Design, characterization and comparison of transdermal delivery of colchicine via borneol-chemically-modified and borneol-physically-modified ethosome.
Authors: Zhang Y, Zhang N, Song H, Li H, Wen J, Tan X, Zheng W Abstract Gout is a kind of joint disease characterized by the accumulation of monosodium urate (MSU) crystals in the joint and its surrounding tissue, causing persistent hyperuricemia. Colchicine is the first choice of treatment for acute gout attacks. Due to strong toxicity of colchicines oral tablets, there are high fluctuations of blood drug concentration and serious irritation of gastrointestinal tract, and hence a transdermal preparation can help to slow down the blood drug concentration, reduce the frequency of drug taking, and improve the patient...
Source: Drug Delivery - February 14, 2019 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Rhodotorula glutinis as a living cell liposome to deliver polypeptide drugs in vivo.
Authors: Fei Z, Li S, Wang J, Wang Y, Jiang Z, Huang W, Sun H Abstract The potential advantages of recombinant microbes as oral drug carriers for curing diseases have attracted much attention. The use of recombinant oil microbes as living cell liposomes to carry polypeptide drugs may be an ideal polypeptide oral drug delivery system. GM4-ΔTS was constructed by LFH-PCR from Rhodotorula glutinis GM4, which was screened and preserved in our laboratory, and then transferred into choline-phosphate cytidylyltransferase (CCT), which is a rate-limiting enzyme for lecithin synthesis. The results showed that the CCT ge...
Source: Drug Delivery - February 14, 2019 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Stereoselectivity evaluation of chiral chitosan microspheres delivery system containing rac-KET in vitro and in vivo.
Authors: Yin LN, Zhang YW, Huang WH, Wang SH, Zheng GL Abstract The influence of chiral excipient D-chitosan (CS) on the stereoselective release of racemic ketoprofen (rac-KET) microspheres has been investigated in comparison to those microspheres containing individual enantiomers in vitro and in vivo. Stereoselectivity was observed in vitro release test, with R-KET release slightly higher than that of S-KET, especially in 3% rac-KET loading microspheres. Stereoselectivity is dependent on the content of chiral excipient and pH of release medium. A molecular docking study between CS and KET enantiomers further revea...
Source: Drug Delivery - February 14, 2019 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

ENHANZE ® drug delivery technology: a novel approach to subcutaneous administration using recombinant human hyaluronidase 20.
This article reviews pharmaceutical properties of rHuPH20, its current applications with approved therapeutics, and the potential for future developments. PMID: 30744432 [PubMed - in process] (Source: Drug Delivery)
Source: Drug Delivery - February 14, 2019 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Permeation-enhancing effects and mechanisms of O-acylterpineol on isosorbide dinitrate: mechanistic insights based on ATR-FTIR spectroscopy, molecular modeling, and CLSM images.
Authors: Li Y, Wang C, Wang J, Chu T, Zhao L, Zhao L Abstract The present study aimed to evaluate the penetration activity of O-acylterpineol derivatives both in vitro and in vivo, and to investigate the enhancing mechanism of O-acylterpineol derivatives which were synthesized by α-terpineol and fatty acid. The promoting activities on the isosorbide dinitrate patch were tested across full thickness rabbit skin both in vitro and in vivo. In order to elucidate the permeation mechanism, attenuated total reflection Fourier transform infrared spectroscopy, molecular modeling, and confocal laser scanning microscopy...
Source: Drug Delivery - February 14, 2019 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Self-assembled angiopep-2 modified lipid-poly (hypoxic radiosensitized polyprodrug) nanoparticles delivery TMZ for glioma synergistic TMZ and RT therapy.
In this study, we prepared angiopep-2 (A2) modified lipid-poly (hypoxic radiosensitized polyprodrug) nanoparticles for TMZ delivery (A2-P(MIs)25/TMZ) to achieve synergistic effects against glioma. This A2-P(MIs)25/TMZ display highly promising advantages: (1) a hydrophobic P-(MIs)25 core where poorly water-soluble TMZ can be encapsulated; (2) nitro groups of the hydrophobic P-(MIs)25 core that are converted into hydrophilic amino groups (P(NH2s)25) under low oxygen conditions to mimic the oxygen-increased sensitization to RT; (3) a lipid monolayer at the interface of the core and the shell to modify the A2 (a specific ligan...
Source: Drug Delivery - February 14, 2019 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Efficient exosome delivery in refractory tissues assisted by ultrasound-targeted microbubble destruction.
