Co-drug delivery of regorafenib and cisplatin with amphiphilic copolymer nanoparticles: enhanced in  vivo antitumor cancer therapy in nursing care.
Co-drug delivery of regorafenib and cisplatin with amphiphilic copolymer nanoparticles: enhanced in vivo antitumor cancer therapy in nursing care. Drug Deliv. 2020 Dec;27(1):1319-1328 Authors: Zhou Z Abstract Cancers continue to be the second leading cause of death worldwide. Despite the development and improvement of surgery, chemotherapy and radiotherapy in cancer management, effective tumor ablation strategies are still in need due to high cancer patient mortality. Hence, we have established a new approach to achieve treatment-actuated modifications in a tumor microenvironment by using synergis...
Source: Drug Delivery - September 17, 2020 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Apatinib-loaded CalliSpheres Beads for embolization in a rabbit VX2 liver tumor: characterization in  vitro, pharmacokinetics and tumor response in vivo.
In conclusion, these findings provide a basis for the potential application of apatinib-loaded CalliSpheres Beads in liver cancer. PMID: 32924634 [PubMed - in process] (Source: Drug Delivery)
Source: Drug Delivery - September 16, 2020 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Type I collagen hydrogels as a delivery matrix for royal jelly derived extracellular vesicles.
Authors: Ramírez OJ, Alvarez S, Contreras-Kallens P, Barrera NP, Aguayo S, Schuh CMAP Abstract Throughout the last decade, extracellular vesicles (EVs) have become increasingly popular in several areas of regenerative medicine. Recently, Apis mellifera royal jelly EVs (RJ EVs) were shown to display favorable wound healing properties such as stimulation of mesenchymal stem cell migration and inhibition of staphylococcal biofilms. However, the sustained and effective local delivery of EVs in non-systemic approaches - such as patches for chronic cutaneous wounds - remains an important challenge for the developm...
Source: Drug Delivery - September 16, 2020 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

A promising drug delivery candidate (CS-g-PMDA-CYS-fused gold nanoparticles) for inhibition of multidrug-resistant uropathogenic Serratia marcescens.
Authors: Shi P, Amarnath Praphakar R, Deepa S, Suganya K, Gupta P, Ullah R, Bari A, Murugan M, Rajan M Abstract Antibiotic resistance amongst microbial pathogens is a mounting serious issue in researchers and physicians. Various alternatives to overcome the multidrug-resistant bacterial infections are under search, and biofilm growth inhibition is one of them. In this investigation, a polymeric drug delivery system loaded with multi-serratial drugs to improve the delivery of drugs against urinary tract infection causative Serratia marcescens. The chitosan grafted pyromellitic dianhydride - cysteine (CS-g-PMDA-CYS) ...
Source: Drug Delivery - September 6, 2020 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Long-term sustained release Poly(lactic-co-glycolic acid) microspheres of asenapine maleate with improved bioavailability for chronic neuropsychiatric diseases.
Authors: Zhai J, Wang YE, Zhou X, Ma Y, Guan S Abstract Schizophrenia and bipolar disorder are severe chronic neuropsychiatric diseases, affecting hundreds of millions of people worldwide. Asenapine maleate (ASM) has been demonstrated as a safe and effective therapeutic agent under twice-daily administration. However, lower compliance is observed when patients are treated with ASM, which significantly limits its application in schizophrenia and bipolar disorder. Moreover, the low bioavailability of ASM caused by first-pass metabolism and poor aqueous solubility also impairs the treatment effect. A formulation of AS...
Source: Drug Delivery - September 6, 2020 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Supersaturable organic-inorganic hybrid matrix based on well-ordered mesoporous silica to improve the bioavailability of water insoluble drugs.
In conclusion, the supersaturated organic-inorganic hybrid matrix can serve as a modular strategy to enhance the oral availability of water insoluble drugs. PMID: 32885715 [PubMed - in process] (Source: Drug Delivery)
Source: Drug Delivery - September 6, 2020 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Modulating barriers of tumor microenvironment through nanocarrier systems for improved cancer immunotherapy: a review of current status and future perspective.
Authors: Lan H, Zhang W, Jin K, Liu Y, Wang Z Abstract Cancer immunotherapy suppresses and destroys tumors by re-activating and sustaining the tumor-immune process, and thus improving the immune response of the body to the tumor. Immunotherapeutic strategies are showing promising results in pre-clinical and clinical trials, however, tumor microenvironment (TME) is extremely immunosuppressive. Thus, their translation from labs to clinics still faces issues. Recently, nanomaterial-based strategies have been developed to modulate the TME for robust immunotherapeutic responses. The combination of nanotechnology with im...
