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Drug Delivery and Translational Research

Maria José Alonso
No abstract text is available yet for this article.
May 16, 2019: Drug Delivery and Translational Research
Herman Weiss, Bridget Martell, Ginger D Constantine, Sarah M Davis, Justin D Vidal, Philip R Mayer, Martin Doorbar, David R Friend
The objectives of this work were to evaluate the in vitro release and in vivo pharmacokinetics and local tolerability of a novel, segmented ethylene-vinyl acetate (EVA) intravaginal ring (IVR) delivering progesterone (P) in drug-naïve ovariectomized female Dorset crossbred sheep. Following preparation and assessment of in vitro release of P, animals were randomized into one of six treatment groups: group 1 Crinone® 8% gel (90 mg); group 2 Prometrium® 200-mg capsules; group 3 placebo IVR; group 4 progesterone (P) IVR 4 mg/day; group 5 P IVR 8 mg/day; or group 6 P IVR 12 mg/day...
May 7, 2019: Drug Delivery and Translational Research
Eunmi Ban, Taek-Hyun Kwon, Aeri Kim
MicroRNAs (miRNAs) are short non-coding RNAs that play important roles in many cellular processes such as development, proliferation, differentiation, and apoptosis. For this reason, miRNAs have been proposed and investigated as biomarkers and therapeutics for various diseases such as cancer, diabetes, and cardiovascular disease. However, delivery of miRNAs and their antagomirs to target sites remains challenging because of poor cellular uptake and degradation by nucleases. Various delivery systems have been investigated for enhanced delivery of miRNAs to cells, organs, and tissues of interest, thereby enabling evaluation of their biological functions and clinical trials...
May 2, 2019: Drug Delivery and Translational Research
Manish Kumar, Pooja Upadhayay, Ravi Shankar, Monika Joshi, Shailendra Bhatt, Anuj Malik
The aim of the present study was to fabricate a thermosensitive gel containing chlorpheniramine maleate (CPM)-loaded nanoparticles following intranasal administration for effective treatment of allergic rhinitis. Chitosan-based nanoparticles were prepared by a precipitation method followed by the addition of developed NPs within the poloxamer 407- and carbopol 934P-based mucoadhesive thermoreversible gel. Developed formulations were evaluated for particle size, PDI, % entrapment efficiency, and % cumulative drug permeation...
May 2, 2019: Drug Delivery and Translational Research
Piyali Dey, Subham Banerjee, Santa Mandal, Pronobesh Chattopadhyay
Resealed erythrocytes (RSE) are potential, site-specific carrier system for drug delivery with prolonged drug release activity. In this study, erythrocytes obtained from Wistar albino rats were loaded with ambroxol hydrochloride (AH) with the focus to convenience the lung targeting possibility of the carrier erythrocytes. AH loading in erythrocytes using preswell dilution technique with glutaraldehyde (GA) as a cross-linking agent was evaluated and validated. Drug-loaded erythrocyte was characterized in terms of in vitro drug release followed by osmotic fragility study which showed amplified drug entrapment efficiency (DEE) and hemoglobin content values as well...
April 23, 2019: Drug Delivery and Translational Research
Simon Vanstone, James M Stone, Sergey N Gordeev, Richard H Guy
Optical poration, or drilling, of the human nail has the potential to drastically improve transungual drug delivery. However, this approach is accompanied by thermal damage to the nail tissue surrounding the laser radiation-created pore. In this paper, fluorescence microscopy has been employed to quantitatively evaluate thermal damage to the nail induced by laser ablation with 80 MHz, nanojoule, femtosecond pulses delivered via a hollow-core fibre. An empirical relation has been established between the intensity of the resulting fluorescence signal and temperature to which the nail was exposed...
April 23, 2019: Drug Delivery and Translational Research
Sarah S Nasr, Maha M A Nasra, Heba A Hazzah, Ossama Y Abdallah
The present work aimed to prepare silymarin-loaded mesoporous silica nanoparticles (MSNs) and to assess the system's dissolution enhancement ability on the pharmacodynamic performance of silymarin as a hepatoprotective agent. For this purpose, a soft-templating technique was used to prepare silymarin-loaded MSNs. The loaded MSNs were further characterized for their particle size, zeta potential, surface properties, and in vitro drug dissolution testing. In addition, differential scanning calorimetry (DSC) and Fourier transform infrared spectroscopy (FTIR) were also carried out...
April 18, 2019: Drug Delivery and Translational Research
Sagar Dhoble, Vandana Patravale
Pulmonary arterial hypertension (PAH) is the increase in mean pulmonary arterial pressure (> 25 mmHg). The development of the non-reversible plexiform lesions on the arterial walls of the pulmonary arteries has evolved as the reason to increase the pressure. The current treatments are directed towards the vasodilation of the pulmonary arteries via the endothelin, prostacyclin, and NO pathways which provides symptomatic relief. Deeper understanding of the disease leads to the various pathophysiological targets that play an important role in the development of PAH...