In this study, we explore the possibility that UTMD assists exosome delivery in these intrinsically resistant tissues. Mice were subjected to tail vein injection of DiR-labeled exosomes together with/without UTMD of SonoVueTM, followed by in vivo and ex vivo tracking of the exosomes. As expected, heart, adipose tissue, and skeletal muscle were found reluctant to exosomes from different origins. Targeted destruction of the ultrasound microbubbles (SonoVueTM) in the heart and adipose tissue region significantly increased the exosome infiltration and endocytosis there, as revealed by fluorescence imaging and confocal laser sc...
Source: Drug Delivery - February 14, 2019 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Improved drug targeting to liver tumor by sorafenib-loaded folate-decorated bovine serum albumin nanoparticles.
CONCLUSION: FA-modified albumin nanoparticles are good carriers for delivering SRF to the tumor tissue, which can improve the therapeutic effect and reduce the side effects of the drug. PMID: 30744448 [PubMed - in process] (Source: Drug Delivery)
Source: Drug Delivery - February 14, 2019 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Intranasal administration of erythropoietin rescues the photoreceptors in degenerative retina: a noninvasive method to deliver drugs to the eye.
Authors: Tao Y, Li C, Yao A, Qu Y, Qin L, Xiong Z, Zhang J, Wang W Abstract Inherited retinopathies typically lead to photoreceptor loss and severe visual impairments in the subjects. Intranasal administration is an efficient approach to deliver therapeutic agents to the targeted tissue. The present study is designed to deliver the erythropoietin (EPO) into the N-methyl-N-nitrosourea (MNU) induced mice, a pharmacological retinopathy model via intranasal or intravenous route. The mice were then subjected to bioavailability assay and therapeutic effects evaluation. Our results showed that the intranasal delivery of E...
Source: Drug Delivery - February 14, 2019 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Enhanced chemotherapeutic efficacy of the low-dose doxorubicin in breast cancer via nanoparticle delivery system crosslinked hyaluronic acid.
In this study, we further investigated the antitumor effect of X-NP-DOX NP delivery system using low-dose DOX in both in vitro and in vivo systems. We demonstrated that low-dose X-NP-DOX possessed the ability for inhibiting MCF-7 breast cancer cell growth, invasion, and migration, and inducing apoptosis in vitro. In in vivo experiments, injection of low-dose X-NP-DOX into tumor-bearing mouse resulted in significant reduction of tumor size. Terminal deoxynucleotidyl transferase-mediated dUTP nick end labeling staining further revealed that low-dose X-NP-DOX induced higher percentage of apoptotic cells compared with free DOX...
Source: Drug Delivery - January 31, 2019 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Photodynamic therapy - hypericin tetraether liposome conjugates and their antitumor and antiangiogenic activity.
Authors: Plenagl N, Duse L, Seitz BS, Goergen N, Pinnapireddy SR, Jedelska J, Brüßler J, Bakowsky U Abstract Photodynamic therapy (PDT) is an established noninvasive tumor treatment. The hydrophobic natural occurring pigment hypericin shows a lot of attractive properties for the application in PDT. Hence, the administration to biological systems or patients requires the formulation in drug carriers enabling sufficient bioavailability. Therefore, free hypericin was encapsulated by the thin film hydration method or a hypericin-hydroxypropyl-β-cyclodextrin inclusion complex (Hyp-HPβCD) was incorpo...
Source: Drug Delivery - January 31, 2019 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Identification and imaging of miR-155 in the early screening of lung cancer by targeted delivery of octreotide-conjugated chitosan-molecular beacon nanoparticles.
In this study, lung cancer cells, subcutaneous xenografts of lung cancer in nude mice, and Lox-Stop-lox K-ras G12D transgenic mice were used as models. The transgenic mice displayed the dynamic processes from normal lung tissue to atypical hyperplasia, adenomas, carcinoma in situ and lung adenocarcinoma. It was found that miR-155 and somatostatin receptor 2 (SSTR2) were expressed in all the disease stages of transgenic mice. Through molecular beacon (MB) technology and nanotechnology, chitosan-molecular beacon (CS-MB) nanoparticles and targeted octreotide (OCT) were conjugated and synthesized. The octreotide-conjugated chi...
Source: Drug Delivery - January 11, 2019 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Antitumor activities of novel glycyrrhetinic acid-modified curcumin-loaded cationic liposomes in vitro and in H22 tumor-bearing mice.
In this study, we presented a novel delivery system - the glycyrrhetinic acid modified curcumin-loaded cationic liposomes (GAMCLCL) and investigated its antitumor activities on HepG2 cells in vitro and in H22 tumor-bearing mice. The experimental results demonstrated that GAMCLCL was a cationic liposome and could be Intravenous administration. Compared to free curcumin, GAMCLCL exhibited stronger antitumor activities in vitro and in vivo. The antitumor results of GAMCLCL after intravenous administration were very similar to those after intratumoral administration. The main activities of GAMCLCL and curcumin included inhibit...