Source: Drug Delivery - September 2, 2020 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Enhanced antitumor activity of bovine lactoferrin through immobilization onto functionalized nano graphene oxide: an in  vitro/in vivo study.
This study aims to improve the anticancer activity of bovine lactoferrin through enhancing its stability by immobilization onto graphene oxide. Bovine lactoferrin was conjugated onto graphene oxide and the conjugation process was confirmed by FT-IR, SDS-PAGE, and UV spectrophotometry. Physical characterization was performed by DLS analysis and atomic force microscopy. The cytotoxicity and cellular uptake of the final construct (CGO-PEG-bLF) was inspected on lung cancer TC-1 cells by MTT assay and flow cytometry/confocal microscopy. The anticancer mechanism of the CGO-PEG-bLF was studied by cell cycle analysis, apoptosis as...
Source: Drug Delivery - August 21, 2020 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Functional differences between protamine preparations for the transfection of mRNA.
Authors: Jarzebska NT, Lauchli S, Iselin C, French LE, Johansen P, Guenova E, Kündig TM, Pascolo S Abstract Protamine is a natural cationic peptide mixture used as a drug for the neutralization of heparin and in formulations of slow-release insulin. In addition, Protamine can be used for the stabilization and delivery of nucleic acids (antisense, small interfering RNA (siRNA), immunostimulatory nucleic acids, plasmid DNA, or messenger RNA) and is therefore included in several compositions that are in clinical development. Notably, when mixed with RNA, protamine spontaneously generates particles in the siz...
Source: Drug Delivery - August 18, 2020 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Sustained delivery of 17 β-estradiol by human amniotic extracellular matrix (HAECM) scaffold integrated with PLGA microspheres for endometrium regeneration.
Sustained delivery of 17β-estradiol by human amniotic extracellular matrix (HAECM) scaffold integrated with PLGA microspheres for endometrium regeneration. Drug Deliv. 2020 Dec;27(1):1165-1175 Authors: Chen Y, Fei W, Zhao Y, Wang F, Zheng X, Luan X, Zheng C Abstract The endometrial injury usually results in intrauterine adhesions (IUAs). However, there is no effective treatment to promote the regeneration of the endometrium currently. The decellularized amnion membrane (AM) is a promising material in human tissue repair and regeneration due to its biocompatibility, biodegradability, as well as the...
Source: Drug Delivery - August 13, 2020 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Engineered bovine serum albumin-based nanoparticles with pH-sensitivity for doxorubicin delivery and controlled release.
Authors: Yang Z, Zhang N, Ma T, Liu L, Zhao L, Xie H Abstract In this work, we prepared a stimuli-responsive system for drug delivery and controlled release by engineering the bovine serum albumin (BSA). The doxorubicin (DOX)-loaded BSA nanoparticles (NPs) were conveniently prepared using desolvation method, followed by crosslinking through Schiff base bonds, leading to pH-sensitive DOX-loaded system (DOXs@BSA NPs). The resulted DOXs@BSA NPs showed high drug loading capacity (21.4%), and the particle size was about 130 nm with narrow polydispersity and high negative surface charge (-20.5 mV). The pH-s...
Source: Drug Delivery - August 13, 2020 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Thiopental sodium loaded solid lipid nano-particles attenuates obesity-induced cardiac dysfunction and cardiac hypertrophy via inactivation of inflammatory pathway.
Authors: Zhu C, Li W, Wang X, Xue J, Zhao L, Song Y, Zhou T, Zhang M Abstract This work evaluates solid lipid nanoparticles of thiopental sodium against obesity-induced cardiac dysfunction and hypertrophy and explores the possible mechanism of action. TS loaded SLNs were formulated by hot-homogenization and solvent diffusion method. TS-SLNs were scrutinized for entrapment efficiency, drug loading capacity, gastric stability, particle size, in vitro drug release. Mice were feed with the normal chow or high-fat diet for 08 weeks to induce obesity and primary cardiomyocytes. The therapeutic effects of thio...
Source: Drug Delivery - August 13, 2020 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

A comparative study on the in  vitro and in vivo antitumor efficacy of icaritin and hydrous icaritin nanorods.
A comparative study on the in vitro and in vivo antitumor efficacy of icaritin and hydrous icaritin nanorods. Drug Deliv. 2020 Dec;27(1):1176-1187 Authors: Li H, Li Y, Ao H, Fu J, Guo Y, Han M, Yan X, Chen X, Wang X Abstract Icaritin (ICT) and hydrous icaritin (HICT) are two similar flavonoids compounds isolated from Epimedium Genus. This is the first comparative study on their in vitro and in vivo antitumor effects. Nanorods (NRs) were prepared for ICT and HICT by anti-solvent precipitation method using D-alpha tocopherol acid polyethylene glycol succinate (TPGS) as a stabilizer. T...
