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Drug Delivery and Translational Research

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https://www.readbyqxmd.com/read/29134556/process-optimization-and-particle-engineering-of-micronized-drug-powders-via-milling
#1
REVIEW
A Brunaugh, H D C Smyth
Process control and optimization is a critical aspect of process analytical technology (PAT), quality by design (QbD), and the implementation of continuous manufacturing procedures. While process control and optimization techniques have been utilized in other manufacturing industries for decades, the pharmaceutical industry has only recently begun to adopt these procedures. Micronization, particularly milling, is a generally low-yield, high-energy consumption process that is well suited for a process optimization mindset...
November 13, 2017: Drug Delivery and Translational Research
https://www.readbyqxmd.com/read/29134555/ciprofloxacin-loaded-calcium-alginate-wafers-prepared-by-freeze-drying-technique-for-potential-healing-of-chronic-diabetic-foot-ulcers
#2
Asif Ahmed, Giulia Getti, Joshua Boateng
Calcium alginate (CA) wafer dressings were prepared by lyophilization of hydrogels to deliver ciprofloxacin (CIP) directly to the wound site of infected diabetic foot ulcers (DFUs). The dressings were physically characterized by scanning electron microscopy (SEM), texture analysis (for mechanical and in vitro adhesion properties), X-ray diffraction (XRD), and Fourier transform infrared spectroscopy (FTIR). Further, functional properties essential for wound healing, i.e., porosity, in vitro swelling index, water absorption (Aw), equilibrium water content (EWC), water vapor transmission rate (WVTR), evaporative water loss (EWL), moisture content, in vitro drug release and kinetics, antimicrobial activity, and cell viability (MTT assay) were investigated...
November 13, 2017: Drug Delivery and Translational Research
https://www.readbyqxmd.com/read/29134554/ex-vivo-rabbit-cornea-diffusion-studies-with-a-soluble-insert-of-moxifloxacin
#3
María Sebastián-Morelló, María Aracely Calatayud-Pascual, Vicent Rodilla, Cristina Balaguer-Fernández, Alicia López-Castellano
The objective of this research was to develop and evaluate an ocular insert for the controlled drug delivery of moxifloxacin which could perhaps be used in the treatment of corneal keratitis or even bacterial endophthalmitis. We have evaluated the ex vivo ocular diffusion of moxifloxacin through rabbit cornea, both fresh and preserved under different conditions. Histological studies were also carried out. Subsequently, drug matrix inserts were prepared using bioadhesive polymers. The inserts were evaluated for their physicochemical parameters...
November 13, 2017: Drug Delivery and Translational Research
https://www.readbyqxmd.com/read/29134553/biological-characterization-of-a-novel-hybrid-copolymer-carrier-system-based-on-glycogen
#4
Markéta Jirátová, Aneta Pospíšilová, Maria Rabyk, Martin Pařízek, Jan Kovář, Andrea Gálisová, Martin Hrubý, Daniel Jirák
The effective drug delivery systems for cancer treatment are currently on high demand. In this paper, biological behavior of the novel hybrid copolymers based on polysaccharide glycogen were characterized. The copolymers were modified by fluorescent dyes for flow cytometry, confocal microscopy, and in vivo fluorescence imaging. Moreover, the effect of oxazoline grafts on degradation rate was examined. Intracellular localization, cytotoxicity, and internalization route of the modified copolymers were examined on HepG2 cell line...
November 13, 2017: Drug Delivery and Translational Research
https://www.readbyqxmd.com/read/29134552/intranasal-delivery-of-%C3%AE-asarone-to-the-brain-with-lactoferrin-modified-mpeg-pla-nanoparticles-prepared-by-premix-membrane-emulsification
#5
Linmei Pan, Jing Zhou, Feng Ju, Huaxu Zhu
Alpha-asarone is a bioactive component of Acorus tatarincuii Schott with low bioavailability, which is often used for treatments of various brain diseases in clinical setting. This study was to formulate biodegradable methoxy polyethylene glycol-polylactic acid (mPEG-PLA) nanoparticles (NPs) surface-modified by lactoferrin (Lf), for delivering α-asarone into the brain following intranasal administration. Alpha-asarone NPs were prepared by premix membrane emulsification. The relative parameters were optimized by a Box-Behnken experimental design...