Source: Drug Delivery - December 2, 2018 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Development of dual-drug-loaded stealth nanocarriers for targeted and synergistic anti-lung cancer efficacy.
Authors: Chen J, Yang X, Huang L, Lai H, Gan C, Luo X Abstract Combination chemotherapy is widely exploited for suppressing drug resistance and achieving synergistic anticancer efficacy in the clinic. In this paper, the nanostructured targeting methotrexate (MTX) plus pemetrexed (PMX) chitosan nanoparticles (CNPs) were developed by modifying methoxy polye (thylene glycol) (mPEG), in which PEGylation CNPs was used as stealth nanocarriers (PCNPs) and MTX was employed as a targeting ligand and chemotherapeutic agent as well. Studies were undertaken on human lung adenocarcinoma epithelial (A549) and Lewis lung carcinom...
Source: Drug Delivery - November 27, 2018 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Laser-assisted delivery enhances topical uptake of the anticancer agent cisplatin.
Authors: Wenande E, Olesen UH, Boesen MR, Persson DP, Lerche CM, Stürup S, Gammelgaard B, Husted S, Anderson RR, Haedersdal M Abstract Systemic chemotherapy with the anticancer agent cisplatin is approved for advanced non-melanoma skin cancer (NMSC), but topical treatment is limited by insufficient cutaneous penetration. We studied the impact of ablative fractional laser (AFL) exposure on topical cisplatin's pharmacokinetics and biodistribution in skin, using microscopic ablation zones reaching the mid- (MAZ-MD; 620 μm depth) and deep dermis (MAZ-DD; 912 μm depth) (λ = ...
Source: Drug Delivery - November 27, 2018 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Dual-modified natural high density lipoprotein particles for systemic glioma-targeting drug delivery.
Authors: Cui L, Wang Y, Liang M, Chu X, Fu S, Gao C, Liu Q, Gong W, Yang M, Li Z, Yu L, Yang C, Su Z, Xie X, Yang Y, Gao C Abstract Therapeutic outcome for the treatment of glioma was often limited due to the two barriers involved: the blood-brain barrier (BBB) and blood-brain tumor barrier (BBTB). Therefore, the development of nanocarriers that possess both BBB and BBTB permeability and glioma-targeting ability is of great importance for the chemotherapy of glioma. New frontiers in nanomedicine are advancing the research of new biomaterials. Here we constructed a natural high-density lipoprotein particle (HDL)-bas...
Source: Drug Delivery - November 27, 2018 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Multistage delivery of CDs-DOX/ICG-loaded liposome for highly penetration and effective chemo-photothermal combination therapy.
Authors: Xue X, Fang T, Yin L, Jiang J, He Y, Dai Y, Wang D Abstract Nanoparticles (NPs) have proven to be effective drug carriers in diagnosis and therapy of cancer. But, they faced a contradictory issue that NPs with large size appear weak tumor penetration, meanwhile small size resulted in poor tumor retention. Herein, we fabricated doxorubicin conjugated carbon dots (CDs-DOX) and indocyanine green (ICG)-loaded liposomes (ICG-LPs) named CDs-ICG-LPs using a modified reverse phase evaporation process, and with high incorporation in the aqueous core. The CDs-ICG-LPs exhibited good monodispersity, excellent fluoresc...
Source: Drug Delivery - November 23, 2018 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Effects of solvents and penetration enhancers on transdermal delivery of thymoquinone: permeability and skin deposition study.
Authors: Haq A, Michniak-Kohn B Abstract Thymoquinone (TQ) is a quinone-based phytochemical that was first identified in 1963 in Nigella sativa (black cumin seed) by El-Dakhakhany. Based on the ideal characteristics of transdermal delivery, TQ is potentially an attractive candidate for transdermal drug delivery. The aim of this study was to investigate the feasibility of transdermal delivery of TQ and to assess the effect of an ethanol and propylene glycol donor solvent system along with various compositions of receptor solvents. The effects of penetration enhancers on the in vitro skin permeation and TQ skin absor...
Source: Drug Delivery - November 23, 2018 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Designing multifunctional cancer-targeted nanosystem for magnetic resonance molecular imaging-guided theranostics of lung cancer.
Authors: Gao P, Mei C, He L, Xiao Z, Chan L, Zhang D, Shi C, Chen T, Luo L Abstract The integration of diagnosis and therapy is an effective way to improve therapeutic effects for cancer patients, which has acquired widely attentions from researchers. Herein, a multifunctional drug-loaded nanosystem (F/A-PLGA@DOX/SPIO) has been designed and synthesized to reduce the side effects of traditional chemotherapy drugs and realize simultaneous tumor diagnosis and treatment. The surface modification of folic acid (FA) and activatable cell-penetrating peptide (ACPP) endows the nanosystem with excellent cancer targeting capa...
