Stereocomplexation Assisted Assembly of Poly(γ-glutamic Acid)-graft-polylactide Nano-micelles and Their Efficacy as Anticancer Drug Carrier

2018 ◽  
Vol 18 (2) ◽  
pp. 302-311
Author(s):  
Shulin Dai ◽  
Yucheng Feng ◽  
Shuyi Li ◽  
Yuxiao Chen ◽  
Meiqing Liu ◽  
...  
Keyword(s):  
Glutamic Acid ◽  
Drug Carrier ◽  
Drug Loading ◽  
Drug Carriers ◽  
Cancer Drug ◽  
Drug Release Profile ◽  
Sustained Drug Release ◽  
Anti Cancer ◽  
Physical Interactions

Background: Micelles as drug carriers are characterized by their inherent instability due to the weak physical interactions that facilitate the self-assembly of amphiphilic block copolymers. As one of the strong physical interactions, the stereocomplexation between the equal molar of enantiomeric polylactides, i.e., the poly(L-lactide) (PLLA) and poly(D-lactide) (PDLA), may be harnessed to obtain micelles with enhanced stability and drug loading capacity and consequent sustained release. </P><P> Aims/Methods: In this paper, stereocomplexed micelles gama-PGA-g-PLA micelles) were fabricated from the stereocomplexation between poly(gama-glutamic acid)-graft-PLLA gama-PGA-g-PLA) and poly(gamaglutamic acid)-graft-PDLA gama-PGA-g-PLA). These stereocomplexed micelles exhibited a lower CMC than the corresponding enantiomeric micelles. Result: Furthermore, they showed higher drug loading content and drug loading efficiency in addition to more sustained drug release profile in vitro. In vivo imaging confirmed that the DiR-encapsulated stereocomplexed gama-PGA-g-PLA micelles can deliver anti-cancer drug to tumors with enhanced tissue penetration. Overall, gama-PGA-g-PLA micelles exhibited greater anti-cancer effects as compared with the free drug and the stereocomplexation may be a promising strategy for fabrication of anti-cancer drug carriers with significantly enhanced efficacy.

scholarly journals Polypeptides Micelles Composed of Methoxy-Poly(Ethylene Glycol)-Poly(l-Glutamic Acid)-Poly(l-Phenylalanine) Triblock Polymer for Sustained Drug Delivery

Pharmaceutics ◽  
2018 ◽  
Vol 10 (4) ◽  
pp. 230 ◽  
Author(s):  
Xingzheng Liu ◽  
Rongrong Fan ◽  
Boting Lu ◽  
Yuan Le
Keyword(s):  
Drug Release ◽  
Ethylene Glycol ◽  
Glutamic Acid ◽  
Drug Carrier ◽  
Drug Loading ◽  
Poly Ethylene Glycol ◽  
Sustained Drug Release ◽  
Poly Ethylene ◽  
Triblock Polymers

Methoxy-poly(ethylene glycol)-poly(l-glutamic acid)-poly(l-phenylalanine) triblock polymers with different architecture were synthesized as drug carrier to obtain sustained and controlled release by tuning the composition. These triblock polymers were prepared by ring opening polymerization and poly(ethylene glycol) was used as an initiator. Polymerization was confirmed by 1H NMR, FT-IR and gel penetration chromatography. The polymers can self-assemble to form micelles in aqueous medium and their critical micelle concentrations values were examined. The micelles were spherical shape with size of 50–100 nm and especially can arranged in a regular manner. Sorafenib was selected as the model drug and the drug loading performance was dependent on the composition of the block copolymer. In vitro drug release indicated that the polymers can realize controlled and sustained drug release. Furthermore, in vitro cytotoxicity assay showed that the polymers were biocompatible and the drug-loaded micelles can increase toxicity towards tumor cells. Confocal fluorescence microscopy assays illustrated that the micelles can be uptaken quickly and release drug persistently to inhibit tumor cell growth.

Synthesis and characterization of fluorescent chitosan–ZnSe/ZnS nanoparticles for potential drug carriers

RSC Advances ◽  
2015 ◽  
Vol 5 (49) ◽  
pp. 38810-38817 ◽  
Author(s):  
Yeping Li ◽  
Jingbo Xu ◽  
Yun Xu ◽  
Liying Huang ◽  
Junli Wang ◽  
...  
Keyword(s):  
Quantum Dots ◽  
Drug Carrier ◽  
Drug Carriers ◽  
Cancer Drug ◽  
Synthesis And Characterization ◽  
Potential Drug ◽  
Zns Nanoparticles ◽  
New Approach ◽  
Anti Cancer

The objective of the study is to describe a new approach of combining quantum dots into chitosan as an anti-cancer drug carrier.

