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International Journal of Pharmaceutics

Ryoma Tanaka, Kenta Kojima, Yusuke Hattori, Kazuhide Ashizawa, Makoto Otsuka
No abstract text is available yet for this article.
July 9, 2018: International Journal of Pharmaceutics
Shubhangi Mahajan, Abhimanyu Patharkar, Kaushik Kuche, Rahul Maheshwari, Pran Kishore Deb, Kiran Kalia, Rakesh K Tekade
In recent time, carbon nanotubes (CNTs) have gained vital importance for pharmaceutical formulation scientist for delivering drugs and genes, owing to their excellent surface properties. For example, their aspect ratio is thought to be responsible for their excellent cell penetration aptitude; anisotropic conductivity/semi-conductivity along their axis is ideal for integration with nervous and muscular tissue; an ultrahigh surface area maximizes their ability to "talk" with biological matter; the hollow interior provides an enormous cargo-carrying capacity for drug delivery; and their exteriors are readily functionalized to permit tailoring of solubility and biological recognition...
July 8, 2018: International Journal of Pharmaceutics
Heba Mohamed Fahmy, Engy Abd El-Malek Saeed Saad, Neveen Moustafa Sabra, Amal Ahmed El-Gohary, Faten Fathy Mohamed, Mohamed Hassaneen Gaber
Elevation of the intraocular pressure (IOP) is recognized as a risk factor for glaucoma development. Latanoprost (LAT) is a prostaglandin analog used to reduce the (IOP). Thymoquinone (TQ) is a major bioactive ingredient of Nigella sativa. The aim of this study was to develop novel liposomal drug carriers for ocular delivery of LAT, TQ and a mixture of them to investigate their IOP lowering efficacy upon subconjunctival injection in glaucoma-induced rabbit's eye. The aim of the present work extends also to study the effect of the different liposome formulations on the aqueous humor oxidative stress...
July 8, 2018: International Journal of Pharmaceutics
Gesmi Milcovich, Filipe E Antunes, Mario Grassi, Fioretta Asaro
The limited stability of catanionic vesicles has discouraged their wide use for encapsulation and controlled release of active substances. Their structure can easily break down to form lamellar phases, micelles or rearrange into multilamellar vesicles, as a consequence of small changes in their composition. However, despite the limited stability, catanionic vesicles possess an attractive architecture, which is able to efficiently encapsulate both hydrophobic and hydrophilic molecules. Therefore, improving the stability of the vesicles, as well as the control on unilamellar structures, are prerequisites for their wider application range...
July 7, 2018: International Journal of Pharmaceutics
Allan J Williams, Faron Jordan, Gareth King, Andrew L Lewis, Lisbeth Illum, Tahir Masud, Alan C Perkins, Richard G Pearson
No abstract text is available yet for this article.
July 5, 2018: International Journal of Pharmaceutics
Jiaojiao Yang, Caroline Alvebratt, Xi Lu, Christel A S Bergström, Maria Strømme, Ken Welch
Formulating active pharmaceutical ingredients (APIs) in the amorphous state can increase their apparent aqueous solubility and dissolution rate and consequently improve their bioavailability. This study demonstrates, for the first time, the ability to stabilize an API in the amorphous state using a solid dispersion of magnesium carbonate nanoparticles within the API. Specifically, high proportions of ibuprofen were able to be stabilized in the amorphous state using as little as 17% wt/wt amorphous magnesium carbonate nanoparticles, and drug release rates 83 times faster than from the crystalline state were achieved...
July 5, 2018: International Journal of Pharmaceutics
Xinyuan Xu, Hui Shang, Tianyu Zhang, Panjing Shu, Yanpeng Liu, Jing Xie, Dongyue Zhang, Hong Tan, Jianshu Li
Injection of insulin is an effective therapy to treat most patients with the type I diabetes and some with type II diabetes. Additionally, the release of insulin under specific conditions has attracted widespread interest. In this study, a smart drug carrier that can release insulin depending on the changes in blood glucose levels was designed. Combining two popular molecules through facile synthetic processes, a drug carrier of reversible phenylboronate group modified cyclodextrin (β-CD-EPDME) was fabricated...
July 5, 2018: International Journal of Pharmaceutics
Ayat A Allam, Sarah J Potter, Sergey L Bud'ko, Donglu Shi, Dina F Mohamed, Fawzia S Habib, Giovanni M Pauletti
Poor aqueous solubility, chemical instability, and indiscriminate cytotoxicity have limited clinical development of camptothecin (CPT) as potent anticancer therapeutic. This research aimed at fabricating thermoresponsive nanocomposites that enhance solubility and stability of CPT in aqueous milieu and enable stimulus-induced drug release using magnetic hyperthermia. 1,2-Dipalmitoyl-sn-glycero-3-phosphocholine (DPPC) and L-α-dipalmitoylphosphatidyl glycerol (DPPG) (1:1, mol/mol) were immobilized on the surface of superparamagnetic Fe3 O4 nanoparticles (SPIONs) via high affinity avidin-biotin interactions...