Source: Drug Delivery - November 23, 2018 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Primary M1 macrophages as multifunctional carrier combined with PLGA nanoparticle delivering anticancer drug for efficient glioma therapy.
In conclusion, the results provided a new strategy exploiting M1 macrophage as carrier for drug delivery, which improved targeting efficiency and therapeutic efficacy of chemodrugs for glioma therapy. PMID: 30465444 [PubMed - in process] (Source: Drug Delivery)
Source: Drug Delivery - November 23, 2018 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Design, characterization and in vivo evaluation of nanostructured lipid carriers (NLC) as a new drug delivery system for hydrochlorothiazide oral administration in pediatric therapy.
Authors: Cirri M, Maestrini L, Maestrelli F, Mennini N, Mura P, Ghelardini C, Di Cesare Mannelli L Abstract The hydrochlorothiazide (HCT) low solubility and permeability give rise to limited and variable bioavailability; its low stability makes it difficult to develop stable aqueous liquid formulations; its low dose makes the achievement of a homogeneous drug distribution very difficult. Thus, the aim of this study was to investigate the effectiveness of a strategy based on the development of nanostructured lipid carriers (NLC) as an innovative oral pediatric formulation of HCT with improved therapeutic efficacy. T...
Source: Drug Delivery - November 20, 2018 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

A Bayesian network meta-analysis on the efficacy and safety of eighteen targeted drugs or drug combinations for pulmonary arterial hypertension.
Authors: Wang S, Yu M, Zheng X, Dong S Abstract Pulmonary arterial hypertension (PAH) can be relieved by pharmacological interventions, especially the targeted drug, which is classified into endothelin receptor antagonist, phosphodiesterase 5 inhibitor, prostaglandin I2, soluble guanylate cyclase stimulator and selective non-prostanoid prostacyclin receptor agonist. To solve the contradictions existing in reported trials and provide a comprehensive guideline for clinical practice. PubMed, Embase, Cochrane library, and clinicaltrials.gov were searched. The basic information about the article, trial, arm, interventio...
Source: Drug Delivery - November 19, 2018 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Solutol HS15 based binary mixed micelles with penetration enhancers for augmented corneal delivery of sertaconazole nitrate: optimization, in vitro, ex vivo and in vivo characterization.
Authors: Younes NF, Abdel-Halim SA, Elassasy AI Abstract Keratomycosis is a serious corneal disease that can cause a permanent visual disability if not treated effectively. Sertaconazole nitrate (STZ), a novel broad spectrum antifungal drug, was suggested as a promising treatment. However, its utility in the ocular route is restricted by its poor solubility, along with other problems facing the ocular delivery like short residence time, and the existing corneal barrier. Therefore, the objective of this study was to formulate STZ loaded binary mixed micelles (STZ-MMs) enriched with different penetration enhancers us...
Source: Drug Delivery - November 19, 2018 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Potential combination topical therapy of anal fissure: development, evaluation, and clinical study †.
Potential combination topical therapy of anal fissure: development, evaluation, and clinical study†. Drug Deliv. 2018 Nov;25(1):1672-1682 Authors: Salem AE, Mohamed EA, Elghadban HM, Abdelghani GM Abstract To treat anal fissure, internal anal sphincterotomy may be associated with surgical risks and incidence of incontinence. Botulinum toxin injection into the anal sphincter is invasive and expensive. Headache and hypotension hindered topical treatment with glyceryl trinitrate. Greater patient compliance, potentiated efficacy, reduced side effects, and lower cost are the major advantages offered ...
Source: Drug Delivery - November 17, 2018 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Brain-targeted delivery of PEGylated nano-bacitracin A against Penicillin-sensitive and -resistant Pneumococcal meningitis: formulated with RVG29 and Pluronic ® P85 unimers.
In this study, the potential application of this micelle for the treatment of both Penicillin-sensitive and -resistant PM was studied. To address BBB-targeting and -crossing issues, PEGylated Nano-BA12K was formulated with a specific brain-targeting peptide (rabies virus glycopeptide-29, RVG29) and a P-glycoprotein inhibitor (Pluronic® P85 unimers) to construct a mixed micellar system (RVG29-Nano-BAP85). RVG29-Nano-BAP85 demonstrated a strong antibacterial potency against 13 clinical isolates of S. pneumonia, even higher than that of Penicillin G, a conventional anti-PM agent. RVG29-Nano-BAP85 had more cellular uptake ...