April 18, 2019: Drug Delivery and Translational Research
Bo Lou, Kate Connor, Kieron Sweeney, Ian S Miller, Alice O'Farrell, Eduardo Ruiz-Hernandez, David M Murray, Garry P Duffy, Alan Wolfe, Enrico Mastrobattista, Annette T Byrne, Wim E Hennink
The development of an effective and safe treatment for glioblastoma (GBM) represents a significant challenge in oncology today. Downregulation of key mediators of cell signal transduction by RNA interference is considered a promising treatment strategy but requires efficient, intracellular delivery of siRNA into GBM tumor cells. Here, we describe novel polymeric siRNA nanocarriers functionalized with cRGD peptide that mediates targeted and efficient reporter gene silencing in U87R invasive human GBM cells. The polymer was synthesized via RAFT copolymerization of N-(2-hydroxypropyl)-methacrylamide (HPMA) and N-acryloxysuccinimide (NAS), followed by post-polymerization modification with cholesterol for stabilization, cationic amines for siRNA complexation, and azides for copper-free click chemistry...
April 9, 2019: Drug Delivery and Translational Research
Zahra Mahmoodi, Javad Mohammadnejad, Sajad Razavi Bazaz, Ali Abouei Mehrizi, Mohammad Adel Ghiass, Massoud Saidijam, Rassoul Dinarvand, Majid Ebrahimi Warkiani, Masoud Soleimani
Dexamethasone is a widely used drug in medical and biological applications. Since the systematic and controllable release of this drug is of significant importance, encapsulation of this anti-inflammatory drug in poly(lactic-co-glycolic acid) (PLGA) nanoparticles can minimize uncontrolled issues. As dexamethasone-encapsulated PLGA nanoparticles are synthesized in the presence of organic solvents, poly(dimethylsiloxane) (PDMS)-based microchannels collapse due to the swelling problem. In present study, PTFE nanoparticles were used for the surface modification of the microchannels to prevent absorption and adhesion of solvents into the microchannels' wall...
April 4, 2019: Drug Delivery and Translational Research
Arvind Bagde, Ketan Patel, Shallu Kutlehria, Nusrat Chowdhury, Mandip Singh
Solid lipid nanoparticles (SLN) have been formulated using various batch processes, e.g., solvent diffusion evaporation, emulsification solvent evaporation followed by size reduction using high-pressure homogenization (HPH) or ultrasonication. However, for the manufacturing of formulations, continuous processes are always preferred over batch processes since they are more efficient and offer better quality of the end product. Hence, we developed topical SLN of ibuprofen (IBU) using hot melt extrusion (HME), prepared a gel formulation, and performed its in vitro and in vivo evaluation...
March 28, 2019: Drug Delivery and Translational Research
Jivan Jyoti, Nandha Kumar Anandhakrishnan, Sachin Kumar Singh, Bimlesh Kumar, Monica Gulati, K Gowthamarajan, Rajesh Kumar, Ankit Kumar Yadav, Bhupinder Kapoor, Narendra Kumar Pandey, Sananda Som, Souvik Mohanta, Indu Melkani, Rubiya Khursheed, Rakesh Narang
The aim of present study was to co-administer curcumin (CRM) liquisolid pellets and coated duloxetine hydrochloride (DXH) pellets in rats to treat neuropathic pain (NP) associated with chronic constriction injury (CCI). To formulate liquisolid pellets of CRM, it was first dissolved in Tween-80 and then adsorbed on the porous surface of MCC PH102 and Syloid XDP that were used as carrier and coating materials, respectively. Central composite design was used to optimize the liquisolid formulation. The results of powder X-ray diffraction studies, differential scanning calorimetry, and scanning electron microscopy showed complete solubility of drug in Tween-80 followed by its complete adsorption on the porous surface of Syloid XDP and MCC PH102...
March 25, 2019: Drug Delivery and Translational Research
Dhanya Narayanan, Gopikrishna J Pillai, Shantikumar V Nair, Deepthy Menon
This study reports the development of a nanoformulation of diclofenac sodium, a potent non-steroidal anti-inflammatory drug, at its clinical dose, utilizing a FDA approved polymer, hydroxyethyl starch. The study specifically focused on the control of pharmacokinetics, pharmacodynamics, and biodistribution by particle surface functionalization and alteration of excipient levels in the final formulation. Stable diclofenac sodium-loaded hydroxyethyl starch nanoparticles (nanodiclo) of size 170 ± 5 nm and entrapment efficiency 72 ± 3% were prepared...
March 22, 2019: Drug Delivery and Translational Research
Amit Mirani, Harish Kundaikar, Shilpa Velhal, Vainav Patel, Atmaram Bandivdekar, Mariam Degani, Vandana Patravale
A vaginal microbicide is a front-line women-dependent approach and an alternative to a condom for prevention of unprotected sexual intercourse-associated HIV. The microbicide research is still in its infancy with several products in the clinical studies being reported to have good efficacy, safe, but with poor adherence. One such molecule reported with an excellent efficacy when tested preclinically is curcumin, a natural polyphenol derived from Curcuma longa. Despite its potential HIV-1 inhibitory activity, it has intense yellow color staining properties, which would result in poor consumer compliance and adherence for vaginal application...
