Targeted HS-Mediated Gas Therapy with pH-Sensitive Release Property for Myocardial Ischemia-Reperfusion Injury by Platelet Membrane.

Management of myocardial ischemia-reperfusion injury (MIRI) in reperfusion therapy remains a major obstacle in the field of cardiovascular disease, but current available therapies have not yet been achieved in mitigating myocardial injury due to the complex pathological mechanisms of MIRI. Exogenous delivery of hydrogen sulfide (HS) to the injured myocardium can be an effective strategy for treating MIRI due to the multiple physiologic functions of HS, including anti-inflammatory, anti-apoptotic, and mitochondrial protective effects. Here, to realize the precise delivery and release of HS, we proposed the targeted HS-mediated gas therapy with pH-sensitive release property mediated by platelet membranes (PMs).

Ionic liquids as the effective technology for enhancing transdermal drug delivery: Design principles, roles, mechanisms, and future challenges.

Ionic liquids (ILs) have been proven to be an effective technology for enhancing drug transdermal absorption. However, due to the unique structural components of ILs, the design of efficient ILs and elucidation of action mechanisms remain to be explored. In this review, basic design principles of ideal ILs for transdermal drug delivery system (TDDS) are discussed considering melting point, skin permeability, and toxicity, which depend on the molar ratios, types, functional groups of ions and inter-ionic interactions.

M1 Macrophage-Biomimetic Targeted Nanoparticles Containing Oxygen Self-Supplied Enzyme for Enhancing the Chemotherapy.

Tumor hypoxia is considered one of the key causes of the ineffectiveness of various strategies for cancer treatment, and the non-specific effects of chemotherapy drugs on tumor treatment often lead to systemic toxicity. Thus, we designed M1 macrophage-biomimetic-targeted nanoparticles (DOX/CAT@PLGA-M1) which contain oxygen self-supplied enzyme (catalase, CAT) and chemo-therapeutic drug (doxorubicin, DOX). The particle size of DOX/CAT@PLGA-M1 was 202.

Design of Dual-Targeted pH-Sensitive Hybrid Polymer Micelles for Breast Cancer Treatment: Three Birds with One Stone.

Breast cancer has a high prevalence in the world and creates a substantial socio-economic impact. Polymer micelles used as nano-sized polymer therapeutics have shown great advantages in treating breast cancer. Here, we aim to develop a dual-targeted pH-sensitive hybrid polymer (HPPF) micelles for improving the stability, controlled-release ability and targeting ability of the breast cancer treatment options.

Mechanistic Study of Release Characteristics of Two Active Ingredients in Transdermal Patch Containing Lidocaine-Flurbiprofen Ionic Liquid.

Ionic liquids (ILs) have been proven to be an efficient technology for enhancing drug skin permeability. However, the question of whether the two components of ILs are released synchronously in transdermal preparations has remained unclear. Thus, this study aimed to investigate the release characteristics of two components of ILs and their underlying molecular mechanism.

Effect of the combination of permeation enhancer and ion-pairs strategies on transdermal delivery of tofacitinib.

The aim of the present study was to develop a tofacitinib (TOF) transdermal patch by the combination of ion-pairs and chemical permeation enhancer strategies. And a theory of controlled release of chemical permeation enhancers by counterion was proposed on the basis of in vitro skin permeation and skin retention study. Through the in vitro skin permeation study, the formulation factors such as counterion, pressure sensitive adhesive (PSA), drug loading and patch thickness were investigated, and the optimized patch (6.

An investigation on the effect of drug physicochemical properties on the enhancement strength of enhancer: The role of drug-skin-enhancer interactions.

The aim of present work was to investigate the influence of drug physicochemical properties on the enhancement effect of enhancers, which guided the application of enhancers in different drug transdermal prescriptions. Firstly, Polyglyceryl-3 dioleate (POCC) was selected as a model enhancer and its enhancement effect on ten drugs was assessed by in vitro skin permeation experiment. Secondly, the correlation analysis of physicochemical properties of drugs was carried out from the aspects of partition and permeation.

The molecular design of drug-ionic liquids for transdermal drug delivery: Mechanistic study of counterions structure on complex formation and skin permeation.

Though ionic liquids (ILs) as novel enhancers had garnered wide attention, detailed studies elucidating molecular design of drug-ILs were missing and mechanisms of their formation and skin permeation were still lacking. Herein, we systematically investigated effects of counterions structures on formation and skin permeation of drug-ILs. Firstly, effects of counterions on formation of drug-ILs were dependent on polarizability, molecular weight (M.

An investigation on percutaneous permeation of flurbiprofen enantiomers: The role of molecular interaction between drug and skin components.

This work aimed to investigate skin permeation profiles of chiral flurbiprofen and clarify the molecular mechanism of transdermal permeation difference of enantiomers. The in vitro transdermal permeation of enantiomers through rat skin was studied by diffusion cells. Physicochemical parameters of model chiral drugs were determined.

Mechanism insight on drug skin delivery from polyurethane hydrogels: Roles of molecular mobility and intermolecular interaction.