Source: Drug Delivery - November 10, 2018 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

PD-1/PD-L1 pathway and angiogenesis dual recognizable nanoparticles for enhancing chemotherapy of malignant cancer.
Authors: Sun Z, Zhang Y, Cao D, Wang X, Yan X, Li H, Huang L, Qu X, Kong C, Qin H, Wang M, Xu W, Liang L Abstract Although the cancer immunotherapy represents one of the most promising strategies for cancer treatment, the PD-1/PD-L1 pathway, which involves a receptor-ligand interaction, can induced immunosuppression by disabling tumor-infiltrating lymphocytes (TILs). In the present study, we coupled a PD-L1 (Programmed cell death 1 ligand 1) recognizable peptide DPPA-1 to the sequence of CGKRK, a namely tumor vasculature affinity peptide, to form a new molecule CD peptide. Thereafter, the paclitaxel (PTX)-loaded PC...
Source: Drug Delivery - November 6, 2018 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

The challenges of oral drug delivery via nanocarriers.
Authors: Reinholz J, Landfester K, Mailänder V Abstract The oral application of pharmaceuticals is unarguably the most convenient method of application. Especially for protein- or peptide-based drugs, however, the effectiveness is significantly reduced due to enzymatic digestion in the stomach as well as a poor bioavailability in the small intestine. For these difficult formulations, the encapsulation into nanocarriers would protect the sensitive drug and thus could considerably improve the efficiency of oral drug delivery. In the last years, many candidate biodegradable nanomaterials for such carrier systems ...
Source: Drug Delivery - November 6, 2018 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Enhanced blood-brain barrier penetration and glioma therapy mediated by T7 peptide-modified low-density lipoprotein particles.
In this study, we demonstrate a strategy for glioma targeting by encapsulating vincristine sulfate (VCR) into a naturally available low-density lipoprotein particles (LDL)-based drug delivery system with the modification of T7 peptide ligand (T7-LDL). LDL, endogenous lipid transporters, can specifically bind to brain endothelial cells and glioma cells via interacting with the low-density lipoprotein receptors (LDLR). T7 is a seven-peptide ligand of transferrin receptors (TfR) capable of circumventing the BBB and then targeting glioma. By combining the dual-targeting delivery effect of T7 peptide and parent LDL, T7-LDL disp...
Source: Drug Delivery - November 6, 2018 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Dual-mode imaging and therapeutic effects of drug-loaded phase-transition nanoparticles combined with near-infrared laser and low-intensity ultrasound on ovarian cancer.
Authors: Chen S, Liu Y, Zhu S, Chen C, Xie W, Xiao L, Zhu Y, Hao L, Wang Z, Sun J, Chang S Abstract Chemotherapy and photo-sonodynamic therapy (PSDT) can be combined through drug delivery nano-platforms to enhance the anti-tumor efficacy, however, which is limited by hypoxia in tumor, thereby causing chemotherapy resistance. Perfluoropentane (PFP) has the ability to carry oxygen and to enhance ultrasound or photoacoustic imaging after vaporization. Herein, we constructed a kind of nanoparticles (PTX/ICG and oxygen loaded PLGA nanoparticles (PIO_NPs)), which had PFP core carrying oxygen and PLGA shell loaded indocya...
Source: Drug Delivery - October 24, 2018 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Ganoderma lucidum-derived polysaccharide enhances coix oil-based microemulsion on stability and lung cancer-targeted therapy.
Authors: Guo J, Yuan C, Huang M, Liu Y, Chen Y, Liu C, Chen Y Abstract The aim of this study is to explore the influence of Ganoderma lucidum-derived polysaccharides (GLP) to coix oil-based microemulsion on pharmaceutical performance and anti-lung cancer treatment. GLP-integrated coix oil-based microemulsion (MEs(PS-GLP)) exhibited a clear spherical shape, small particle size, and good hydrodynamics similar to the coix oil-based microemulsion, but showed a lower zeta potential and a better stability. Fluorescence resonance energy transfer analysis presented that GLP was integrated with microemulsion as a single sys...
Source: Drug Delivery - October 24, 2018 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Stacking of doxorubicin on folic acid-targeted multiwalled carbon nanotubes for in vivo chemotherapy of tumors.
Authors: Yan Y, Wang R, Hu Y, Sun R, Song T, Shi X, Yin S Abstract In this work, we developed a novel active targeting and pH-responsive system for delivering the drug doxorubicin (DOX) to tumor sites using folic acid (FA)-modified multiwalled carbon nanotubes (MWCNTs). Acid-treated MWCNTs with carboxyl groups were first covalently conjugated with polyethyleneimine (PEI). Subsequent sequential modification with FA (via a polyethylene glycol spacer), fluorescein isothiocyanate (FI), and acetic anhydride/triethylamine resulted in multifunctional FA-bound MWCNT (MWCNT-PEI.Ac-FI-PEG-FA) nanomaterials that possessed exc...
