A comparison study to investigate the effect of the drug-loading site on its delivery efficacy using double hydrophilic block copolymer-based prodrugs

2017 ◽  
Vol 5 (23) ◽  
pp. 4443-4454 ◽  
Author(s):  
Xufeng Zhou ◽  
Cong Chang ◽  
Yang Zhou ◽  
Lu Sun ◽  
Hua Xiang ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Block Copolymer ◽  
Drug Loading ◽  
Hydrophobic Core ◽  
Comparison Study ◽  
Hydrophilic Shell

Two types of thermo-sensitive DHBCs-based micelle prodrugs with drug tethered to the hydrophilic shell or encapsulated with the hydrophobic core was fabricated, and compared further for their drug delivery efficacy.

A Smart Drug Delivery System Based on Thermo-Responsive Polymer Gated Au NRs@SiO2 Nano-Platform

2021 ◽  
Vol 16 (7) ◽  
pp. 1029-1036
Author(s):  
Hongzhu Wang ◽  
Mengxun Chen ◽  
Liping Song ◽  
Youju Huang
Keyword(s):  
Drug Delivery ◽  
Block Copolymer ◽  
Drug Release ◽  
Drug Delivery System ◽  
Delivery System ◽  
Photothermal Therapy ◽  
Drug Loading ◽  
Temperature Sensitive

A key challenge for nanoparticles-based drug delivery system is to achieve manageable drug release in tumour cell. In this study, a versatile system combining photothermal therapy and controllable drug release for tumour cells using temperature-sensitive block copolymer coupled Au NRs@SiO2 is reported. While the Au NRs serve as hyperthermal agent and the mesoporous silica was used to improve the drug loading and decrease biotoxicity. The block copolymer acted as “gatekeeper” to regulate the release of model drug (Doxorubicin hydrochloride, DOX). Through in vivo and in vitro experiments, we achieved the truly controllable drug release and photothermal therapy with the collaborative effect of the three constituents of the nanocomposites. The reported nanocomposites pave the way to high-performance controllable drug release and photothermal therapy system.

Supramolecular micellar drug delivery system based on multi-arm block copolymer for highly effective encapsulation and sustained-release chemotherapy

2019 ◽  
Vol 7 (37) ◽  
pp. 5677-5687 ◽  
Author(s):  
Li Zhang ◽  
Dongjian Shi ◽  
Chunling Shi ◽  
Tatsuo Kaneko ◽  
Mingqing Chen
Keyword(s):  
Drug Delivery ◽  
Block Copolymer ◽  
Sustained Release ◽  
Drug Delivery System ◽  
Delivery System ◽  
Drug Loading ◽  
High Drug ◽  
Release Drug ◽  
Drug Loading Efficiency ◽  
High Drug Loading

A novel multi-arm polyphosphoester-based nanomaterial provides high drug loading efficiency and sustained-release drug delivery for effective chemotherapy.

scholarly journals Novel Composite Nanocarriers

2020 ◽  
pp. 1-4
Author(s):  
Ignác Capek ◽  
Ignác Capek
Keyword(s):  
Drug Delivery ◽  
Functional Groups ◽  
Cell Lines ◽  
Cancer Cell ◽  
Colloidal Stability ◽  
Covalent Immobilization ◽  
Hydrophobic Core ◽  
Physiochemical Properties ◽  
Whole Cells ◽  
Hydrophilic Shell

Need for materials with high biocompatible properties have led to the development of prodrug-decorated nanoparticles. The structure of present nanostructures consists of the hydrophobic core and hydrophilic shell. The shell acts as an external envelop which enhances the colloidal stability of dispersion which protects the prodrug of the nanoparticles from photo- and thermal-initiated degradation. The composite nanoparticles coated by organic shells with functional groups were considered to govern the covalent immobilization of therapeutics/biomolecules. The nanoparticles with unique physiochemical properties may be useful as biosensors in living whole cells. The enhanced cellular drug delivery to cancer cell lines via nanoconjugates revealed that smart nanoparticles are an effective tool for transporting and delivering drugs.

scholarly journals Reversible Cross-Linked Mixed Micelles for pH Triggered Swelling and Redox Triggered Degradation for Enhanced and Controlled Drug Release