Source: Drug Delivery - August 13, 2020 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Effect of nanostructured lipid carriers on transdermal delivery of tenoxicam in irradiated rats.
In conclusion, the present findings suggest that TNX-NLCs hydrogel could be a potential transdermal drug delivery system alternative to the oral formulation for the treatment of various inflammatory conditions. PMID: 32772730 [PubMed - in process] (Source: Drug Delivery)
Source: Drug Delivery - August 13, 2020 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Synthesis and toxicity assessment of Fe3O4 NPs grafted by  ∼ NH2-Schiff base as anticancer drug: modeling and proposed molecular mechanism through docking and molecular dynamic simulation.
Synthesis and toxicity assessment of Fe3O4 NPs grafted by ∼ NH2-Schiff base as anticancer drug: modeling and proposed molecular mechanism through docking and molecular dynamic simulation. Drug Deliv. 2020 Dec;27(1):1201-1217 Authors: Eshaghi Malekshah R, Fahimirad B, Aallaei M, Khaleghian A Abstract Superparamagnetic iron oxide nanoparticles have been synthesized using chain length of (3-aminopropyl) triethoxysilane for cancer therapy. First, we have developed a layer by layer functionalized with grafting 2,4-toluene diisocyanate as a bi-functional covalent linker onto a nano-Fe3O4 su...
Source: Drug Delivery - August 13, 2020 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Development, optimization, and evaluation of PEGylated brucine-loaded PLGA nanoparticles.
The objective of the current investigation was to develop and evaluate the passive targeting of long-circulating PLGA NPs loaded with BRU. NPs were characterized in terms of drug-excipient compatibility studies, including FTIR and DSC; physicochemical evaluations including particle size, zeta potential, morphological evaluation, entrapment efficiency and percentage yield; total serum protein adsorbed onto NP surfaces; and in vitro release of the loaded drug. Factorial design was employed to attain optimal PLGA-loaded NPs. Finally, the in vivo anti-tumor activity of BRU-loaded PLGA NPs was evaluated in tumor-beari...
Source: Drug Delivery - August 1, 2020 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Dissolving microneedles for transdermal delivery of huperzine A for the treatment of Alzheimer's disease.
Authors: Yan Q, Wang W, Weng J, Zhang Z, Yin L, Yang Q, Guo F, Wang X, Chen F, Yang G Abstract Increasingly attention has been paid to the transdermal drug delivery systems with microneedles owing to their excellent compliance, high efficiency, and controllable drug release, therefore, become promising alternative with tremendous advantages for delivering specific drugs such as huperzine A (Hup A) for treatment of Alzheimer's disease (AD) yet with low oral bioavailability. The purpose of the present study is to design, prepare, and evaluate a dissolving microneedle patch (DMNP) as a transdermal delivery system for ...
Source: Drug Delivery - August 1, 2020 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

A theoretical mathematical model for assessing diclofenac release from chitosan-based formulations.
Authors: Iftime MM, Dobreci DL, Irimiciuc SA, Agop M, Petrescu T, Doroftei B Abstract The paper reports a new mathematical model for understanding the mechanism delivery from drug release systems. To do this, two drug release systems based on chitosan and diclofenac sodium salt as a drug model, were prepared by in situ hydrogelation in the presence of salicylaldehyde. The morphology of the systems was analyzed by scanning electron microscopy and polarized light microscopy and the drug release was in vitro investigated into a medium mimicking the in vivo environment. The drug release mechanism was firstly ...
Source: Drug Delivery - July 30, 2020 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Polymeric micelles for the ocular delivery of triamcinolone acetonide: preparation and in  vivo evaluation in a rabbit ocular inflammatory model.
Polymeric micelles for the ocular delivery of triamcinolone acetonide: preparation and in vivo evaluation in a rabbit ocular inflammatory model. Drug Deliv. 2020 Dec;27(1):1115-1124 Authors: Safwat MA, Mansour HF, Hussein AK, Abdelwahab S, Soliman GM Abstract The aim of this study was to prepare triamcinolone acetonide (TA)-loaded poly(ethylene glycol)-block-poly(ε-caprolactone) (PEG-b-PCL) and poly(ethylene glycol)-block-poly(lactic acid) (PEG-b-PLA) micelles as a potential treatment of ocular inflammation. The micelles were evaluated for particle size, drug loading capacity and drug rele...