November 13, 2017: Drug Delivery and Translational Research
https://www.readbyqxmd.com/read/29127610/pvp-va64-as-a-novel-release-modifier-for-sustained-release-mini-matrices-prepared-via-hot-melt-extrusion
#6
Yongcheng Li, Ming Lu, Chuanbin Wu
The purpose of this study was to explore poly(vinylpyrrolidone-co-vinyl acetate) (PVP VA64) as a novel release-modifier to tailor the drug release from ethylcellulose (EC)-based mini-matrices prepared via hot melt extrusion (HME). Quetiapine fumarate (QF) was selected as model drug. QF/EC/PVP VA64 mini-matrices were extruded with 30% drug loading. The physical state of QF in extruded mini-matrices was characterized using differential scanning calorimetry, X-ray powder diffraction, and confocal Raman microscopy...
November 10, 2017: Drug Delivery and Translational Research
https://www.readbyqxmd.com/read/29090413/enhanced-transdermal-delivery-with-less-irritation-by-magainin-pore-forming-peptide-with-a-n-lauroylsarcosine-and-sorbitan-monolaurate-mixture
#7
Haerin Lee, Juhyun Park, Yeu-Chun Kim
Transdermal drug delivery is advantageous over other conventional drug administration routes. However, it can be inefficient because of the natural barrier of the stratum corneum which is the uppermost layer of the skin. A previous study verified that the treatment of magainin pore-forming peptide with N-lauroylsarcosine (NLS) on human skin can increase skin permeability by 47-fold. However, NLS is well known as a potential skin irritant. The irritation potential of NLS is known to decrease when mixed with sorbitan monolaurate (S20)...
October 31, 2017: Drug Delivery and Translational Research
https://www.readbyqxmd.com/read/29079916/formulation-of-99m-technetium-labeled-leuprolide-loaded-liposomes-and-its-biodistribution-study-in-new-zealand-white-female-rabbits-for-assessment-of-its-uterine-targeting-efficiency
#8
Arpita Patel, Amit Tyagi, Rakesh Kumar Sharma, Hetal Thakkar
Leuprolide acetate (LPA), a GnRH analogue, is drug of choice for treatment of uterine fibroids and endometriosis. The current marketed formulations of LPA show severe systemic side effects. This project aims to formulate LPA loaded liposomes to be administered by vaginal route for uterine targeting. Liposomes were prepared by thin film hydration method using 1:1 M ratio of DSPC: Cholesterol and characterized for vesicle size, zeta potential, entrapment efficiency, and loading. Radiolabeling of LPA was performed by direct labeling with reduced technetium-99m...
October 27, 2017: Drug Delivery and Translational Research
https://www.readbyqxmd.com/read/29063498/inhibiting-influenza-virus-replication-and-inducing-protection-against-lethal-influenza-virus-challenge-through-chitosan-nanoparticles-loaded-by-sirna
#9
Abbas Jamali, Fatemeh Mottaghitalab, Asghar Abdoli, Meshkat Dinarvand, Aida Esmailie, Masoumeh Tavassoti Kheiri, Fatemeh Atyabi
Influenza virus causes a highly contagious viral respiratory tract infection with potentially fatal outcomes in humans and animals. There is now widespread influenza virus resistance to commercial drugs due to the genetic diversity of virus. Therefore, new therapeutic formulation needs to be developed. Chitosan/siRNA nanoparticles were generated as a new therapeutic approach against influenza virus infections both in vitro and in vivo. Designed siRNA against influenza nucleoprotein was formulated in chitosan polymer as siRNA/chitosan nanoparticle complex...
October 23, 2017: Drug Delivery and Translational Research
https://www.readbyqxmd.com/read/29058205/monocyte-mediated-drug-delivery-systems-for-the-treatment-of-cardiovascular-diseases
#10
REVIEW
Gil Aizik, Etty Grad, Gershon Golomb
Major advances have been achieved in understanding the mechanisms and risk factors leading to cardiovascular disorders and consequently developing new therapies. A strong inflammatory response occurs with a substantial recruitment of innate immunity cells in atherosclerosis, myocardial infarction, and restenosis. Monocytes and macrophages are key players in the healing process that ensues following injury. In the inflamed arterial wall, monocytes, and monocyte-derived macrophages have specific functions in the initiation and resolution of inflammation, principally through phagocytosis, and the release of inflammatory cytokines and reactive oxygen species...