Surface Engineered Porous Silicon-based Nanostructures for Cancer Therapy

2012 ◽  
Vol 1416 ◽  
Author(s):  
Adi Tzur-Balter ◽  
Naama Massad-Ivanir ◽  
Ester Segal
Keyword(s):  
Porous Silicon ◽  
Surface Chemistry ◽  
Electrochemical Etching ◽  
Release Kinetics ◽  
Drug Carrier ◽  
Drug Loading ◽  
Nitrogen Adsorption ◽  
Cancer Drug ◽  
Cytotoxicity Studies

ABSTRACTIn this work, nanostructured porous silicon (PSi) hosts, synthesized by electrochemical etching of Si, are designed to carry and release the anti cancer drug, mitoxantrone dihydrochloride (MTX). We study the effect of surface chemistry of the Si scaffold on its properties as a drug carrier. The freshly-etched PSi is modified by surface alkylation using thermal hydrosilylation with 1-dodecene. Fourier-transform infrared spectroscopy and nitrogen adsorption-desorption measurements are employed to characterize the PSi carriers after chemical modification. Both, drug loading efficiency and release kinetics are found to be significantly affected by surface chemistry of the PSi. In vitro cytotoxicity studies on human breast carcinoma (MDA-MB-231) cells show that the MTX released from the PSi hosts maintains its cytotoxic functionality.

Development and Characterization of Binary Solid Lipid Nano Suspension of Atorvastatin: In-Vitro Drug Release and In-Vivo Pharmacokinetic Studies

2019 ◽  
Vol 11 (11) ◽  
pp. 1522-1530
Author(s):  
Mahwish Kamran ◽  
Mir Azam Khan ◽  
Muhammad Shafique ◽  
Maqsood ur Rehman ◽  
Waqar Ahmed ◽  
...  
Keyword(s):  
Drug Release ◽  
Oral Bioavailability ◽  
Drug Loading ◽  
Lipid Lowering ◽  
Diffusion Method ◽  
Pharmacokinetic Studies ◽  
Drug Release Profile ◽  
Sustained Drug Release ◽  
Solid Lipid

Atorvastatin is an extensively used lipid lowering agent. But the vital issue associated with it is low oral bioavailability (12%) owing to poor aqueous solubility. To overcome this tribulation, binary solid lipid nano suspension of Atorvastatin (ATO) was formulated by solvent diffusion method. The combination of stearic acid and oleic acid was utilized as a lipid carrier with Tween-80 (surfactant) along with Polyvinylpyrrolidone (co-surfactant). Optimized nano formulation was prepared by changing the formulation variables. Optimized nano suspension (ATO-4) represented particle size 228.3 ± 2.1 nm and polydispersity index (PDI) 0.225 ± 0.02 with zeta potential (ZP) – 33.6 ± 0.02 mV. Encapsulation efficiency along with drug loading capacity was 88.3 ± 2.5% and 4.9 ± 0.14% respectively. Scanning electron microscopic (SEM) analysis exposed spherical shaped amorphous particles. Differential scanning calorimetry (DSC) as well as X-ray powder diffraction (P-XRD) established reduction in drug's crystalline state. Fourier transform infrared (FTIR) spectroscopy exposed no interaction amongst the drug and formulation contents. In-vitro studies revealed sustained pattern of drug release. Stability studies confirmed refrigerated temperature as most suitable for storage of binary solid lipid nano suspension. Plasma concentration versus time curve ascertained 2.78-fold increase in oral bioavailability of ATO nano suspension compared to the marketed product (Lipitor®). Findings proposed desired improvement in oral bioavailability of ATO nano suspension with sustained drug release profile. Thus, binary solid lipid nano suspension could be utilized as an advanced drug delivery system for oral deliverance of hydrophobic drugs.