Pharmaceutics ◽  
2020 ◽  
Vol 12 (3) ◽  
pp. 258 ◽  
Author(s):  
Di Xiong ◽  
Liyang Wen ◽  
Shiyuan Peng ◽  
Jianchang Xu ◽  
Lijuan Zhang
Keyword(s):  
Drug Delivery ◽  
Aqueous Solution ◽  
Drug Release ◽  
Tumor Cells ◽  
Disulfide Bonds ◽  
Mixed Micelle ◽  
Mixed Micelles ◽  
Controlled Drug Release ◽  
Hydrophobic Core ◽  
Hydrophilic Shell

Good stability and controlled drug release are important properties of polymeric micelles for drug delivery. A good candidate for drug delivery must have outstanding stability in a normal physiological environment, followed with low drug leakage and side effects. Moreover, the chemotherapeutic drug in the micellar core should also be quickly and “on-demand” released in the intracellular microenvironment at the tumor site, which is in favor of overcoming multidrug resistance (MDR) effects of tumor cells. In this work, a mixed micelle was prepared by the simple mix of two amphiphilic copolymers, namely PCL-SS-P(PEGMA-co-MAEBA) and PCL-SS-PDMAEMA, in aqueous solution. In the mixed micelle’s core–shell structure, PCL blocks were used as the hydrophobic core, while the micellar hydrophilic shell consisted of two blocks, namely P(PEGMA-co-MAEBA) and PDMAEMA. In the micellar shell, PEGMA provided hydrophilicity and stability, while MAEBA introduced the aldehyde sites for reversible crosslinking. Meanwhile, the PDMAEMA blocks were also introduced in the micellar shell for pH-responding protonation and swelling of the micelle. The disulfide bonds between the hydrophobic core and hydrophilic shell had redox sensitive properties. Reversible cross-linked micelles (RCLMs) were obtained by crosslinking the micellar shell with an imine structure. RCLMs showed good stability and excellent ability against extensive dilution by aqueous solution. In addition, the stability in different conditions with various pH values and glutathione (GSH) concentrations was studied. Then, the anticancer drug doxorubicin (DOX) was selected as the model drug to evaluate drug entrapment and release capacity of mixed micelles. The in vitro release profiles indicated that this RCLM had controlled drug release. In the simulated normal physiological environment (pH 7.4), the drug release of the RCLMs was restrained obviously, and the cumulative drug release content was only 25.7 during 72 h. When it came to acidic conditions (pH 5.0), de-crosslinking of the micelles occurred, as well as protonation of PDMAEMA blocks and micellar swelling at the same time, which enhanced the drug release to a large extent (81.4%, 72 h). Moreover, the drug release content was promoted further in the presence of the reductant GSH. In the condition of pH 5.0 with 10 mM GSH, disulfide bonds broke-up between the micelle core and shell, followed by shedding of the shell from the inner core. Then, the micellar disassembly (degradation) happened based on the de-crosslinking and swelling, and the drug release was as high as 95.3%. The MTT assay indicated that the CLSMs showed low cytotoxicity and good biocompatibility against the HepG2 cells. In contrast, the DOX-loaded CLSMs could efficiently restrain the proliferation of tumor cells, and the cell viability after 48 h incubation was just 13.2%, which was close to that of free DOX. This reversible cross-linked mixed micelle with pH/redox responsive behaviors is a potential nanocarrier for chemotherapy.

scholarly journals Recent developments in nano micelles as drug delivery system

2020 ◽  
Vol 11 (1) ◽  
pp. 176-184
Author(s):  
Pooja Mallya ◽  
Gowda D V ◽  
Mahendran B ◽  
Bhavya M V ◽  
Vikas Jain
Keyword(s):  
Drug Delivery ◽  
Colloidal Particles ◽  
Polymeric Micelles ◽  
Aggregation Number ◽  
Drug Loading ◽  
Polymer Concentration ◽  
Therapeutic Interventions ◽  
Solution Viscosity ◽  
Hydrophobic Core ◽  
Amphiphilic Copolymers