October 20, 2017: Drug Delivery and Translational Research
https://www.readbyqxmd.com/read/28975503/the-environmental-pollutant-polychlorinated-biphenyls-and-cardiovascular-disease-a-potential-target-for-antioxidant-nanotherapeutics
#11
REVIEW
Prachi Gupta, Brendan L Thompson, Banrida Wahlang, Carolyn T Jordan, J Zach Hilt, Bernhard Hennig, Thomas Dziubla
Despite production having stopped in the 1970s, polychlorinated biphenyls (PCBs) represent persistent organic pollutants that continue to pose a serious human health risk. Exposure to PCBs has been linked to chronic inflammatory diseases, such as cardiovascular disease, type 2 diabetes, obesity, as well as hepatic disorders, endocrine dysfunction, neurological deficits, and many others. This is further complicated by the PCB's strong hydrophobicity, resulting in their ability to accumulate up the food chain and to be stored in fat deposits...
October 3, 2017: Drug Delivery and Translational Research
https://www.readbyqxmd.com/read/28967043/jet-dispensing-of-multi-layered-films-for-the-co-delivery-of-three-antihypertensive-agents
#12
Nicolaos Scoutaris, Maria Malamatari, Adrien Letellier, Dennis Douroumis
Three-layer thin films comprising of two polymers as substrate (ethyl cellulose and, copovidone K28) and three antihypertensive agents (hydrochlorothiazide, amiloride HCl, and carvedilol) were printed using jet dispensing technology. Two film formulations with different ethyl cellulose to copovidone K28 ratio (i.e., 90/10 and 50/50 w/w) were prepared using a three-course dispensing. The films were characterized regarding surface morphology, solid-state properties, polymer-drug interactions, drug distribution in each layer, and in vitro drug release...
October 2, 2017: Drug Delivery and Translational Research
https://www.readbyqxmd.com/read/28944416/regulating-the-alky-chain-length-of-fatty-acid-didanosine-prodrugs-and-evaluating-its-role-in-albumin-binding
#13
Hongxiang Chen, Gang Wang, Lanzhen Sun, Huicong Zhang, Mengchi Sun, Jin Sun, Lei Shang, Cong Luo
Rational design of prodrugs for efficient albumin binding shows distinct advantages in drug delivery in terms of drug availability, systemic circulation, and potential targeting effect. And fatty acids are good candidates due to their high affinity to albumin. However, how the alkyl chain length of fatty acids affects the binding dynamics between prodrugs and albumin, despite its importance, is still unclear. In the present study, three prodrugs of didanosine (DDI) and fatty acids were designed and synthesized to evaluate the effect of the alkyl chain length on prodrug-albumin binding process, including capric acid-didanosine (CA-DDI), myristic acid-didanosine (MA-DDI), and stearic acid-didanosine (SA-DDI)...
September 24, 2017: Drug Delivery and Translational Research
https://www.readbyqxmd.com/read/28875468/multifunctional-jnk-inhibiting-nanotherapeutics-for-augmented-elastic-matrix-regenerative-repair-in-aortic-aneurysms
#14
Andrew Camardo, Dhruv Seshadri, Tom Broekelmann, Robert Mecham, Anand Ramamurthi
Growth of abdominal aortic aneurysms (AAA), localized aortal wall expansions, is driven by the disruption and subsequent loss of aortal wall elastic fibers by matrix metalloproteases (MMPs). Since elastic fibers do not naturally regenerate or repair, arresting/reversing AAA growth has not been possible. Previously, we showed utility of doxycycline (DOX), an MMP inhibitor drug, to stimulate elastic matrix neoassembly and crosslinking at low microgram per milliliter doses in addition to inhibiting MMPs. We currently show in aneurysmal smooth muscle cell (SMC) cultures that effects of exogenous DOX in this dose range are linked to its upregulation of transforming growth factor beta (TGF-β1) via its inhibition of the regulatory protein c-Jun-N-terminal kinase 2 (JNK 2)...
