scholarly journals Polymeric Micelles: A Novel Approach towards Nano-Drug Delivery System

2021 ◽  
Vol 18 (4) ◽  
pp. 629-649
Author(s):  
Rutuja Hemant Vinchurkar ◽  
Ashwin Bhanudas Kuchekar
Keyword(s):  
Drug Delivery ◽  
Self Assembly ◽  
Inner Core ◽  
Polymeric Micelles ◽  
Solvent Polarity ◽  
Physicochemical Characteristics ◽  
Polymeric Micelle ◽  
Absorption Mechanism ◽  
Novel Approach ◽  
Poorly Soluble

Nano delivery systems, polymeric micelles represent one of the most promising delivery platforms for therapeutic compounds. It has shown that a poorly soluble molecule which has high potency and remarkable toxicity can be encapsulated with the polymeric micelle. There are various poorly soluble drugs used in micellar preparations, mostly for their anti-cancer activity. Drugs in the inner core protect the drug from degradation and allow drug accumulation in the tumour site in the case of cancer treatment. Block copolymers are chosen based on the physicochemical characteristics of medicinal drugs. The amphiphilic block copolymer structure has both lipophilic and hydrophilic blocks, which enclose tiny hydrophobic molecules. It is a targeted drug delivery method because of its high effectiveness for drug retention in tissue, prevention of enzymes from degradation, and improvement of the cellular absorption mechanism. In an experimental environment, variations in temperature and solvent polarity stimulate copolymer micelle self-assembly. This is a thermodynamically guided procedure in which self-assembly happens by converting polymeric micelles. These aggregates go from a non-equilibrium to a thermodynamically equilibrium state, and they stay stable for a long time. The balance of thermodynamic and kinetic forces is critical in micelles self-assembly because the kinetic process predicts assembly behaviour and hierarchical structure. The purpose of this special issue is to provide an updated overview of micelles, a number of polymers and drugs commonly used in micellar preparation and their application.

Enzyme-responsive polymeric micelles with fluorescence fabricated through aggregation-induced copolymer self-assembly for anticancer drug delivery

2020 ◽  
Vol 11 (48) ◽  
pp. 7704-7713
Author(s):  
Ke Yan ◽  
Shujing Zhang ◽  
Kun Zhang ◽  
Yalei Miao ◽  
Yudian Qiu ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Anticancer Drug ◽  
Self Assembly ◽  
Polymeric Micelles ◽  
Polymeric Micelle ◽  
Anticancer Drug Delivery ◽  
Hydrophobic Chain

The TPE moiety with AIE is employed as functional hydrophobic chain to induce copolymer self-assembly and form polymeric micelle that can show enzyme-responsive drug delivery.

Polymeric Micelles for Enhanced Solubility of Meloxicam in Oral Drug Delivery

2014 ◽  
Vol 1060 ◽  
pp. 7-11
Author(s):  
Thisirak Woraphatphadung ◽  
Warayuth Sajomsang ◽  
Theerasak Rojanarata ◽  
Tanasait Ngawhirunpat ◽  
Praneet Opanasopit
Keyword(s):  
Drug Delivery ◽  
Inner Core ◽  
Polymeric Micelles ◽  
Oral Drug Delivery ◽  
Polymeric Micelle ◽  
Oral Drug ◽  
Hydrophobic Drug ◽  
Enhanced Solubility ◽  
Incorporation Efficiency

N-arylsuccinyl chitosan was successfully synthesized by introducing hydrophobic and hydrophilic moieties into the chitosan backbone. Incorporation efficiency of the drug-loaded micelles, particle size, in vitro cytotoxicity, and in vitro drug release were investigated. Meloxicam (MX) as a model drug was loaded into the inner core of the micelles by solvent evaporation method. The critical micelle concentration (CMC) of micelles was found to be 0.0385 mg/ml. N-arylsuccinyl chitosan micelles were able to entrap hydrophobic drug (MX) and have particle sizes in the range of 342.1- 444.2 nm. The micelles could enhance solubility of MX with high incorporation efficiency (32.72%). The cytotoxicity in Caco-2 cells to be dependent on the concentration of N-arylsuccinyl chitosan with the IC50 value of 3.23 +/- 0.08 mg/ml. Therefore, N-arylsuccinyl chitosan polymeric micelle presents interest to improve solubility of hydrophobic drug for oral drug delivery.