Paclitaxel-tyroserleutide Conjugates Self-assembly into Nanocarrier for Drug Delivery

2019 ◽  
Vol 16 (8) ◽  
pp. 882-891
Author(s):  
Yongjia Liu ◽  
Leilei Shi ◽  
Bangshang Zhu ◽  
Yue Su ◽  
Hui Li ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Self Assembly ◽  
Water Solubility ◽  
Drug Carrier ◽  
Drug Loading ◽  
Cancer Therapeutics ◽  
Drug Carriers ◽  
Pharmacokinetic Studies ◽  
Assembly Method

Background: The drug-drug self-assembly was considered as a simple and efficient approach to prepare high drug loading nano-drug carriers and present new opportunities for cancer therapeutics. The strategy of PTX amphiphiles preparation would be a possible way to solve the poor water solubility of PTX. Methods: The PTX-YSL conjugate were synthesized and characterized. The PTX-YSL nanocarriers was prepared by a simple self-assembly method. In vitro cell studies and pharmacokinetic studies were evaluated for their in vitro anti-tumor activities and blood retention time. Results: The structures of PTX-YSL conjugate were confirmed by LC-MS, 1H NMR and FTIR. The size and morphology of the PTX-YSL self-assembled nanocarriers were observed with TEM and DLS. PTX-YSL nanocarriers could facilitate cellular uptake and had low cytotoxicity. PTX-YSL nanocarriers have longer blood retention for enhancing accumulation in the tumor tissues via EPR effect. Conclusion: This drug delivery system formed by PTX-YSL conjugates constitutes a promising and effective drug carrier in cancer therapy.

scholarly journals pH-Sensitive Dendrimersomes of Hybrid Triazine-Carbosilane Dendritic Amphiphiles-Smart Vehicles for Drug Delivery

Nanomaterials ◽  
2020 ◽  
Vol 10 (10) ◽  
pp. 1899 ◽  
Author(s):  
Evgeny Apartsin ◽  
Nadezhda Knauer ◽  
Valeria Arkhipova ◽  
Ekaterina Pashkina ◽  
Alina Aktanova ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Drug Loading ◽  
Drug Carriers ◽  
Ph Sensitive ◽  
Cancer Drug ◽  
Smart Vehicles ◽  
New Class ◽  
Self Assembling ◽  
Anti Cancer ◽  
Cancer Drug Delivery

Supramolecular constructions of amphiphilic dendritic molecules are promising vehicles for anti-cancer drug delivery due to the flexibility of their architecture, high drug loading capacity and avoiding off-target effects of a drug. Herein, we report a new class of amphiphilic dendritic species—triazine-carbosilane dendrons readily self-assembling into pH-sensitive dendrimersomes. The dendrimersomes efficiently encapsulate anticancer drugs doxorubicin and methotrexate. Chemodrug-loaded dendrimersomes have dose-related cytotoxic activity against leukaemia cell lines 1301 and K562. Our findings suggest that triazine-carbosilane dendrimersomes are prospective drug carriers for anti-cancer therapy.

scholarly journals Cellular Analysis and Chemotherapeutic Potential of a Bi-Functionalized Halloysite Nanotube

Pharmaceutics ◽  
2020 ◽  
Vol 12 (10) ◽  
pp. 962
Author(s):  
Yangyang Luo ◽  
Ahmed Humayun ◽  
Teresa A. Murray ◽  
Benjamin S. Kemp ◽  
Antwine McFarland ◽  
...  
Keyword(s):  
Cancer Cells ◽  
Drug Carrier ◽  
Drug Loading ◽  
Cancer Drug ◽  
Intracellular Location ◽  
Cellular Analysis ◽  
Osteoblast Cell Line ◽  
Wide Range ◽  
Anti Cancer ◽  
Target Cancer

The surface of halloysite nanotubes (HNTs) was bifunctionalized with two ligands—folic acid and a fluorochrome. In tandem, this combination should selectively target cancer cells and provide a means for imaging the nanoparticle. Modified bi-functionalized HNTs (bi-HNTs) were then doped with the anti-cancer drug methotrexate. bi-HNTs were characterized and subjected to in vitro tests to assess cellular growth and changes in cellular behavior in three cell lines—colon cancer, osteosarcoma, and a pre-osteoblast cell line (MC3T3-E1). Cell viability, proliferation, and cell uptake efficiency were assessed. The bi-HNTs showed cytocompatibility at a wide range of concentrations. Compared with regular-sized HNTs, reduced HNTs (~6 microns) were taken up by cells in more significant amounts, but increased cytotoxicity lead to apoptosis. Multi-photon images confirmed the intracellular location of bi-HNTs, and the method of cell entry was mainly through caveolae-mediated endocytosis. The bi-HNTs showed a high drug loading efficiency with methotrexate and a prolonged period of release. Most importantly, bi-HNTs were designed as a drug carrier to target cancer cells specifically, and imaging data shows that non-cancerous cells were unaffected after exposure to MTX-doped bi-HNTs. All data provide support for our nanoparticle design as a mechanism to selectively target cancer cells and significantly reduce the side-effects caused by off-targeting of anti-cancer drugs.