July 5, 2018: International Journal of Pharmaceutics
Jari Rubbens, Raf Mols, Joachim Brouwers, Patrick Augustijns
The small intestine is generally considered the major site of absorption after oral drug administration. Absorption from the stomach is often disregarded, though passive diffusion across the gastric mucosal barrier is theoretically possible. In this study, an in situ gastric bolus administration model was used to study the gastric absorption of pharmaceutical compounds in fasted and fed state rats. Three drugs [paracetamol (neutral), diclofenac (acidic) and posaconazole (basic)] were administered directly into the stomach as solution (paracetamol and diclofenac) or suspension (posaconazole)...
July 4, 2018: International Journal of Pharmaceutics
F Casati, F Briatico-Vangosa, F Baldi, A Melocchi, A Maroni, A Gazzaniga, L Zema
The present work focuses on application of an investigational approach to assess the hot-processability of pharmaceutical-grade polymers with a potential for use in the manufacturing of reservoir drug-delivery systems via micromolding, and the performance of resulting molded barriers. An inert thermoplastic polymer, ethylcellulose (EC), widely exploited for preparation of prolonged-release systems, was employed as a model component of the release-controlling barriers. Moldability studies were performed with plasticized EC, as such or in admixture with release modifiers, by the use of disk-shaped specimens ≥ 200 µm in thickness...
July 4, 2018: International Journal of Pharmaceutics
Fiona Y Glassman, Sathy V Balu-Iyer
A major complication with enzyme replacement therapy of Factor VIII (FVIII) in Hemophilia A (HA) is the development of anti-drug antibodies. Recently, we have shown that FVIII administration in the presence of heterogeneous phosphatidylserine (PS) nanoparticles derived from a natural source induces tolerance to FVIII, suggesting that PS converts an immunogen to a tolerogen. However, the specific structural features responsible for the immune-regulatory properties of PS is unclear. Identifying a specific PS species that is responsible is critical in order to further develop and optimize this nanoparticle...
July 4, 2018: International Journal of Pharmaceutics
Ramona Strob, Adrian Dobrowolski, Gerhard Schaldach, Peter Walzel, Markus Thommes
The preparation of submicron-sized particles is relevant in chemical, food and pharmaceutical applications. In pharmaceutics, spray dried submicron-sized particles (0.1-1µm) can increase the dissolution rate as well as the solubility of poorly water-soluble drugs. Since the particle size during spray drying is mainly influenced by the droplet size, the preparation of uniform droplets smaller than 3µm is of particular interest. In this work, a two-fluid nozzle was combined with a cyclone droplet separator...
July 4, 2018: International Journal of Pharmaceutics
Siyam M Ansar, Wenlei Jiang, Thilak Mudalige
To understand the quality, efficacy, and safety of liposomal drugs, it is necessary to develop a robust and accurate method for the separation and the quantification of unencapsulated and liposome-associated drugs (or liposomal encapsulated drugs). Conventional methods involve separation of unencapsulated and liposome-associated drug using solid phase extraction and further drug quantification. This is a lengthy process, and sometimes solid phase extraction induces drug leakage from the liposomes causing erroneous results...
July 4, 2018: International Journal of Pharmaceutics
Varun Kushwah, Sameer S Katiyar, Ashish Kumar Agrawal, Isha Saraf, Inder Pal Singh, Dimitrios A Lamprou, Ramesh C Gupta, Sanyog Jain
The present study investigates effect of linkers [zero length (without linker), short length linker (glycine and lysine) and long length linker (PEG1000, PEG2000 and PEG3500)] on pharmacokinetics and toxicity of docetaxel (DTX) and gemcitabine (GEM) bio-conjugates. Conjugates were synthesized via carbodiimide chemistry and characterized by 1 H-NMR and FTIR. Conjugation of DTX and GEM via linkers showed diverse physiochemical and plasma stability profile. Cellular uptake mechanism in MCF-7 and MDA-MB-231 cell lines revealed clathrin mediated internalization of bio-conjugates developed by using long length linkers, leading to higher cytotoxicity compared with free drug congeners...
