Abstract：
: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. Like other NNRTIs, MIV-150 has EC50 values in the subnanomolar to nanomolar range against wild type and NNRTI or RT-resistant HIVs. While less potent than NNRTIs, ZA was shown to be active in primary cells against laboratory-adapted and primary HIV-1 isolates and HIV-1 isolates/clones with NNRTI and RT resistance mutations, with EC50 values between 20 and 110 μM. The MIV-150/ZA combination had a potent and broad antiviral activity in primary cells. In vitro resistance selection studies revealed that previously described NNRTI-resistant mutations were selected by MIV-150. ZA-resistant virus retained susceptibility to MIV-150 (and other RTIs) and MIV-150-selected virus remained sensitive to ZA. Notably, resistant virus was not selected when cultured in the presence of both ZA and MIV-150. This underscores the potency and breadth of the MIV-150/ZA combination, supporting preclinical macaque studies and the advancement of MZC microbicides into clinical testing.
journal_name
Drug Deliv Transl Resjournal_title
Drug delivery and translational researchauthors
Mizenina O,Hsu M,Jean-Pierre N,Aravantinou M,Levendosky K,Paglini G,Zydowsky TM,Robbiani M,Fernández-Romero JAdoi
10.1007/s13346-017-0421-4subject
Has Abstractpub_date
2017-12-01 00:00:00pages
859-866issue
6eissn
2190-393Xissn
2190-3948pii
10.1007/s13346-017-0421-4journal_volume
7pub_type
杂志文章abstract：:The efforts of the topical microbicide field to identify a safe and effective topical microbicide were realized in July of 2010 with the reporting of the results of the Centre for the AIDS Programme of Research in South Africa 004 trial. In this trial, a 1% tenofovir gel was found to reduce women's risk for HIV acquis...
journal_title：Drug delivery and translational research
pub_type： 杂志文章
doi：10.1007/s13346-011-0034-2
更新日期：2011-06-01 00:00:00
abstract：:Inhalation therapy of lipid-based carriers has great potential in direct target towards the root of respiratory diseases, which make them superior over other drug deliveries. With the successful entry of lipid carriers into the target cells, drugs can be absorbed in a sustained release manner and yield extended medici...
journal_title：Drug delivery and translational research
pub_type： 杂志文章,评审
doi：10.1007/s13346-018-0550-4
更新日期：2018-10-01 00:00:00
abstract：:Over the past two decades, polymersomes have been widely investigated for the delivery of diagnostic and therapeutic agents in cancer therapy. Polymersomes are stable polymeric vesicles, which are prepared using amphiphilic block polymers of different molecular weights. The use of high molecular weight amphiphilic cop...
journal_title：Drug delivery and translational research
pub_type： 杂志文章,评审
doi：10.1007/s13346-020-00789-2
更新日期：2020-10-01 00:00:00
abstract：:Trans -resveratrol (t-RES) is a natural polyphenolic compound with extensive therapeutic activities; however, its clinical application is circumscribed due to its poor solubility and low bioavailability. The purpose of this study was to prepare stable t-RES nanocrystals (t-RES-NCs) with different stabilizers to improv...
journal_title：Drug delivery and translational research
pub_type： 杂志文章
doi：10.1007/s13346-017-0362-y
更新日期：2017-06-01 00:00:00
abstract：:The objective of the present work was to develop polymeric nanoparticles of uricase and aceclofenac (NSAID) and to incorporate them into gel, for delivering drugs to synovial joints, for effective treatment of Gout. Nanoparticles containing uricase and aceclofenac were prepared by double emulsion solvent evaporation m...
journal_title：Drug delivery and translational research
pub_type： 杂志文章
doi：10.1007/s13346-015-0219-1
更新日期：2015-06-01 00:00:00
abstract：:RNAi-based nanomedicine platforms (RNPs) have progressed from tools to study gene expression in vitro into clinical trials. Numerous RNPs strategies have been documented with an efficient ability to condense RNAi payloads and induce potent gene silencing. Moreover, some of these RNPs have been explored in various anim...
journal_title：Drug delivery and translational research
pub_type： 杂志文章
doi：10.1007/s13346-013-0158-7
更新日期：2014-02-01 00:00:00
abstract：:Elastin is a vital component of the extracellular matrix, providing soft connective tissues with the property of elastic recoil following deformation and regulating the cellular response via biomechanical transduction to maintain tissue homeostasis. The limited ability of most adult cells to synthesize elastin precurs...
journal_title：Drug delivery and translational research
pub_type： 杂志文章
doi：10.1007/s13346-012-0070-6
更新日期：2012-10-01 00:00:00
abstract：:Supersaturated drug delivery systems are commonly used to address the problems of poor aqueous solubility posed by most of the active pharmaceutical ingredients (APIs). However, the supersaturated systems are highly unstable due to their high free energy levels and demonstrate a tendency to precipitate. Understanding ...