Targeting of the drug directly to the cells, tissues, or organs with no impact on healthy cells is a challenge. In the current era, it's been made possible by therapeutic interventions. The novel drug delivery systems such as nano particulates, liposomes, aquasomes, phytosomes, dendrimers, nano sponges, nano micelles are developed. Nano micelles are developed for efficient targeting and are currently in trend as therapeutic carriers of water-insoluble drugs. Micelles are self-assembling Nano-sized colloidal particles with a hydrophobic core and hydrophilic shell. Among the micelle-forming compounds, amphiphilic copolymers, i.e., polymers consisting of hydrophobic block and hydrophilic block, are gaining increasing attention. Polymeric micelles possess high stability both in vitro and in vivo with good biocompatibility. Nano micelles are used widely because of the smaller size range of 10 to 100nm, with greater drug loading capacity. Advantages over other dosage forms include solubilization of poorly soluble drugs, sustained release, protection of drugs from degradation and metabolism. The property discussed includes CMC, size, and aggregation number, and stability. CMC is the minimum polymer concentration required for micelle formation. Aggregation number (Nₐ) is the number of polymeric chains required to form micelles, and it ranges between tens to hundreds. Thermodynamic stability is based on size, the optical clarity of solution, viscosity, and surface tension. Kinetic stability accounts for micellar integrity. This review will discuss some recent trends in using micelles as pharmaceutical carriers such as to deliver drugs in conditions such as TB, cancer, ocular complications, etc.

Preparation of Interface-Cross-Linked Micelles as Drug Delivery via RAFT Polymerization

2013 ◽  
Vol 716 ◽  
pp. 147-152
Author(s):  
Jian Ping Li ◽  
Lian Lai Cui ◽  
Xin Tan ◽  
Ling Zhang
Keyword(s):  
Drug Delivery ◽  
Block Copolymer ◽  
Block Copolymers ◽  
Cell Line ◽  
Raft Polymerization ◽  
Drug Loading ◽  
Micellar System ◽  
Cross Link ◽  
Copolymer Micelle ◽  
Ring Open

Block copolymer PLA200-b-PPEGMEMA225 were prepared via ring-open polymerization and RAFT process. Further stabilization of the micellar system was performed in water using a dimethacrylate (EDGMA), and the RAFT to cross-link the interface. The interface-cross-linked micelle was found to present better properties than the uncross-linked block copolymer micelle during the drug loading and releasing experiment. Both block copolymers and cross-linked micelles show no toxicity on COS-7 cell line.

An Overview of Second Generation Nanoparticles− Nanostructure Lipid Carrier Drug Delivery System

2020 ◽  
Vol 13 (6) ◽  
pp. 5181-5189
Author(s):  
Prabhat Kumar Sahoo ◽  
Neha S.L ◽  
Arzoo Pannu
Keyword(s):  
Drug Delivery ◽  
Drug Delivery System ◽  
Delivery System ◽  
Second Generation ◽  
Drug Loading ◽  
Scale Up ◽  
Delivery Systems ◽  
Route Of Administration ◽  
Random Structure ◽  
Stability Parameters

Lipids are used as vehicles for the preparation of various formulations prescribed for administrations, including emulsions, ointments, suspension, tablets, and suppositories. The first parental nano-emulsion was discovered from the 1950s when it was added to the intravenous administration of lipid and lipid-soluble substances. Lipid-based drug delivery systems are important nowadays. Solid nanoparticles (SLN) and Nanostructured lipid carriers (NLC) are very proficient due to the ease of production process, scale-up capability, bio-compatibility, the biodegradability of formulation components and other specific features of the proposed route. The administration or nature of the materials must be loaded into these delivery systems. The main objectives of this review are to discuss an overview of second-generation nanoparticles, their limitations, structures, and route of administration, with emphasis on the effectiveness of such formulations. NLC is the second generation of lipid nanoparticles having a structure like nanoemulsion. The first generation of nanoparticles was SLN. The difference between both of them is at its core. Both of them are a colloidal carrier in submicron size in the range of 40-1000 nm. NLC is the most promising novel drug delivery system over the SLN due to solving the problem of drug loading and drug crystallinity. Solid and liquid lipids combination in NLC formation, improve its quality as compare to SLN. NLC has three types of structures: random, amorphous, and multiple. The random structure containing solid-liquid lipids and consisting crystal and the liquid lipid irregular in shape; thereby enhance the ability of the lipid layer to pass through the membrane. The second is the amorphous structure. It is less crystalline in nature and can prevent the leakage of the loaded drug. The third type is multiple structures, which have higher liquid lipid concentrations than other types. The excipients used to form the NLC are bio-compatible, biodegradable and non-irritating, most of which can be detected using GRAS. NLC is a promising delivery system to deliver the drug through pulmonary, ocular, CNS, and oral route of administration. Various methods of preparation and composition of NLC influence its stability Parameters. In recent years at the educational level, the potential of NLC as a delivery mechanism targeting various organs has been investigated in detail.

