigami, Shintaro Onishi, Masaki Yamamoto, Kenjirou Higashi, Kunikazu Moribe
A novel amorphous solid dispersion (ASD) of poorly water-soluble nobiletin (Nob) with highly water-soluble methyl hesperidin (MeHes) was developed. Mixtures of Nob and excipients (MeHes, cellulose derivatives, and synthetic polymers) were processed by hot-melt extrusion (HME). Powder X-ray diffraction analysis proved that most of the HME products were fully amorphized. In dissolution studies, Nob-MeHes ASD showed a prominently higher Nob concentration than other HME products with polymeric excipients. Nob concentration upon dissolution of Nob-MeHes ASD was 400 and 7...
January 14, 2019: International Journal of Pharmaceutics
Luke Schenck, Amanda Mann, Zhen Liu, Mikolaj Milewski, Siwei Zhang, Jie Ren, Kristel Dewitt, Andre Hermans, Aaron Cote
No abstract text is available yet for this article.
January 14, 2019: International Journal of Pharmaceutics
Keun Sang Oh, Changsoon Hwang, Ha-Yeon Lee, Jin Sook Song, Hyun-Ji Park, Chul-Kyu Lee, InO Song, Tae-Hong Lim
Postoperative pain is a common form of acute pain that has been treated commonly by local anesthetics through regional nerve blocking. In this study, a series of experiments were conducted using rats to investigate the pharmacokinetic, distribution, and efficacy of a temperature responsive hydrogel based drug delivery device (PF-72) containing ropivacaine (0.75%) for extended relief of postoperative pain by allowing prolonged release of ropivacaine. When the ropivacaine was administered using PF-72, its concentration-time curve (AUClast ) and peak concentration (Cmax ) were 577...
January 14, 2019: International Journal of Pharmaceutics
Samira Gholami, Mohammad-Masoud Mohebi, Ensiyeh Hajizadeh-Saffar, Mohammad-Hossein Ghanian, Ibrahim Zarkesh, Hossein Baharvand
Microneedle patches have been widely used as transdermal transport systems because of their painless and easy application. Marked rigidity, strength, biocompatibility, and physiological stability are unique features of microneedles fabricated from ceramic materials to be used as microneedle patches. However, the conventional ceramic microneedles are typically dense structures with limited free space for biomolecule loading. A facile method is required for fabrication of biocompatible ceramic microneedles with interconnected porosity...
January 14, 2019: International Journal of Pharmaceutics
S Shakiba, S Mansouri, C Selomulya, M W Woo
The surface structure of the crystalline particles affects the functionality of the particles in drug delivery. Prediction of the final structure of particles that crystallize easily within the spray dryer is of interests of many applications. A theoretical framework was developed for the prediction of crystal structure precipitating on the surface of the particle. Mannitol was produced under different processing conditions in order to validate the theoretical model. The theoretical framework was developed based on the dimensionless Damkohler number (Da), to be an indicator of final particle morphology...
January 11, 2019: International Journal of Pharmaceutics
Yoshihiro Hayashi, Yuki Marumo, Takumi Takahashi, Yuri Nakano, Atsushi Kosugi, Shungo Kumada, Daijiro Hirai, Kozo Takayama, Yoshinori Onuki
The purpose of this study was to explore the potential of a quantitative structure-property relationship (QSPR) model to predict tablet density. First, we calculated 3381 molecular descriptors for 81 active pharmaceutical ingredients (API). Second, we obtained data that were merged with a dataset including powder properties that we had constructed previously. Next, we prepared 81 types of tablet, each containing API, microcrystalline cellulose, and magnesium stearate using direct compression at 120, 160, and 200 MPa, and measured the tablet density...
January 11, 2019: International Journal of Pharmaceutics
Ina Petry, Korbinian Löbmann, Holger Grohganz, Thomas Rades, Claudia S Leopold
In the present study the feasibility of an in situ co-amorphisation of the basic drug carvedilol with the acidic co-former aspartic acid was investigated by immersion of film-coated tablets consisting of the two compounds in 0.1MHCl. Tablets containing either crystalline carvedilol with aspartic acid or only crystalline carvedilol were prepared and coated with a gastro-resistant but water-permeable coating of a methacrylic acid - ethyl acrylate copolymer (Eudragit®L55). The film-coated tablets were immersed in 0...