journal_title：Drug delivery and translational research
pub_type： 杂志文章
doi：10.1007/s13346-019-00663-w
更新日期：2020-02-01 00:00:00
abstract：:The objective of this research was to develop polymeric micellar formulations of inhibitors of signal transducer and activator of transcription 3 (STAT3) dimerization, i.e., S3I-1757 and S3I-201, and evaluate the activity of successful formulations in B16-F10 melanoma, a STAT3 hyperactive cancer model, in vitro and in...
journal_title：Drug delivery and translational research
pub_type： 杂志文章
doi：10.1007/s13346-017-0369-4
更新日期：2017-08-01 00:00:00
abstract：:The concept of guided bone regeneration facilitated by barrier membranes has been widely considered to achieve enhanced bone healing in maxillofacial surgery. However, the currently available membranes are limited in their active regulation of cellular activities. In this study, we fabricated polycaprolactone/gelatin ...
journal_title：Drug delivery and translational research
pub_type： 杂志文章
doi：10.1007/s13346-013-0154-y
更新日期：2015-04-01 00:00:00
abstract：:Osteoporosis, due to its prevalence worldwide, is a serious health problem. Topical administration of quercetin, a phytoestrogen, in the form of deformable transfersomes, could be used to treat osteoporosis to overcome its low oral solubility and bioavailability. Formulation process of transfersomes was screened by fr...
journal_title：Drug delivery and translational research
pub_type： 杂志文章
doi：10.1007/s13346-020-00708-5
更新日期：2020-10-01 00:00:00
abstract：:In vivo toxicity and absorption studies of topical ocular drugs are problematic, because these studies involve invasive tissue sampling and toxic effects in animal models. Therefore, different human corneal models ranging from simple monolayer cultures to three-dimensional models have been developed for toxicological ...
journal_title：Drug delivery and translational research
pub_type： 杂志文章,评审
doi：10.1007/s13346-016-0330-y
更新日期：2016-12-01 00:00:00
abstract：:Chemical injury by alkali burn is a major cause of corneal blindness in the clinical setting. Current management advocates multiple therapies aimed to prevent inflammation, initiate quick re-epithelialization, arrest the fibrosis, and avoid dry eye and pain by using bandage contact lenses. We hypothesized sustained de...
journal_title：Drug delivery and translational research
pub_type： 杂志文章
doi：10.1007/s13346-018-0541-5
更新日期：2018-10-01 00:00:00
abstract：:High-energy methods for the manufacturing of nanomedicines are widely used; however, interest in low-energy methods is increasing due to their simplicity, better control over the process, and energy-saving characteristics during upscaling. Here, we developed a novel lipid-core micelle (LCM) as a nanocarrier to encapsu...
journal_title：Drug delivery and translational research
pub_type： 杂志文章
doi：10.1007/s13346-018-0521-9
更新日期：2018-12-01 00:00:00
abstract：:Simvastatin (SIM) is a commonly used cholesterol-lowering drug that can reduce the risk of major cardiovascular events. However, due to its poor intrinsic water solubility, the drug is poorly absorbed from the gastrointestinal tract and exhibits a low oral bioavailability of approximately 5%. The aim of this study was...
journal_title：Drug delivery and translational research
pub_type： 杂志文章
doi：10.1007/s13346-020-00853-x
更新日期：2020-09-11 00:00:00
abstract：:Polyelectrolyte nanoparticle constructs (NPs) comprising salmon calcitonin (sCT), chitosan (CS), and hyaluronic acid (HA) were previously established as having anti-inflammatory potential when injected via the intra-articular (i.a.) route to a mouse model. We attempted to translate the formulation to a large animal mo...
journal_title：Drug delivery and translational research
pub_type： 杂志文章
doi：10.1007/s13346-018-0557-x
更新日期：2018-10-01 00:00:00
abstract：:Hydrogel-forming microneedle array patches (MAPs) have been proposed as viable clinical tools for patient monitoring purposes, providing an alternative to traditional methods of sample acquisition, such as venepuncture and intradermal sampling. They are also undergoing investigation in the management of non-melanoma s...
journal_title：Drug delivery and translational research
pub_type： 杂志文章
doi：10.1007/s13346-020-00727-2
更新日期：2020-06-01 00:00:00
abstract：:Drug nanocrystals have rapidly evolved into a mature drug delivery strategy in the last decade, with almost 16 products currently on the market. Several "top-down" technologies are available in the market for generation of nanocrystals. Despite several advantages, very few bottom-up technologies have been explored for...
journal_title：Drug delivery and translational research
pub_type： 杂志文章
doi：10.1007/s13346-016-0286-y
更新日期：2016-08-01 00:00:00
abstract：:The objectives of this study were to develop biodegradable poly-lactic-co-glycolic acid (PLGA) based injectable phase inversion in situ forming system for sustained delivery of triamcinolone acetonide (TA) and to conduct physicochemical characterisation including in vitro drug release of the prepared formulations. TA ...
journal_title：Drug delivery and translational research
pub_type： 杂志文章
doi：10.1007/s13346-018-0491-y
更新日期：2019-04-01 00:00:00
abstract：:The promise of RNA interference (RNAi) technology in cancer therapeutics aims to deliver small interfering RNA (siRNA) for silencing of gene expression in cell type-specific pathway. However, the challenge for the delivery of stable siRNA is hindered by an immune-hostile tumor microenvironment and physiological barrie...