Source: Drug Delivery - July 30, 2020 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

A pH/ROS cascade-responsive and self-accelerating drug release nanosystem for the targeted treatment of multi-drug-resistant colon cancer.
Authors: Chang N, Zhao Y, Ge N, Qian L Abstract The efficacy of chemotherapeutic agents for colon cancer treatment is limited by multidrug resistance (MDR) and insufficient intracellular release of the administered nanomedicine. To overcome these limitations, we constructed a pH/ROS cascade-responsive and self-accelerating drug release nanoparticle system (PLP-NPs) for the treatment of multidrug-resistant colon cancer. The PLP-NPs comprised a reactive oxygen species (ROS)-sensitive polymeric paclitaxel (PTX) prodrug (DEX-TK-PTX), a pH-sensitive poly(l-histidine) (PHis), and beta-lapachone (Lapa), a ROS-generating a...
Source: Drug Delivery - July 28, 2020 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Combined effect of sonophoresis and a microemulsion on the dermal delivery of celecoxib.
Authors: Subongkot T Abstract The aim of this study was to evaluate the intensity of sonophoresis at which the skin penetration of celecoxib was enhanced and to study the combined effects of sonophoresis and microemulsion application on the dermal delivery of celecoxib. The sonophoresis intensity that provided the highest skin penetration enhancement of celecoxib was 30 Watts/cm2. However, the combination of sonophoresis and the microemulsion resulted in a decrease in celecoxib skin penetration. The results of a confocal laser scanning microscopy study using the colocalization analysis of multifluorescently labeled...
Source: Drug Delivery - July 28, 2020 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Adjudin-loaded redox-sensitive paclitaxel-prodrug micelles for overcoming multidrug resistance with efficient targeted Colon cancer therapy.
Authors: Chen D, Ge S, Zuo L, Wang S, Liu M, Li S Abstract Multidrug resistance (MDR) is the primary cause for the failure of chemotherapy in the treatment of colon cancer. Recent research has indicated that the combination of a chemotherapeutic agent and a mitochondrial inhibitor might represent a promising strategy to help overcome MDR. However, for this approach to be clinically effective, it is important that the two drugs can be actively and simultaneously delivered into tumor cells at an optimal ratio and completely released drug within cells. To address these challenges, we designed and prepared a folate rec...
Source: Drug Delivery - July 28, 2020 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

IGF-1-releasing PLGA nanoparticles modified 3D printed PCL scaffolds for cartilage tissue engineering.
Authors: Wei P, Xu Y, Gu Y, Yao Q, Li J, Wang L Abstract The aim of this study is to fabricate and test a 3D-printed PCL scaffold incorporating IGF-1-releasing PLGA nanoparticles for cartilage tissue engineering. IGF-1 loaded PLGA nanoparticles were produced by the double-emulsion method, and were incorporated onto 3D printed PCL scaffolds via PDA. Particle size, loading effciency (LE) and encapsulation effciency (EE) of the nanoparticles were examined. SEM, pore size, porosity, compression testing, contact angle, IGF-1 release kinetics of the composite scaffolds were also determined. For cell culture studies, CCK-...
Source: Drug Delivery - July 28, 2020 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Precise engineering of Gemcitabine prodrug cocktails into single polymeric nanoparticles delivery for metastatic thyroid cancer cells.
Authors: Liu C, Han Q, Liu H, Zhu C, Gui W, Yang X, Li W Abstract GLOBOCAN estimates 36 types of cancers in 185 countries based on the incidence, mortality, and prevalence in the year 2019. Nowadays, chemotherapy is the most widely used cancer treatment among immune, radio, hormone, and gene therapies. Here, we describe a very simple yet cost-effective approach that synergistically combines drug reconstitution, supramolecular nano-assembly, and tumor-specific targeting to address the multiple challenges posed by the delivery of the chemotherapeutic Gemcitabine (GEM) drug. The GEM prodrugs were gifted to impulsively...
Source: Drug Delivery - July 18, 2020 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Correction.
Authors: PMID: 32672080 [PubMed - as supplied by publisher] (Source: Drug Delivery)
Source: Drug Delivery - July 18, 2020 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Synergistic ultrasonic biophysical effect-responsive nanoparticles for enhanced gene delivery to ovarian cancer stem cells.
This study showed that ultrasound triggering and GSH responsive PSP@MB might provide a novel strategy for OCSCs treatment via sonoporation and enhanced-endocytosis. PMID: 32627597 [PubMed - in process] (Source: Drug Delivery)
Source: Drug Delivery - July 8, 2020 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Intra-articular delivery of flurbiprofen sustained release thermogel: improved therapeutic outcome of collagenase II-induced rat knee osteoarthritis.