Source: Drug Delivery - October 24, 2018 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Borneol, a messenger agent, improves central nervous system drug delivery through enhancing blood-brain barrier permeability: a preclinical systematic review and meta-analysis.
In conclusion, borneol is a promising candidate for CNS drug delivery, mainly through mediating a multi-targeted BBB permeability. PMID: 30334462 [PubMed - in process] (Source: Drug Delivery)
Source: Drug Delivery - October 21, 2018 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

A novel redox/pH dual-responsive and hyaluronic acid-decorated multifunctional magnetic complex micelle for targeted gambogic acid delivery for the treatment of triple negative breast cancer.
Authors: Sang MM, Liu FL, Wang Y, Luo RJ, Huan XX, Han LF, Zhang ZT, Feng F, Qu W, Liu W, Zheng F Abstract Gambogic acid (GA) is a naturally derived potent anticancer agent with extremely poor biocompatibility. In the present study, a novel of redox/pH dual-responsive multifunctional magnetic complex micelle (sPEG/HA/CSO-SS-Hex/Fe3O4/GA), which consisted of a reducible hexadecanol-modified chitosan oligosaccharide polymer micelle (CSO-SS-Hex) coated with hyaluronic acid (HA) and DCA grafted sheddable PEG-PLL (sPEG) copolymers and loaded with gambogic acid (GA) and Fe3O4 nanoparticles were developed for parenteral d...
Source: Drug Delivery - October 21, 2018 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Borneol and Α-asarone as adjuvant agents for improving blood-brain barrier permeability of puerarin and tetramethylpyrazine by activating adenosine receptors.
In this study, we aimed to first evaluate the 'orifice-opening' effect of borneol and α-asarone, both aromatic resuscitation drugs, on improvement of brain delivery of PUE and TMP and second to investigate whether the enhancing effects were associated with adenosine receptors (ARs)-mediated trans-BBB pathway. In vitro BBB model was established and borneol and α-asarone significantly increased the cumulative amount of permeated PUE and TMP and the enhancing effects could be counteracted by AR inhibitors. Borneol and α-asarone could decrease expression of ZO-1, an important BBB junction protein, but inverse...
Source: Drug Delivery - October 21, 2018 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Development and characterization of sorafenib-loaded lipid nanocapsules for the treatment of glioblastoma.
Authors: Clavreul A, Roger E, Pourbaghi-Masouleh M, Lemaire L, Tétaud C, Menei P Abstract Anticancer agents that target both tumor cells and angiogenesis are of potential interest for glioblastoma (GB) therapy. One such agent is sorafenib (SFN), a tyrosine kinase inhibitor. However, poor aqueous solubility and undesirable side effects limit its clinical application, including local treatment. We encapsulated SFN in lipid nanocapsules (LNCs) to overcome these drawbacks. LNCs are nanocarriers formulated according to a solvent-free process, using only components that have received regulatory approval. SFN-LNCs ...
Source: Drug Delivery - October 21, 2018 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Co-delivery of deferoxamine and hydroxysafflor yellow A to accelerate diabetic wound healing via enhanced angiogenesis.
In conclusion, combination of pro-angiogenic small molecule DFO and HSYA in hydrogel provides a promising strategy to productively promote diabetic wound healing as well as better the repair quality. PMID: 30338719 [PubMed - in process] (Source: Drug Delivery)
Source: Drug Delivery - October 21, 2018 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

A journey from the endothelium to the tumor tissue: distinct behavior between PEO-PCL micelles and polymersomes nanocarriers.
This study assessed the in vitro and in vivo passage through the blood vessel wall to tumors of two well-characterized polymeric nanocarriers: poly(ethyleneglycol-b-ε-caprolactone) micelles and polymersomes charged with a fluorescent membrane dye (DiO: 3,3'-dioctadecyloxacarbo-cyanine perchlorate). The internalization and translocation from endothelial (human primary endothelial cells HUVEC) to cancer cells (human tumor cell line HCT-116) was studied in conventional 2D monolayers, 3D tumor spheroids, or in an endothelium model based on transwell assay. Micelles induced a faster DiO internalization compared to polym...
Source: Drug Delivery - October 14, 2018 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Dual-modified cationic liposomes loaded with paclitaxel and survivin siRNA for targeted imaging and therapy of cancer stem cells in brain glioma.