Novel biocompatible fluorescent polymeric micelles based on 1,8-naphthalimide derivatives for cell imaging

2015 ◽  
Vol 6 (3) ◽  
pp. 364-368 ◽  
Author(s):  
Bei-Yu Liu ◽  
Wan-Xia Wu ◽  
Na Wang ◽  
Xiao-Qi Yu
Keyword(s):  
Self Assembly ◽  
Cell Imaging ◽  
Polymeric Micelles ◽  
Ph Sensor ◽  
Polymeric Micelle ◽  
Living Cells ◽  
Amphiphilic Block Copolymers ◽  
Good Potential ◽  
New Type ◽  
Good Biocompatibility

A new type of fluorescent polymeric micelle was developed by the aqueous self-assembly from amphiphilic block copolymers via click chemistry and showed good potential for application in cell imaging with good biocompatibility. Notably, P1 can readily serve as an excellent intracellular pH sensor in whole living cells based on PET inhibition

Biodegradable poly(ethylene glycol)–poly(ε-carprolactone) polymeric micelles with different tailored topological amphiphilies for doxorubicin (DOX) drug delivery

RSC Advances ◽  
2016 ◽  
Vol 6 (63) ◽  
pp. 58160-58172 ◽  
Author(s):  
Y. Chen ◽  
Y. X. Zhang ◽  
Z. F. Wu ◽  
X. Y. Peng ◽  
T. Su ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Ethylene Glycol ◽  
Self Assembly ◽  
Polymeric Micelles ◽  
The Self ◽  
Molar Ratio ◽  
Poly Ethylene Glycol ◽  
Biodegradable Poly ◽  
Poly Ethylene

The self-assembly and drug release of the three PEG–PCL copolymers with different topologies but identical molar ratio between PEG to PCL.

scholarly journals VP6-SUMO Self-Assembly as Nanocarriers for Gastrointestinal Delivery

2015 ◽  
Vol 2015 ◽  
pp. 1-7 ◽  
Author(s):  
V. Palmieri ◽  
F. Bugli ◽  
M. Papi ◽  
G. Ciasca ◽  
G. Maulucci ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Self Assembly ◽  
Oral Delivery ◽  
Drug Stability ◽  
Intestinal Cells ◽  
Chimeric Construct ◽  
Poorly Soluble ◽  
Epithelial Barriers ◽  
Natural Target ◽  
Poor Absorption

High proteolytic degradation and poor absorption through epithelial barriers are major challenges to successful oral delivery of therapeutics. Nanoparticle platforms can enhance drug stability and extend the residence time in gastrointestinal (GI) tract. However, drug delivery systems are often inactivated in acidic environment of stomach or suffer poor absorption from intestinal cells due to the mucus layer. To overcome these issues we developed a drug delivery system constituted by a protein construct made by a Rotavirus capsid protein (VP6) and the small ubiquitin-like modifier SUMO. This chimeric construct allows specificity towards intestinal cells, the Rotavirus natural target, combined by an enhanced stability given by the eukaryotic protein transporter SUMO. Furthermore SUMO can act as a molecular switch that facilitates import/export of its ligand to the nucleus, the hypersensitive subcellular site target of many cell killing therapies. In this paper we show that SUMO-VP6 constructs self-assembly into stable nanocarriers. SUMO-VP6 nanocarriers display ideal features for drug delivery: a small size and high monodispersity, a high stability in different pH conditions and a high uptake in the nuclear and cytoplasmic compartment of intestinal cells. These features make SUMO-VP6 nanocarriers a promising novel system for oral delivery of poorly soluble drugs.

scholarly journals Polymeric micelles for oral drug delivery: Why and how

2004 ◽  
Vol 76 (7-8) ◽  
pp. 1321-1335 ◽  
Author(s):  
M. F. Francis ◽  
Mariana Cristea ◽  
F. M. Winnik
Keyword(s):  
Drug Delivery ◽  
Oral Delivery ◽  
Oral Absorption ◽  
Polymeric Micelles ◽  
Oral Drug Delivery ◽  
Polymeric Micelle ◽  
Water Soluble ◽  
Oral Drug ◽  
Therapeutic Effects ◽  
The Impact