Authors: Li P, Li H, Shu X, Wu M, Liu J, Hao T, Cui H, Zheng L Abstract Knee osteoarthritis (OA) is a common degenerative disease. Intra-articular administration of flurbiprofen is frequently employed in clinic to treat OA, while repeated injections are required because of the limited effective duration. To improve therapeutic outcome and prolong the treatment interval, a poly(ε-caprolactone-co-lactide)-b-poly(ethylene glycol)-b-poly(ε-caprolactone-co-lactide) (PCLA-PEG-PCLA) triblock copolymer based flurbiprofen thermosensitive gel for the sustained intra-articular drug delivery was designed in thi...
Source: Drug Delivery - July 8, 2020 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Enhanced oral bioavailability of magnolol via mixed micelles and nanosuspensions based on Soluplus ®-Poloxamer 188.
Enhanced oral bioavailability of magnolol via mixed micelles and nanosuspensions based on Soluplus®-Poloxamer 188. Drug Deliv. 2020 Dec;27(1):1010-1017 Authors: Li G, Lu Y, Fan Y, Ning Q, Li W Abstract Magnolol, known to have extensive biological activities, is the major bioactive ingredient isolated from the root and stem bark of Magnolia officinalis. However, the clinical application of magnolol is limited by poor aqueous solubility and absorption. The aim of this study is to develop novel mixed micelles and nanosuspensions composed of two biocompatible copolymers, Soluplus® and Poloxamer 188...
Source: Drug Delivery - July 8, 2020 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Strategies to enhance oral delivery of amphotericin B: a comparison of uncoated and enteric-coated nanostructured lipid carriers.
In conclusion, the developed NLCs and Eu-NLCs could be a potential drug delivery system in improving the oral bioavailability of AmB. PMID: 32633144 [PubMed - in process] (Source: Drug Delivery)
Source: Drug Delivery - July 8, 2020 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Co-delivery of doxorubicin and paclitaxel by reduction/pH dual responsive nanocarriers for osteosarcoma therapy.
Authors: Li Y, Hou H, Zhang P, Zhang Z Abstract Nanoparticle-based drug delivery system offers a promising platform for combination cancer therapy. However, the inefficient drug release in cells reduces the therapeutic efficacy of cancer nanomedicines. Herein, a PEGylated poly(α-lipoic acid) copolymer (mPEG-PαLA) was prepared and used as a reduction/pH dual responsive nanocarrier to simultaneously deliver paclitaxel (PTX) and doxorubicin (DOX) for osteosarcoma therapy. The amphiphilic mPEG-PαLA could efficiently encapsulate both PTX and DOX during its self-assembly into micelles in aqueous solutio...
Source: Drug Delivery - July 8, 2020 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Sequential delivery of dual drugs with nanostructured lipid carriers for improving synergistic tumor treatment effect.
In conclusion, NLCs are promising nanocarriers for delivering dual chemotherapeutic drugs sequentially, showing potentials in the synergistic treatment of tumors while reducing adverse effects both in vitro and in vivo. PMID: 32611218 [PubMed - in process] (Source: Drug Delivery)
Source: Drug Delivery - July 4, 2020 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Acylation of the antimicrobial peptide CAMEL for cancer gene therapy.
In this study, we constructed a series of non-viral vectors by attaching fatty acids with different chain lengths to the N-terminus of CAMEL. Our results showed that the cellular uptake and transfection efficiency of acyl-CAMEL started to significantly increase from a chain length of 12 carbons. C18-CAMEL was screened for gene delivery because it had the highest transfection efficiency. Surprisingly, C18-CAMEL/plasmid complexes displayed strong endosomal escape activity after entering cells via endocytosis. Importantly, C18-CAMEL could deliver p53 plasmids to cancer cells and significantly inhibited cell proliferation by t...
Source: Drug Delivery - July 4, 2020 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Biodistribution of etoposide via intratumoral chemotherapy with etoposide-loaded implants.
In this study, we prepared the poly-l-lactic acid (PLLA) based VP16-loaded implants (VP16 implants) by the direct compression method. The VP16 implants were characterized with regards to drug content, micromorphology, drug release profiles, differential scanning calorimetry (DSC) and Fourier transform infrared spectroscopy (FTIR) analyses. Furthermore, the biodistribution of VP16 via intratumoral chemotherapy with VP16 implants was investigated using the murine Lewis lung carcinoma model. Our results showed that VP16 dispersed homogenously in the polymeric matrix. Both in vitro and in vivo drug release profiles of the...