In conclusion, prepared DP-CLPs-PTX-siRNA nanocomplex selectively induced CD133+ glioma stem cell apoptosis in vitro and in vivo exhibits great potential for targeted imaging and therapy of brain glioma stem cells. PMID: 30269613 [PubMed - in process] (Source: Drug Delivery)
Source: Drug Delivery - October 3, 2018 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Enhanced gene transfection efficiency by low-dose 25  kDa polyethylenimine by the assistance of 1.8 kDa polyethylenimine.
This study presents an efficient and safe combined PEI-based non-viral gene delivery strategy with potential for in vivo applications. PMID: 30241446 [PubMed - in process] (Source: Drug Delivery)
Source: Drug Delivery - September 24, 2018 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Touch-actuated microneedle array patch for closed-loop transdermal drug delivery.
Authors: Yang J, Chen Z, Ye R, Li J, Lin Y, Gao J, Ren L, Liu B, Jiang L Abstract To date, only approximately 20 drugs synthesized with small molecules have been approved by the FDA for use in traditional transdermal patches (TTP) owing to the extremely low permeation rate of the skin barrier for macromolecular drugs. A novel touch-actuated microneedle array patch (TMAP) was developed for transdermal delivery of liquid macromolecular drugs. TMAP is a combination of a typical TTP and a solid microneedle array (MA). High doses of liquid drug formulations, especially heat-sensitive compounds can be easily filled and s...
Source: Drug Delivery - September 7, 2018 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

A local drug delivery system based on visible light-cured glycol chitosan and doxorubicin ⋅hydrochloride for thyroid cancer treatment in vitro and in vivo.
In this study, we investigated the feasibility of a local DDS (LDDS) based on visible light-cured glycol chitosan (GC) hydrogel and doxorubicin⋅hydrochloride (DOX⋅HCl), called GC10/DOX, on thyroid cancer treatment in vivo. Visible light irradiation increased the storage modulus and swelling ratio of the GC10/DOX hydrogel precursor. The release of DOX⋅HCl from GC10/DOX exhibited two unique patterns comprising an initial burst within 18 hours, followed by a controlled and sustained release thereafter. In vitro cell viability testing showed that GC10/DOX had a greater antitumor effect than free DOX⋅...
Source: Drug Delivery - September 7, 2018 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Nose-to-brain delivery of temozolomide-loaded PLGA nanoparticles functionalized with anti-EPHA3 for glioblastoma targeting.
Authors: Chu L, Wang A, Ni L, Yan X, Song Y, Zhao M, Sun K, Mu H, Liu S, Wu Z, Zhang C Abstract Glioblastoma is the most common malignant brain tumor. Efficient delivery of drugs targeting glioblastomas remains a challenge. Ephrin type-A receptor 3 (EPHA3) tyrosine kinase antibody-modified polylactide-co-glycolide (PLGA) nanoparticles (NPs) were developed to target glioblastoma via nose-to-brain delivery. Anti-EPHA3-modified, TBE-loaded NPs were prepared using an emulsion-solvent evaporation method, showed a sustained in vitro release profile up to 48 h and a mean particle size of 145.9 ± 8.7 nm. The cellula...
Source: Drug Delivery - September 6, 2018 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Curcumin-loaded PLGA-PEG nanoparticles conjugated with B6 peptide for potential use in Alzheimer's disease.
Authors: Fan S, Zheng Y, Liu X, Fang W, Chen X, Liao W, Jing X, Lei M, Tao E, Ma Q, Zhang X, Guo R, Liu J Abstract Alzheimer's disease is a neurodegenerative disorder mainly characterized by β-amyloid deposit and tau hyperphosphorylation with no curative treatments. Curcumin (Cur) has been proved to have potential use in Alzheimer's disease with its anti-amyloid, anti-inflammatory, and anti-oxidant properties, etc. However, its hydrophobicity and low bioavailability hinder its application. In this paper, we designed a novel brain-target nanoparticle, poly(lactide-co-glycolide)-block-poly(ethylene glycol) (PLGA...
Source: Drug Delivery - August 17, 2018 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Sodium stibogluconate loaded nano-deformable liposomes for topical treatment of leishmaniasis: macrophage as a target cell.
Authors: Dar MJ, Din FU, Khan GM Abstract Topical drug delivery against cutaneous leishmaniasis (CL) signifies an effective alternate for improving the availability and reducing the toxicity associated with the parenteral administration of conventional sodium stibogluconate (SSG) injection. The basic aim of the study was to develop nano-deformable liposomes (NDLs) for the dermal delivery of SSG against CL. NDLs were formulated by a modified thin film hydration method and optimized via Box-Behnken statistical design. The physicochemical properties of SSG-NDLs were established in terms of vesicle size (195.1 n...
Source: Drug Delivery - August 15, 2018 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Efficient treatment of Parkinson's disease using ultrasonography-guided rhFGF20 proteoliposomes.