September 5, 2017: Drug Delivery and Translational Research
https://www.readbyqxmd.com/read/28849577/evaluation-of-the-antitumor-effects-of-vitamin-k2-menaquinone-7-nanoemulsions-modified-with-sialic-acid-cholesterol-conjugate
#15
Jia Shi, Songlei Zhou, Le Kang, Hu Ling, Jiepeng Chen, Lili Duan, Yanzhi Song, Yihui Deng
Numerous studies have recently shown that vitamin K2 (VK2) has antitumor effects in a variety of tumor cells, but there are few reports demonstrating antitumor effects of VK2 in vivo. The antitumor effects of VK2 in nanoemulsions are currently not known. Therefore, we sought to characterize the antitumor potential of VK2 nanoemulsions in S180 tumor cells in the present study. Furthermore, a ligand conjugate sialic acid-cholesterol, with enhanced affinity towards the membrane receptors overexpressed in tumors, was anchored on the surface of the nanoemulsions to increase VK2 distribution to the tumor tissue...
August 28, 2017: Drug Delivery and Translational Research
https://www.readbyqxmd.com/read/28849387/evaluation-of-tablet-punch-configuration-on-mitigating-capping-by-a-quality-by-design-approach
#16
Parind M Desai, Parthiban Anbalagan, Cheryl J N Koh, Paul W S Heng, Celine V Liew
Capping is a common problem in the manufacture of some types of tablets and unless resolved, the tableting process cannot proceed. Hence, all factors that can help to lessen the likelihood of capping without unnecessarily reduce turret speed and/or compaction force would be tenable. This study investigated the influence of tablet punch configuration on mitigation of tablet capping. Tablets were prepared from high-dose paracetamol-potato starch granules in a rotary tablet press with flat face plain (FFP), flat face bevel edge (FFBE) and flat face radius edge (FFRE) punch configurations...
August 28, 2017: Drug Delivery and Translational Research
https://www.readbyqxmd.com/read/28895053/drug-delivery-in-female-reproductive-health
#17
EDITORIAL
David R Friend
No abstract text is available yet for this article.
December 2017: Drug Delivery and Translational Research
https://www.readbyqxmd.com/read/28828592/drug-delivery-for-the-treatment-of-endometriosis-and-uterine-fibroids
#18
REVIEW
David R Friend
Endometriosis and uterine fibroids (also known as uterine leiomyomas) are serious medical conditions affecting large numbers of women worldwide. Many women are asymptomatic but those with symptoms require medical intervention to relieve chronic pain and dysmenorrhea and to address infertility. Drug delivery has played a role in reducing some of the symptoms associated with endometriosis and uterine fibroids. Use of drug delivery systems for both conditions can roughly be divided into two categories: (1) existing systems designed for other indications such as contraception for symptomatic relief and (2) development of novel systems aimed at addressing some of the underlying biochemical changes associated with endometriosis and uterine fibroids such as oxidative stress, angiogenesis, and matrix degradation...
December 2017: Drug Delivery and Translational Research
https://www.readbyqxmd.com/read/28812250/miv-150-and-zinc-acetate-combination-provides-potent-and-broad-activity-against-hiv-1
#19
Olga Mizenina, Mayla Hsu, Ninochka Jean-Pierre, Meropi Aravantinou, Keith Levendosky, Gabriela Paglini, Thomas M Zydowsky, Melissa Robbiani, José A Fernández-Romero
We previously showed that the combination of the non-nucleoside reverse transcriptase inhibitor (NNRTI) MIV-150 with zinc acetate (ZA) formulated in a carrageenan (CG; MZC) gel provided macaques significant protection against vaginal simian-human immunodeficiency virus-RT (SHIV-RT) challenge, better than either MIV-150/CG or ZA/CG. The MZC gel was shown to be safe in a phase 1 clinical trial. Herein, we used in vitro approaches to study the antiviral properties of ZA and the MIV-150/ZA combination, compared to other NNRTIs...
December 2017: Drug Delivery and Translational Research
https://www.readbyqxmd.com/read/28612340/long-acting-systemic-hiv-pre-exposure-prophylaxis-an-examination-of-the-field
#20
REVIEW
William R Lykins, Ellen Luecke, Daniel Johengen, Ariane van der Straten, Tejal A Desai
Oral pre-exposure prophylaxis for the prevention of HIV-1 transmission (HIV PrEP) has been widely successful as demonstrated by a number of clinical trials. However, studies have also demonstrated the need for patients to tightly adhere to oral dosing regimens in order to maintain protective plasma and tissue concentrations. This is especially true for women, who experience less forgiveness from dose skipping than men in clinical trials of HIV PrEP. There is increasing interest in long-acting (LA), user-independent forms of HIV PrEP that could overcome this adherence challenge...
December 2017: Drug Delivery and Translational Research
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