Source: Drug Delivery - July 4, 2020 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Biological investigations on therapeutic effect of chitosan encapsulated nano resveratrol against gestational diabetes mellitus rats induced by streptozotocin.
In this study, the resveratrol-zinc oxide complex is encapsulated with chitosan (CS-ZnO-RS). The synthesized CS-ZnO-RS could be used to deliver the resveratrol with minimized side effects and also improved bioavailability. CS-ZnO-RS were characterized by various techniques such as particle size analyzer, DSC, FT-IR, TEM, SEM, and AFM. The electron microscopic and particle analyzer confirmed that the synthesized CS-ZnO-RS were monodispersed, spherical and its average size was 38 nm. The drug-releasing profile showed that 95% of RS is released from CS-ZnO-RS within 24 h. In vitro studies confirmed that α-...
Source: Drug Delivery - July 4, 2020 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Molecular docking and statistical optimization of taurocholate-stabilized galactose anchored bilosomes for the enhancement of sofosbuvir absorption and hepatic relative targeting efficiency.
Authors: Joseph Naguib M, Moustafa Kamel A, Thabet Negmeldin A, Elshafeey AH, Elsayed I Abstract The work aimed to improve both absorption and hepatic availability of sofosbuvir. Bilosomes and galactose-anchored bilosomes were investigated as potential nanocarriers for this purpose. Sofosbuvir is a class III drug with high solubility and low permeability. Thus, the drug entrapment into lipid-based galactose-anchored carriers would enhance drug permeability and improve its liver availability. The galactosylated taurocholate was designed and synthesized based on molecular docking studies, where both galactose and tau...
Source: Drug Delivery - July 4, 2020 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Combined treatment with ultrasound-targeted microbubble destruction technique and NM-aFGF-loaded PEG-nanoliposomes protects against diabetic cardiomyopathy-induced oxidative stress by activating the AKT/GSK-3 β1/Nrf-2 pathway.
Combined treatment with ultrasound-targeted microbubble destruction technique and NM-aFGF-loaded PEG-nanoliposomes protects against diabetic cardiomyopathy-induced oxidative stress by activating the AKT/GSK-3β1/Nrf-2 pathway. Drug Deliv. 2020 Dec;27(1):938-952 Authors: Zhang M, Zhu NW, Ma WC, Chen MJ, Zheng L Abstract The present study sought to investigate the effect of non-mitogenic acidic fibroblast growth factor (NM-aFGF) loaded PEGylated nanoliposomes (NM-aFGF-PEG-lips) combined with the ultrasound-targeted microbubble destruction (UTMD) technique on modulating diabetic cardiomyopathy (DCM)an...
Source: Drug Delivery - July 4, 2020 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Engineering of fluorescent or photoactive Trojan probes for detection and eradication of β-Amyloids.
Engineering of fluorescent or photoactive Trojan probes for detection and eradication of β-Amyloids. Drug Deliv. 2020 Dec;27(1):917-926 Authors: Aziz AA, Siddiqui RA, Amtul Z Abstract Trojan horse technology institutes a potentially promising strategy to bring together a diagnostic or cell-based drug design and a delivery platform. It provides the opportunity to re-engineer a novel multimodal, neurovascular detection probe, or medicine to fuse with blood-brain barrier (BBB) molecular Trojan horse. In Alzheimer's disease (AD) this could allow the targeted delivery of detection or therapeutic probes...
Source: Drug Delivery - July 2, 2020 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Enhanced anti-hepatoma effect of a novel curcumin analog C086 via solid dispersion technology.
Authors: Deng Y, Chen C, Xiao Z, Huang X, Xu J Abstract The novel curcumin analog C086, previously identified as an oral novel heat shock protein 90 (Hsp90) inhibitor, was found to exhibit anti-hepatoma activity in vitro and in vivo. However, owing to its limited aqueous solubility, the usage of C086 in the clinical application was restricted. This research focused on the increase of the aqueous solubility and bioavailability of C086 via a solid dispersion preparation to improve its accumulation in the liver, which accordingly enhanced anti-hepatoma activity. C086-solid dispersion (C086-SD) was successful...
Source: Drug Delivery - July 2, 2020 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Factors affecting the buccal delivery of deformable nanovesicles based on insulin-phospholipid complex: an in  vivo investigation.