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.

Formulating SLN and NLC as Innovative Drug Delivery Systems for Non-Invasive Routes of Drug Administration

2020 ◽  
Vol 27 (22) ◽  
pp. 3623-3656 ◽  
Author(s):  
Bruno Fonseca-Santos ◽  
Patrícia Bento Silva ◽  
Roberta Balansin Rigon ◽  
Mariana Rillo Sato ◽  
Marlus Chorilli
Keyword(s):  
Drug Delivery ◽  
Particle Size ◽  
Drug Release ◽  
Drug Loading ◽  
Average Particle Size ◽  
Delivery Systems ◽  
Average Particle ◽  
Minor Importance ◽  
Routes Of Administration ◽  
Non Invasive

Colloidal carriers diverge depending on their composition, ability to incorporate drugs and applicability, but the common feature is the small average particle size. Among the carriers with the potential nanostructured drug delivery application there are SLN and NLC. These nanostructured systems consist of complex lipids and highly purified mixtures of glycerides having varying particle size. Also, these systems have shown physical stability, protection capacity of unstable drugs, release control ability, excellent tolerability, possibility of vectorization, and no reported production problems related to large-scale. Several production procedures can be applied to achieve high association efficiency between the bioactive and the carrier, depending on the physicochemical properties of both, as well as on the production procedure applied. The whole set of unique advantages such as enhanced drug loading capacity, prevention of drug expulsion, leads to more flexibility for modulation of drug release and makes Lipid-based nanocarriers (LNCs) versatile delivery system for various routes of administration. The route of administration has a significant impact on the therapeutic outcome of a drug. Thus, the non-invasive routes, which were of minor importance as parts of drug delivery in the past, have assumed added importance drugs, proteins, peptides and biopharmaceuticals drug delivery and these include nasal, buccal, vaginal and transdermal routes. The objective of this paper is to present the state of the art concerning the application of the lipid nanocarriers designated for non-invasive routes of administration. In this manner, this review presents an innovative technological platform to develop nanostructured delivery systems with great versatility of application in non-invasive routes of administration and targeting drug release.

Advances in the use of MOFs for Cancer Diagnosis and Treatment: An Overview

2020 ◽  
Vol 26 (33) ◽  
pp. 4174-4184
Author(s):  
Marina P. Abuçafy ◽  
Bruna L. da Silva ◽  
João A. Oshiro-Junior ◽  
Eloisa B. Manaia ◽  
Bruna G. Chiari-Andréo ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Drug Delivery Systems ◽  
Rational Design ◽  
Gas Adsorption ◽  
Drug Loading ◽  
Drug Carriers ◽  
Delivery Systems ◽  
Academic Community ◽  
Anticancer Drug Delivery ◽  
Diagnostic Agents

Nanoparticles as drug delivery systems and diagnostic agents have gained much attention in recent years, especially for cancer treatment. Nanocarriers improve the therapeutic efficiency and bioavailability of antitumor drugs, besides providing preferential accumulation at the target site. Among different types of nanocarriers for drug delivery assays, metal-organic frameworks (MOFs) have attracted increasing interest in the academic community. MOFs are an emerging class of coordination polymers constructed of metal nodes or clusters and organic linkers that show the capacity to combine a porous structure with high drug loading through distinct kinds of interactions, overcoming the limitations of traditional drug carriers explored up to date. Despite the rational design and synthesis of MOFs, structural aspects and some applications of these materials like gas adsorption have already been comprehensively described in recent years; it is time to demonstrate their potential applications in biomedicine. In this context, MOFs can be used as drug delivery systems and theranostic platforms due to their ability to release drugs and accommodate imaging agents. This review describes the intrinsic characteristics of nanocarriers used in cancer therapy and highlights the latest advances in MOFs as anticancer drug delivery systems and diagnostic agents.

Sign in / Sign up

Export Citation Format

Share Document