Though polyurethane (PU) hydrogel had great potential in topical drug delivery system, drug skin delivery behavior from hydrogel and the underlying molecular mechanism were still unclear. In this study, PU and Carbomer (CP as control) hydrogels were prepared with lidocaine (LID) and ofloxacin (OFX) as model drugs. In vitro skin permeation and tissue distribution study were conducted to evaluate the drug delivery behaviors.

Enhanced Drug Loading in the Drug-in-Adhesive Transdermal Patch Utilizing a Drug-Ionic Liquid Strategy: Insight into the Role of Ionic Hydrogen Bonding.

Though pharmaceutical polymers were widely used in inhibiting drug recrystallization via strong intermolecular hydrogen and ionic bonds, the improved drug stability was achieved at the cost of the drug release rate or amount in the drug-in-adhesive transdermal patch. To overcame the difficulty, this study aimed to increase drug loading utilizing a novel drug-ionic liquid (drug-IL) strategy and illustrate the underlying molecular mechanism. Here, naproxen (NPX) and triamylamine (TAA) were chosen as the model drug and corresponding counterion, respectively.

Mechanistic insights of the controlled release capacity of polar functional group in transdermal drug delivery system: the relationship of hydrogen bonding strength and controlled release capacity.

Background: Hydrogen bonding interaction was considered to play a critical role in controlling drug release from transdermal patch. However, the quantitative evaluation of hydrogen bonding strength between drug and polar functional group was rarely reported, and the relationship between hydrogen bonding strength and controlled release capacity of pressure sensitive adhesive (PSA) was not well understood. The present study shed light on this relationship.

Molecular mechanism of high capacity-high release transdermal drug delivery patch with carboxyl acrylate polymer: Roles of ion-ion repulsion and hydrogen bond.

In this study, a high capacity-high release transdermal patch was conducted with COOH polyacrylate polymer (PA-1) and non-steroidal anti-inflammatory drugs (NSAIDs), which were characterized using miscibility study, in vitro drug release, drug skin absorption studies in vitro and in vivo. And ibuprofen with the highest cargo loading capacity was chosen as a model drug to investigate innovative molecular mechanism, which was proposed based on ion-ion repulsion and hydrogen bond by FT-IR, Raman, C NMR and X-ray photoelectron spectroscopy (XPS). Drug loading and skin absorption in PA-1 was improved up to 2.

A systematic approach to determination of permeation enhancer action efficacy and sites: Molecular mechanism investigated by quantitative structure-activity relationship.

The present study was to systematically evaluate the enhancement action efficacy and sites of chemical permeation enhancer (CPEs), which provided references for the reasonable application of CPEs and the formula optimization of transdermal patch. Enhancement action efficacy was characterized using an indicator of comprehensive enhancement effect (ER). In addition, enhancement action sites were evaluated using a novel enhancement action parameter (β), which was derived from the release enhancement effect (ER) and skin permeation enhancement effect (ER) using seven CPEs with different physicochemical properties.

Investigation of Controlled Release Molecular Mechanism of Oil Phase in Spilanthol Emulsion: Development and In Vitro, In Vivo Characterization.

The aim of the present study was to develop a spilanthol emulsion and investigate the effect of oil and drug physicochemical properties on drug release and skin retention at molecular level. Formulation factors including oil, emulsifier, and humectant were investigated by in vitro skin retention/permeation study and the optimized formulation was evaluated in vitro and in vivo. In addition, the controlled release effect of oil was characterized using drug emulsion distribution study, drug release study, FT-IR, and molecular modeling.

Molecular mechanism of ion-pair releasing from acrylic pressure sensitive adhesive containing carboxyl group: Roles of doubly ionic hydrogen bond in the controlled release process of bisoprolol ion-pair.

Though ion-pair strategy has been employed as an effective and promising method for controlling transdermal delivery of drugs, investigations into the underlying mechanisms involved in the controlled release process of ion-pairs are still limited. In the present study, a brand-new controlled release system combining acrylic pressure sensitive adhesive containing carboxyl group (carboxylic PSA) with ion-pair strategy was developed, and the molecular mechanism of ion-pair releasing from carboxylic PSA was systemically elucidated. Bisoprolol (BSP) and bisoprolol-lauric acid ion-pair (BSP-C) were chosen as model drugs.

The role of carboxyl group of pressure sensitive adhesive in controlled release of propranolol in transdermal patch: Quantitative determination of ionic interaction and molecular mechanism characterization.

Acrylic pressure sensitive adhesives (PSAs) are widely used in transdermal drug delivery system (TDDS). However, there was little research about the quantitative relationship between drug release and drug-PSAs interaction. In this study, five acrylic PSAs with different molar fraction of carboxyl group were designed and synthesized.

[Effects of Goutengsan on model of Alzheimer dementia in rats by AlCl3].

Objective: Observe the effects of Goutengsan on SOD, MAO-B, GSH-PX, NO, LDH, index of brain, rate of death and so on in rats to study therapeutic effects and mechanism of Goutengsan on Alzheimer dementia (AD) model.

Method: One hundred and twenty rats were randomly divided into 6 groups, 3 experimental groups of which were daily administrated with Goutengsan extract whereas the model and control groups were given NS (0.01 mL x g(-1)).