The oral delivery of drugs is regarded as the optimal means for achieving therapeutic effects owing to increased patient compliance. Unfortunately, the oral delivery route is beset with problems such as gastrointestinal (GI) destruction of labile molecules, low levels of macromolecular absorption, etc. To reduce the impact of digestive enzymes and to ensure the absorption of bioactive agents in an unaltered form, molecules may be incorporated into microparticulate carriers. Many approaches to achieve the oral absorption of a wide variety of drugs are currently under investigation. Among the different polymer-based drug delivery systems, polymeric micelles represent a promising delivery vehicle especially intended for poorly water-soluble pharmaceutical active ingredients in order to improve their oral bioavailability. Recent findings of a dextran-based polymeric micelle study for solubilization of a highly lipophilic drug, cyclosporin A (CsA), will be discussed.

scholarly journals Acid-Responsive Adamantane-Cored Amphiphilic Block Polymers as Platforms for Drug Delivery

Nanomaterials ◽  
2021 ◽  
Vol 11 (1) ◽  
pp. 188
Author(s):  
Weiqiu Wen ◽  
Chong Guo ◽  
Jianwei Guo
Keyword(s):  
Drug Delivery ◽  
Polymeric Micelles ◽  
Drug Loading ◽  
Controlled Drug Release ◽  
Polymeric Micelle ◽  
Monomethyl Ether ◽  
Particle Sizes ◽  
Anticancer Efficacy ◽  
Decrease Rate ◽  
Anticancer Drug Delivery

Four-arm star-shaped (denoted as ‘S’) polymer adamantane-[poly(lactic-co-glycolic acid)-b-poly(N,N’-diethylaminoethyl methacrylate) poly(ethylene glycol) monomethyl ether]4 (S-PLGA-D-P) and its linear (denoted as ‘L’) counterpart (L-PLGA-D-P) were synthesized, then their self-assembled micelles were further developed to be platforms for anticancer drug delivery. Two types of polymeric micelles exhibited strong pH-responsiveness and good drug loading capacity (21.6% for S-PLGA-D-P and 22.9% for L-PLGA-D-P). Using doxorubicin (DOX) as the model drug, their DOX-loaded micelles displayed well controlled drug release behavior (18.5–19.0% of DOX release at pH 7.4 and 77.6–78.8% of DOX release at pH 5.0 within 80 h), good cytocompatibility against NIH-3T3 cells and effective anticancer efficacy against MCF-7 cells. However, the star-shaped polymeric micelles exhibited preferable stability, which was confirmed by the lower critical micelle concentration (CMC 0.0034 mg/mL) and decrease rate of particle sizes after 7 days incubation (3.5%), compared with the linear polymeric micelle L-PLGA-D-P (CMC 0.0070 mg/mL, decrease rate of particle sizes was 9.6%). Overall, these developed polymeric micelles have promising application as drug delivery system in cancer therapy.

scholarly journals Self-Assembling Peptides and Their Application in the Treatment of Diseases

2019 ◽  
Vol 20 (23) ◽  
pp. 5850 ◽  
Author(s):  
Lee ◽  
Trinh ◽  
Yoo ◽  
Shin ◽  
Lee ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Controlled Release ◽  
Side Effects ◽  
Tissue Regeneration ◽  
Environmental Conditions ◽  
Self Assembly ◽  
Basic Structure ◽  
Physicochemical Characteristics ◽  
Self Assembling ◽  
Structural Divergence

Self-assembling peptides are biomedical materials with unique structures that are formed in response to various environmental conditions. Governed by their physicochemical characteristics, the peptides can form a variety of structures with greater reactivity than conventional non-biological materials. The structural divergence of self-assembling peptides allows for various functional possibilities; when assembled, they can be used as scaffolds for cell and tissue regeneration, and vehicles for drug delivery, conferring controlled release, stability, and targeting, and avoiding side effects of drugs. These peptides can also be used as drugs themselves. In this review, we describe the basic structure and characteristics of self-assembling peptides and the various factors that affect the formation of peptide-based structures. We also summarize the applications of self-assembling peptides in the treatment of various diseases, including cancer. Furthermore, the in-cell self-assembly of peptides, termed reverse self-assembly, is discussed as a novel paradigm for self-assembling peptide-based nanovehicles and nanomedicines.

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