Authors: Niu J, Xie J, Guo K, Zhang X, Xia F, Zhao X, Song L, Zhuge D, Li X, Zhao Y, Huang Z Abstract Fibroblast growth factor-20 (FGF20) is a paracrine member of the FGF family that is preferentially expressed in the substantia nigra pars compacta (SNpc). Previous studies have demonstrated that FGF20 enhances the survival of dopaminergic neurons suggesting the potential use of FGF20 to treat Parkinson's disease (PD). However, the reduced solubility of the bacterial recombinant human FGF20 (rhFGF20) and the absence of efficient strategies to transport rhFGF20 across the blood-brain barrier (BBB) have halted its cli...
Source: Drug Delivery - July 26, 2018 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Intravenous delivery of a liposomal formulation of voriconazole improves drug pharmacokinetics, tissue distribution, and enhances antifungal activity.
Authors: Veloso DFMC, Benedetti NIGM, Ávila RI, Bastos TSA, Silva TC, Silva MRR, Batista AC, Valadares MC, Lima EM Abstract Voriconazole (VCZ), a triazole with a large spectrum of action is one of the most recommended antifungal agents as the first line therapy against several clinically important systemic fungal infections, including those by Candida albicans. This antifungal has moderate water solubility and exhibits a nonlinear pharmacokinetic (PK) profile. By entrapping VCZ into liposomes, it is possible to circumvent certain downsides of the currently available product such as a reduction in the rate of...
Source: Drug Delivery - July 26, 2018 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Modified translationally controlled tumor protein-derived protein transduction domain enhances nasal delivery of exendin-4 as shown with insulin.
In this study, we applied this approach to the nasal delivery of a different peptide, exendin-4, using as carriers, several modified TCTP-PTDs, such as TCTP-PTD 13M1, 13M2, and 13M3. Nasal co-administration of TCTP-PTD 13M2 with exendin-4 showed the highest exendin-4 uptake among the three analogs in normal rats, and also decreased blood glucose levels by 43.3% compared with that of exendin-4 alone and by 18.6% compared with that of exendin-4 plus TCTP-PTD 13 in diabetic mice. We also designed an additional covalently linked conjugate of TCTP-PTD 13M2 and exendin-4 and evaluated its hypoglycemic effect after subcutaneous o...
Source: Drug Delivery - July 26, 2018 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Self-assembled PEGylated albumin nanoparticles (SPAN) as a platform for cancer chemotherapy and imaging.
Authors: Lee JE, Kim MG, Jang YL, Lee MS, Kim NW, Yin Y, Lee JH, Lim SY, Park JW, Kim J, Lee DS, Kim SH, Jeong JH Abstract Paclitaxel (PTX) is used as a major antitumor agent for the treatment of recurrent and metastatic breast cancer. For the clinical application of PTX, it needs to be dissolved in an oil/detergent-based solvent due to its poor solubility in an aqueous medium. However, the formulation often causes undesirable complications including hypersensitivity reactions and limited tumor distribution, resulting in a lower dose-dependent antitumor effect. Herein, we introduce a facile and oil-free method to p...
Source: Drug Delivery - July 26, 2018 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Superior anti-neoplastic activities of triacontanol-PEG conjugate: synthesis, characterization and biological evaluations.
Authors: Zhou Y, Li N, Qiu Z, Lu X, Fang M, Chen X, Ren L, Wang G, Ouyang P Abstract Triacontanol (TA, C30H62O), abundantly present in plant cuticle waxes and bee waxes, has been found to display promising anti-neoplastic potentials. As a long chain fatty alcohol, TA possesses limited aqueous solubility, which hinders its medicinal application. To overcome its solubility barrier, a polymer prodrug was synthesized through attaching TA to poly ethylene glycol (PEG), using succinic acid as a linker with bifunctional amide and ester bonds. Anti-neoplastic effects of PEG-TA were assessed in LoVo and MCF7 cells, anti-pro...
Source: Drug Delivery - July 21, 2018 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Porous silicon based intravitreal platform for dual-drug loading and controlled release towards synergistic therapy.
This study demonstrates the use of porous silicon (pSi) particles sequentially loaded with daunorubicin (DNR) and dexamethasone (DEX) to create a synergistic intravitreally injectable dual-drug delivery system. DEX targets chronic inflammation while DNR inhibits excessive cell proliferation as well as suppresses hypoxia-inducible factor 1 to reduce scarring. This pSi-based delivery system releases therapeutic concentrations of DNR for 100 days and DEX for over 165 days after a single dose. This intravitreal dual-drug delivery system is also well tolerated after injection into the rabbit eye model, attested by...
Source: Drug Delivery - July 13, 2018 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research