January 11, 2019: International Journal of Pharmaceutics
Kyu-Yeol Nam, Sang Min Cho, Youn-Woong Choi, Chulhun Park, Nileshkumar M Meghani, Jun-Bom Park, Beom-Jin Lee
Commercially available cilostazol (CIL) tablet releases drug immediately and is given twice a day as an antiplatelet and vasodilatory agent. However, clinical usefulness of immediate release (IR) preparation is limited due to its extremely poor water solubility and the difficulty in sustaining the blood concentration, resulting in unwanted side effects such as headaches, pyknocardia and heavy-headed symptoms. To achieve once a day dosage form with enhanced solubility and controlled release, double controlled release CIL matrix tablets (DCRT) were designed by modulating a sol-gel process of binary polymeric blends of a pH-independent hydroxylpropylmethylcellulose (HPMC) and a pH-dependent polymer (carbomer) assisted with anionic surfactant (sodium lauryl sulfate, SLS)...
January 11, 2019: International Journal of Pharmaceutics
Moustafa S Ali, Abdelkader A Metwally, Rania H Fahmy, Rihab Osman
Remarkable efforts are currently devoted to the area of nanodiamonds (NDs) research due to their superior properties viz: biocompatibility, minute size, inert core, and tunable surface chemistry. The use of NDs for the delivery of anticancer drugs has been at the forefront of NDs applications owing to their ability to increase chemosensitivity, sustain drug release, and minimize drug side effects. Accelerated steps towards the move of NDs from bench side to bedside have been recently witnessed. In this review, the effects of NDs production and purification techniques on NDs' final properties are discussed...
January 11, 2019: International Journal of Pharmaceutics
Pravin Shende, Narayan Ture, R S Gaud, F Trotta
Recently, promising strategies of plexes include the complexation of nucleic acids with lipids (lipoplexes) and different kinds of polymers (polyplexes) for delivery of actives and genetic material in abnormal conditions like cancer, cystic fibrosis and genetic disorders. The present review article focuses on the comparative aspects of lipoplexes and polyplexes associated with molecular structure, cellular transportation and formulation aspects. The major advantages of lipoplexes and polyplexes over conventional liposomes involve non-immunogenic viral gene transfer, facile manufacturing and preservation of genetic material encapsulated within the nanocarriers...
January 11, 2019: International Journal of Pharmaceutics
Samer R Abulateefeh, Mahmoud Y Alkawareek, Alaaldin M Alkilany
Poly(D,L-lactide-co-glycolide) (PLGA) and poly(D,L-lactide) (PLA) polymers were used successfully in the preparation of polymer shell microcapsules with mononuclear aqueous cores by the internal phase separation method. These microcapsules were prepared with varying amounts of polymer and water and loaded with fluorescein sodium as a model water soluble drug. Evaluation of drug loading and encapsulation efficiency reveals an optimum polymer to water ratio of around 1:3. Prepared PLGA and PLA microcapsules exhibit sustained drug release over 7 and 49 days, respectively...
January 11, 2019: International Journal of Pharmaceutics
Daniel Hassan, Calvin A Omolo, Ramesh Gannimani, Ayman Y Waddad, Chunderika Mocktar, Sanjeev Rambharose, Nikhil Agrawal, Thirumala Govender
The development of novel antibiotic systems is needed to address the methicillin-resistant Staphylococcus aureus (MRSA) infections. The aim of the study was to explore the novel nanoplex delivery method for vancomycin (VCM) against MRSA using dextran sulfate sodium salt (DXT) as a polyelectrolyte complexing agent. Nanoplexes were formulated by the self-assembling amphiphile polyelectrolyte complexation method and characterized. The size, polydispersity index (PDI), and zeta potential (ZP) of the optimized VCM nanoplexes were 84...
January 11, 2019: International Journal of Pharmaceutics
Lidia Mielczarek, Pamela Krug, Maciej Mazur, Małgorzata Milczarek, Zdzisław Chilmonczyk, Katarzyna Wiktorska
A new combination of sulforaphane (a natural compound obtained from Brassicaceae vegetables) and the cytostatic drug doxorubicin was entrapped in nanometer-sized liposomes. In vitro experiments were performed to investigate the cytotoxicity of these structures on the human breast cancer cell line MDA-MB-231. Confocal microscopy studies revealed enhanced cellular endocytotic internalization, followed by the release of the examined combination from the lysosomes. The in vitro interaction analysis using the Chou-Talalay approach showed high synergistic activity of the examined combination...
January 11, 2019: International Journal of Pharmaceutics
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