In this study, we designed a series of DNVs, based on an insulin-phospholipid complex (IPC-DNVs), to investigate the influence of drug dose, buccal administration methods, and key quality characteristics of IPC-DNVs for buccal delivery. IPC-DNVs showed a non-linear dose-response relationship between 8 and 12 IU. There was no significant effect of drug delivery site (sublingual mucosa/buccal mucosa) or ligation time (15 or 30 min) on buccal absorption of IPC-DNVs. However, the area above the curve of reduction in blood glucose level overtime (AAC0-6h) for oral mucosa administration was significantly higher tha...
Source: Drug Delivery - July 2, 2020 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Functionalized MoS2-nanoparticles for transdermal drug delivery of atenolol.
Authors: Zhang K, Zhuang Y, Zhang W, Guo Y, Liu X Abstract Molybdenum disulfide (MoS2) has excellent photothermal conversion abilities, an ultra-high specific surface area, and has been extensively explored for use in biomedicine. However, the high toxicity associated with MoS2 has limited its biological applications for in vivo photothermal therapy and drug delivery systems. Herein, we have developed cationic hydroxyethyl cellulose (JR400) surface-modified MoS2 nanoparticles (NPs) that are responsive to near-infrared (NIR) laser irradiation as a transdermal drug delivery system (TDDS). Herein, we confirmed th...
Source: Drug Delivery - July 2, 2020 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Formulation and investigation of pilocarpine hydrochloride niosomal gels for the treatment of glaucoma: intraocular pressure measurement in white albino rabbits.
Authors: Jain N, Verma A, Jain N Abstract The present study was focused on investigating niosomal gels loaded with cholinergic drug; pilocarpine HCl, for prolonged precorneal residence time and improved bioavailability for glaucoma treatment. Pilocarpine HCl niosomes were prepared using various nonionic surfactants (span 20, span 60 and span 80), in the presence of cholesterol in different molar ratios by ether injection method. The selected formulations were incorporated into carbopol 934 and locust bean gum-based gels. TEM analysis confirmed that niosomes formed were spherical in shape and has a definite internal...
Source: Drug Delivery - June 21, 2020 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

NIR triggered PLGA coated Au-TiO2 core loaded CPT-11 nanoparticles for human papillary thyroid carcinoma therapy.
Authors: Yu T, Tong L, Ao Y, Zhang G, Liu Y, Zhang H Abstract MDR (multi-drug resistance) is one of the significant deterrents of effective chemotherapy for malignant growth. One of the powerful ways to deal with defeat of the MDR is to utilize inorganic nanoparticle-intervened tranquilize conveyance to build the medication aggregations in cancerous growth cells. In this work, we have developed the presentation that is accurately made of medication conveyance framework dependent on the TiO2 nanoparticles stacked CPT-11 to defeat the thyroid malignancy cells. The synthesized nanoparticles are characterized by spectr...
Source: Drug Delivery - June 11, 2020 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Multifunctional magnetite nanoparticles to enable delivery of siRNA for the potential treatment of Alzheimer's.
This study aims to explore the ability of a multifunctional conjugate based on magnetite nanoparticles for the cellular delivery of siRNA against the expression of the BACE1 gene. We immobilized the siRNA strand on PEGylated magnetite nanoparticles and investigated the effects on biocompatibility and efficacy of the conjugation. Similarly, we co-immobilized the translocating protein OmpA on PEGylated nanoparticles to enhance cellular uptake and endosomal escape. BACE1 suppression was statistically significant in HFF-1 cells, without any presence of a cytotoxic effect. The delivery of the nanoconjugate was achieved through ...
Source: Drug Delivery - June 11, 2020 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Self-assembled dihydroartemisinin nanoparticles as a platform for cervical cancer chemotherapy.
Authors: Lu Y, Wen Q, Luo J, Xiong K, Wu Z, Wang B, Chen Y, Yang B, Fu S Abstract Dihydroartemisinin (DHA) is a potent anti-cancer drug that has limited clinical applications due to poor water solubility and low bioavailability. We designed a biodegradable poly(ethylene glycol) methyl ether-poly(ε-caprolactone) (MPEG-PCL) micelle carrier for DHA using the self-assembly method. The DHA/MPEG-PCL nanoparticles were spherical with an average particle size of 30.28 ± 0.27 nm, and released the drug in a sustained manner in aqueous solution. The drug-loaded nanoparticles showed dose-dep...
Source: Drug Delivery - June 11, 2020 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

In vivo antitumor effects of carboxymethyl chitosan-conjugated triptolide after oral administration.