journal_title：Drug delivery and translational research
pub_type： 杂志文章,评审
doi：10.1007/s13346-016-0352-5
更新日期：2017-04-01 00:00:00
abstract：:Bovine mastitis caused by bacterial infections of the mammary gland (udder) of dairy cows is a costly pathology for the dairy industry due to direct and indirect losses in production. Penethamate, a pro-drug of benzylpenicillin, is used by intramuscular injection (IM). The existing products are powders which must be r...
journal_title：Drug delivery and translational research
pub_type： 杂志文章
doi：10.1007/s13346-017-0388-1
更新日期：2018-04-01 00:00:00
abstract：:The present research work summarises the development of an in situ gelling ophthalmic nanoemulsion of brinzolamide providing sustained release and prolonged therapeutic effect for the treatment of glaucoma. Nanoemulsions were prepared using castor oil, polyoxyl 35 castor oil and polysorbate 80 and with gellan gum as t...
journal_title：Drug delivery and translational research
pub_type： 杂志文章
doi：10.1007/s13346-019-00697-0
更新日期：2020-04-01 00:00:00
abstract：:Gemcitabine is used as a first-line drug for treating many solid tumours. However, it suffers from a major drawback of strong side effects and short plasma half-life because of degradation by enzyme when administered intravenously. Polyesters and copolyesters are the most widely used and preferred class of biodegradab...
journal_title：Drug delivery and translational research
pub_type： 杂志文章
doi：10.1007/s13346-017-0372-9
更新日期：2017-06-01 00:00:00
abstract：:In this work, we studied the effect of gamma irradiation on nano-bioactive glass (NBG) structure, bioactivity, drug loading efficiency, and drug release kinetic. Gamma irradiation was mainly introduced as a safe and cheap method to tailor the drug loading and release efficiencies. NBG was investigated before and after...
journal_title：Drug delivery and translational research
pub_type： 杂志文章
doi：10.1007/s13346-014-0214-y
更新日期：2015-02-01 00:00:00
abstract：:Nanoparticulate systems have emerged as prevalent drug delivery systems over the past few decades. These delivery systems (such as liposomes, emulsions, nanocrystals, and polymeric nanocarriers) have been extensively used to improve bioavailability, prolong pharmacological effects, achieve targeted drug delivery, as w...
journal_title：Drug delivery and translational research
pub_type： 杂志文章
doi：10.1007/s13346-013-0129-z
更新日期：2013-10-01 00:00:00
abstract：:A new PEGylated liposomal formulation containing both gemcitabine (GEM) and paclitaxel (PTX) was investigated in order to realize an innovative multidrug carrier (MDC) to test on human cancer cells. The MDC in question was realized by the liposome extrusion method. Photocorrelation spectroscopy was used for the physic...
journal_title：Drug delivery and translational research
pub_type： 杂志文章
doi：10.1007/s13346-010-0007-x
更新日期：2011-02-01 00:00:00
abstract：:The work describes systematic development of nanomicellar cationic supersaturable self-nanoemulsifying drug delivery systems (CS-SNEDDS) for augmenting oral biopharmaceutical performance of raloxifene hydrochloride. Plain SNEDDS formulation containing Capryol 90, Cremophor RH 40, and Transcutol HP was optimized using ...
journal_title：Drug delivery and translational research
pub_type： 杂志文章
doi：10.1007/s13346-018-0514-8
更新日期：2018-06-01 00:00:00
abstract：:The present work investigates the targeting efficacy of a novel thiolated polymer-based nanocomposite reinforced with glycyrrhetinic acid (GA) and loaded with 5-fluorouracil in hepatocellular carcinoma (HCC). The thiolated polymers were synthesized by EDAC-mediated conjugation reactions and lyophilization. The nanopar...
journal_title：Drug delivery and translational research
pub_type： 杂志文章
doi：10.1007/s13346-020-00894-2
更新日期：2021-01-11 00:00:00
abstract：:Curcumin (CUR), a natural polyphenolic compound, is considered as one of the most potential candidates against Alzheimer disease (AD) by targeting multiple pathologies such as amyloid-beta, tau phosphorylation, and oxidative stress. Poor physicochemical profile and oral bioavailability (BA) are the major contributors ...
journal_title：Drug delivery and translational research
pub_type： 杂志文章
doi：10.1007/s13346-018-0570-0
更新日期：2018-10-01 00:00:00
abstract：:In this study, we developed, characterized, and tested in vivo polymeric nanoparticle of ethambutol labeled with 99mTc as nanoradiopharmaceutical for early diagnosis of tuberculosis by single-photon emission computed tomography, also as a therapeutic choice. Nanoparticles were developed by double emulsification. All c...
journal_title：Drug delivery and translational research
pub_type： 杂志文章
doi：10.1007/s13346-018-0577-6
更新日期：2019-02-01 00:00:00