Polymer-Tethered pH-Sensitive Magnetic Nanoparticles for Targeted Delivery of Anti-Cancer Drug

2014 ◽  
Vol 936 ◽  
pp. 723-727
Author(s):  
Yue Qing Shen ◽  
Meng Lu Pu ◽  
Wei Jiang
Keyword(s):  
Targeted Delivery ◽  
Drug Carrier ◽  
Ph Sensitive ◽  
Cancer Drug ◽  
Lysosomal Ph ◽  
Efficient Delivery ◽  
Chemical Grafting ◽  
Anti Cancer ◽  
Ph Sensitive Polymer

Efficient delivery of drug to tumor cells is one of the crucial issues in cancer therapy. This letter addresses for the first time that poly (acrylic acid) (PAA), a pH-sensitive polymer, is tethered to the surface of the nanoparticles by chemical grafting. The release rates of doxorubicin (DOX) are subsequently studied in vitro. The results reveal that DOX can be released preferentially at the desired lysosomal pH, and show that the anti-cancer drug carrier can be applied to the biomedical applications.

Synthesis, Characterization and in-vitro drug release studies of a macromolecular prodrug of Didanosine.

2010 ◽  
Vol 2 (2) ◽  
Author(s):  
Neeraj Agrawal ◽  
M.J. Chandrasekar ◽  
U.V. Sara ◽  
Rohini A.
Keyword(s):  
Drug Release ◽  
Drug Level ◽  
Drug Release Profile ◽  
Sustained Drug Release ◽  
In Vitro Drug Release ◽  
Alkaline Environment ◽  
Stomach Acid ◽  
Release Studies ◽  
Macromolecular Prodrug

A macromolecular prodrug of didanosine (ddI) for oral administration was synthesized and evaluated for in-vitro drug release profile. Didanosine was first coupled to 2-hydroxy ethyl methacrylate (HEMA) through a succinic spacer to form HEMA-Suc-ddI monomeric conjugate which was subsequently polymerized to yield Poly(HEMA-Suc-ddI) conjugate. The structures of the synthesized compounds were characterized by FT-IR, Mass and 1H-NMR spectroscopy. The prodrug was subjected for in-vitro drug release studies in buffers of pH 1.2 and 7.4 mimicking the upper and lower GIT. The results showed that the drug release from the polymeric backbone takes place in a sustained manner over a period of 24 h and the amount of drug released was comparatively higher at pH 7.4 indicating that the drug release takes place predominantly at the alkaline environment of the lower GIT rather than at the acidic environment of the upper GIT. This pH dependent sustained drug release behavior of the prodrug may be capable of reducing the dose limiting toxicities by maintaining the plasma drug level within the therapeutic range and increasing t1/2 of ddI. Moreover, the bioavailability of the drug should be improved as the prodrug releases ddI predominantly in the alkaline environment which will reduce the degradation of ddI in the stomach acid.

Chitosan-based Polymer Matrix for Pharmaceutical Excipients and Drug Delivery

2019 ◽  
Vol 26 (14) ◽  
pp. 2502-2513 ◽  
Author(s):  
Md. Iqbal Hassan Khan ◽  
Xingye An ◽  
Lei Dai ◽  
Hailong Li ◽  
Avik Khan ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Drug Delivery Systems ◽  
Drug Carrier ◽  
Drug Loading ◽  
Delivery Systems ◽  
Cancer Drug ◽  
Release Mechanism ◽  
Innovative Drug ◽  
Pharmaceutical Excipients ◽  
Weight Variation

The development of innovative drug delivery systems, versatile to different drug characteristics with better effectiveness and safety, has always been in high demand. Chitosan, an aminopolysaccharide, derived from natural chitin biomass, has received much attention as one of the emerging pharmaceutical excipients and drug delivery entities. Chitosan and its derivatives can be used for direct compression tablets, as disintegrant for controlled release or for improving dissolution. Chitosan has been reported for use in drug delivery system to produce drugs with enhanced muco-adhesiveness, permeation, absorption and bioavailability. Due to filmogenic and ionic properties of chitosan and its derivative(s), drug release mechanism using microsphere technology in hydrogel formulation is particularly relevant to pharmaceutical product development. This review highlights the suitability and future of chitosan in drug delivery with special attention to drug loading and release from chitosan based hydrogels. Extensive studies on the favorable non-toxicity, biocompatibility, biodegradability, solubility and molecular weight variation have made this polymer an attractive candidate for developing novel drug delivery systems including various advanced therapeutic applications such as gene delivery, DNA based drugs, organ specific drug carrier, cancer drug carrier, etc.

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