Authors: Zeng H, Zhu X, Tian Q, Yan Y, Zhang L, Yan M, Li R, Li X, Wang G, Ma J, Su Y, Zhang X, Ma L, Zhang Z, Wu X Abstract The purpose of this study is to evaluate in vitro and in vivo antitumor efficacy and subacute toxicity of triptolide (TP) prodrug, a conjugate between TP and carboxymethyl chitosan (CC). The CCTP conjugate contained 4∼ wt % TP and displayed excellent aqueous solubility (5 mg/mL) as compared to the native TP (17 μg/mL). In vitro cytotoxicity of CCTP conjugate was evaluated by CCK8 assay against human pancreatic cancer (PC) cell lines, showing comparable the half ...
Source: Drug Delivery - June 10, 2020 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

F7 and topotecan co-loaded thermosensitive liposome as a nano-drug delivery system for tumor hyperthermia.
Authors: Du C, Li S, Li Y, Galons H, Guo N, Teng Y, Zhang Y, Li M, Yu P Abstract In order to enhance the targeting efficiency and reduce anti-tumor drug's side effects, topotecan (TPT) and F7 were co-loaded in thermosensitive liposomes (F7-TPT-TSL), which show enhanced permeability and retention in tumors, as well as local controlled release by heating in vitro. TPT is a water-soluble inhibitor of topoisomerase I that is converted to an inactive carboxylate structure under physiological conditions (pH 7.4). F7 is a novel drug significantly resistant to cyclin-dependent kinase but its use was restricted by its ...
Source: Drug Delivery - June 10, 2020 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Calcium enhances polyplex-mediated transfection efficiency of plasmid DNA in Jurkat cells.
Authors: Ayyadevara VSSA, Roh KH Abstract Jurkat, an immortalized cell line derived from human leukemic T lymphocytes, has been employed as an excellent surrogate model of human primary T-cells for the advancement of T-cell biology and their applications in medicine. However, presumably due to its T-cell origin, Jurkat cells are very difficult to transfect. Thus, for the genetic modification of Jurkat cells, expensive and time-consuming viral vectors are normally required. Despite many previous efforts, non-viral vectors have not yet overcome the hurdles of low transfection efficiency and/or high toxicity in transf...
Source: Drug Delivery - June 5, 2020 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Hyaluronic acid reduction-sensitive polymeric micelles achieving co-delivery of tumor-targeting paclitaxel/apatinib effectively reverse cancer multidrug resistance.
Authors: Zhang X, Ren X, Tang J, Wang J, Zhang X, He P, Yao C, Bian W, Sun L Abstract Multidrug resistance (MDR) of cancer cells is a significant challenge in chemotherapy, highlighting the urgent medical need for simple and reproducible strategies to reverse this process. Here, we report the development of an active tumor-targeting and redox-responsive nanoplatform (PA-ss-NP) using hyaluronic acid-g-cystamine dihydrochloride-poly-ε-(benzyloxycarbonyl)-L-lysine (HA-ss-PLLZ) to co-deliver paclitaxel (PTX) and apatinib (APA) for effective reversal of MDR. This smart nanoplatform specifically bound to CD44 rec...
Source: Drug Delivery - June 5, 2020 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Preparation of hydroxy genkwanin nanosuspensions and their enhanced antitumor efficacy against breast cancer.
Authors: Ao H, Li Y, Li H, Wang Y, Han M, Guo Y, Shi R, Yue F, Wang X Abstract Hydroxy genkwanin (HGK), a flavonoid compound from natural resources, showed good inhibition against the growth of breast tumor cells. However, the poor solubility restricted the further study and the in vivo drug delivery of HGK. We prepared HGK nanosuspensions by antisolvent precipitation method and investigated their characterization, stability, hemolysis probability, release behavior in vitro, antitumor activity in vitro and in vivo, and preliminary safety through acute toxicity experiments. The resultant HGK nano...
Source: Drug Delivery - June 5, 2020 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Combined photodynamic-chemotherapy investigation of cancer cells using carbon quantum dot-based drug carrier system.
Authors: Li X, Vinothini K, Ramesh T, Rajan M, Ramu A Abstract The combined chemotherapy and photodynamic therapy have significant advantages for cancer treatments, which have higher therapeutic effects compared with other medicines. Herein, we focused on the synthesis of carbon quantum dot (CQD) based nanocarrier system. CQD and 5-aminolevulinic acid (5-ALA) were conjugated with mono-(5-BOC-protected-glutamine-6-deoxy) β-cyclodextrin (CQD-Glu-β-CD) moiety, and finally, the anticancer chemotherapy doxorubicin (DOX) drug was loaded in the 5-ALA-CQD-Glu-β-CD system. The stepwise physicochemical changes...
Source: Drug Delivery - May 19, 2020 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research