July 4, 2018: International Journal of Pharmaceutics
C Bode, H Kranz, F Siepmann, J Siepmann
Different types of in-situ forming implants based on poly(lactic-co-glycolic acid) (PLGA) and N-methyl-pyrrolidone (NMP) were prepared for controlled ocular delivery of dexamethasone. The impact of the volume of the release medium, initial drug content, polymer molecular weight and PLGA concentration on the resulting drug release kinetics were studied and explained based on a thorough physico-chemical characterization of the systems. This included for instance the monitoring of dynamic changes in the implants' wet and dry mass, morphology, PLGA polymer molecular weight, pH of the surrounding bulk fluid and water/NMP contents upon exposure to phosphate buffer pH 7...
July 4, 2018: International Journal of Pharmaceutics
Manju Kanamala, Brian D Palmer, William R Wilson, Zimei Wu
To facilitate the development of PEG-cleavable pH-sensitive liposomes (CL-pPSL), this study aimed to fully characterize a new pH-sensitive polymer, PEGB -Hz-CHEMS. Polyethylene glycol (PEG) functionalised with 4-carboxybenzaldehyde (PEGB ) was linked to cholesteryl hemisuccinate (CHEMS) via an acid labile hydrazide-hydrazone hybrid bond (-CO-NH-N=CH-) to form PEGB -Hz-CHEMS. The polymer was post-inserted into DOPE/CHEMS liposomes to form CL-pPSL. A validated stability-indicating HPLC-UV method was developed with the aid of multiple linear regression for the mobile phase...
July 4, 2018: International Journal of Pharmaceutics
Wessam Hamdy Abd-Elsalam, Sara Nageeb El-Helaly, Mohammed Abdallah Ahmed, Abdulaziz Mohsen Al-Mahallawi
The study aimed to fabricate innovative drug-phospholipid complexes termed "sonocomplexes" adopting ultrasound irradiation to increase the liposolubility and to enhance the intestinal absorption of rosuvastatin as a model drug for BCS class III active pharmaceutical ingredients (APIs). A 22 full factorial design was fashioned to investigate the influence of phosphatidylcholine content in the phospholipid (∼30 and 60%) and molar ratio of phospholipid to rosuvastatin (1:1 and 2:1) on physicochemical properties of sonocomplexes...
July 3, 2018: International Journal of Pharmaceutics
Sophia Malli, Christian Bories, Mickaël Bourge, Philippe M Loiseau, Kawthar Bouchemal
Previous data from our research group showed that chitosan-coated poly(isobutylcyanoacrylate) nanoparticles (NPs) (denoted PIBCA/Chito20) exhibited intrinsic anti-Trichomonas vaginalis activity, while PIBCA/pluronic® F68 without chitosan (PIBCA/F68) were inactive. However, the mechanism of anti-T. vaginalis activity of chitosan-coated PIBCA NPs is still unknown. Our hypothesis is that chitosan-coated NPs are internalized by the parasite, contrarily to PIBCA/F68. In this investigation, the impact of NP surface on their internalization by the protozoan was studied using flow cytometry and parasite morphological changes after different incubation times with PIBCA/Chito20 NPs were monitored by electron microscopy...
July 3, 2018: International Journal of Pharmaceutics
Prakash Khadka, Jack Dummer, Philip C Hill, Shyamal C Das
Drug delivery via the inhaled route has advantages for treating local and systemic diseases. Pulmonary drug delivery may have potential in treating tuberculosis (TB), which is mainly localised in the lung (pulmonary tuberculosis ∼75%) while also affecting other organs (extra-pulmonary tuberculosis). Currently, rifampicin, a first-line anti-tubercular drug, is given orally and the maximum daily oral dose is the lesser of 10 mg/kg or 600 mg. Since only a small fraction of this dose is available in the lung, concentrations may frequently fail to reach bactericidal levels, and therefore, contribute to the development of multi-drug resistant pulmonary TB...
July 3, 2018: International Journal of Pharmaceutics
Jingjunjiao Long, Ashveen V Nand, Sudip Ray, Sam Mayhew, David White, Craig R Bunt, Ali Seyfoddin
Customisation of sustained and controlled release of contraceptives plays a key role in veterinary applications. A biodegradable projectile containing different doses of contraceptive progesterone was prepared using fused deposition modelling 3D printing. Three concentrations of progesterone (2, 5 and 10% w/w) with polylactic acid was prepared as a 1.75 mm filament by hot melt extrusion. Solvent dissolution tests confirmed the successful incorporation of progesterone in the polymer while microscopic (SEM) studies indicated the drug was melted and thoroughly mixed with the polymer matrix and pore-formation after dissolution...
July 2, 2018: International Journal of Pharmaceutics
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