March 21, 2019: Drug Delivery and Translational Research
Zahid Hussain, Shahzeb Khan, Muhammad Imran, Muhammad Sohail, Syed Wadood Ali Shah, Marcel de Matas
On account of heterogeneity, intrinsic ability of drug resistance, and the potential to invade to other parts of the body (malignancy), the development of a rational anticancer regimen is dynamically challenging. Chemotherapy is considered the gold standard for eradication of malignancy and mitigation of its reoccurrence; nevertheless, it has also been associated with detrimental effects to normal tissues owing to its nonselectivity and nominal penetration into the tumor tissues. In recent decades, nanotechnology-guided interventions have been well-acclaimed due to their ability to facilitate target-specific delivery of drugs, avoidance of nontarget distribution, alleviated systemic toxicity, and maximized drug internalization into cancer cells...
March 20, 2019: Drug Delivery and Translational Research
Wei Wang, Hou Ming Liu, Jing Zhou, Yu Guang Wang, Xi Feng, Hao Tang, Qinying Yan, Rong Sheng Zhu, Yu Wei Wu, Xing Guo Wang, Dan He, Fan Chen
BACKGROUND: The tuberculin skin test (TST) is a long-established screening method for tuberculosis. However, the Mantoux technique is often difficult to reliably perform, which affects testing results and safety, which causes local skin pain and pruritus. METHODS: In this study, dissolving microneedle-array patches (MNP) were used to deliver purified protein derivative (PPD) tuberculin into the skin. The skin reaction was compared between MNP delivery and conventional injection...
March 19, 2019: Drug Delivery and Translational Research
Derek J Overstreet, Vajra S Badha, John M Heffernan, Erin P Childers, Rex C Moore, Brent L Vernon, Alex C McLaren
Local antimicrobial delivery is a promising strategy for improving treatment of deep surgical site infections (SSIs) by eradicating bacteria that remain in the wound or around its margins after surgical debridement. Eradication of biofilm bacteria can require sustained exposure to high antimicrobial concentrations (we estimate 100-1000 μg/mL sustained for 24 h) which are far in excess of what can be provided by systemic administration. We have previously reported the development of temperature-responsive hydrogels based on poly(N-isopropylacrylamide-co-dimethylbutyrolactone acrylate-co-Jeffamine M-1000 acrylamide) (PNDJ) that provide sustained antimicrobial release in vitro and are effective in treating a rabbit model of osteomyelitis when instilled after surgical debridement...
March 19, 2019: Drug Delivery and Translational Research
Kuldeep Nigam, Atinderpal Kaur, Amit Tyagi, Md Nematullah, Farah Khan, Reema Gabrani, Shweta Dang
Direct nose-to-brain delivery of drugs and faster onset of action have made intra-nasal route a much sought-after alternative to conventional routes of drug delivery to the brain. Lamotrigine is used for the treatment and management of neuropathic pain, and in the present work, lamotrigine (LTG)-PLGA nanoparticles were developed for intra-nasal delivery. The LTG-PLGA nanoparticles were prepared using modified nanoprecipitation method via high-speed homogenization and ultra-sonication techniques. Entrapment efficiency (EE%) of developed LTG-PLGA-NPs was found to be 84...
March 18, 2019: Drug Delivery and Translational Research
Christina Leichner, Randi Angela Baus, Max Jelkmann, Melanie Plautz, Jan Barthelmes, Sarah Dünnhaupt, Andreas Bernkop-Schnürch
The objective of the study was the development and in vitro characterization of a self-emulsifying drug delivery system (SEDDS) for the nasal application of dimenhydrinate. Final composition of SEDDS was established based on drug solubility and stability studies. Dimenhydrinate was loaded into the SEDDS pre-concentrates to 7.5% (m/v). The droplet size of the final SEDDS formulations was in a range between 60 and 220 nm. Permeability, as well as tissue toxicity, of the formulations was investigated using bovine nasal mucosa...
March 14, 2019: Drug Delivery and Translational Research
N Kanwar, R Bhandari, A Kuhad, V R Sinha
Rasagiline mesylate is an irreversible MAO-B inhibitor which requires daily oral administration for treatment of Parkinson's disease due to its short half-life. Patients with Parkinson's disease also develop dysphagia, i.e., difficulty in swallowing. Encapsulating rasagiline in polycaprolactone microspheres can alleviate the problem of daily oral administration by prolonging drug release from polymeric microspheres for 1 month by single subcutaneous administration. Polycaprolactone shows absence of any acidic environment generation during its degradation in body which is its advantage over poly (lactic-co-glycolic) acid...
March 14, 2019: Drug Delivery and Translational Research
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