scholarly journals Complex Polymeric Architectures Self-Assembling in Unimolecular Micelles: Preparation, Characterization and Drug Nanoencapsulation

Pharmaceutics ◽  
2018 ◽  
Vol 10 (4) ◽  
pp. 209 ◽  
Author(s):  
Stefania Ordanini ◽  
Francesco Cellesi
Keyword(s):  
Single Molecule ◽  
Drug Delivery Systems ◽  
Polymeric Micelles ◽  
Analytical Techniques ◽  
Hydrophobic Core ◽  
Guest Molecules ◽  
Self Assembling ◽  
Dendritic Core ◽  
Supramolecular Aggregates ◽  
Hydrophilic Shell

Unimolecular polymeric micelles are a class of single-molecule amphiphilic core-shell polymeric architectures, where the hydrophobic core is well stabilized by the hydrophilic shell, avoiding intermolecular core-core interactions. Multi-arm copolymers with a dendritic core, as well as hyperbranched and comb-like polymers, can form unimolecular micelles easily. In this review, examples of polymers able to form detectable unimolecular micelles will be presented, summarizing the analytical techniques used to characterize the unimolecular micelles and discriminate them from other supramolecular aggregates, such as multi-micelle aggregates. Unimolecular micelles are suitable for the nanoencapsulation of guest molecules. Compared to traditional supramolecular micelles, unimolecular micelles do not disassemble under dilution and are stable to environmental modifications. Recent examples of their application as drug delivery systems, endowed with increased stability and transport properties, will be discussed.

scholarly journals Development and Characterization of Lecithin-based Self-assembling Mixed Polymeric Micellar (saMPMs) Drug Delivery Systems for Curcumin

2016 ◽  
Vol 6 (1) ◽  
Author(s):  
Ling-Chun Chen ◽  
Yin-Chen Chen ◽  
Chia-Yu Su ◽  
Wan-Ping Wong ◽  
Ming-Thau Sheu ◽  
...  
Keyword(s):  
Particle Size ◽  
Polymeric Micelles ◽  
Drug Loading ◽  
Physical Stability ◽  
Sodium Deoxycholate ◽  
Hydrophobic Core ◽  
Self Assembling ◽  
Human Disorders

Abstract Self-assembling mixed polymeric micelles (saMPMs) were developed for overcoming major obstacles of poor bioavailability (BA) associated with curcumin delivery. Lecithin added was functioned to enlarge the hydrophobic core of MPMs providing greater solubilization capacity. Amphiphilic polymers (sodium deoxycholate [NaDOC], TPGS, CREMOPHOR, or a PLURONIC series) were examined for potentially self-assembling to form MPMs (saMPMs) with the addition of lecithin. Particle size, size distribution, encapsulation efficacy (E.E.), and drug loading (D.L.) of the mixed micelles were optimally studied for their influences on the physical stability and release of encapsulated drugs. Overall, curcumin:lecithin:NaDOC and curcumin:lecithin:PLURONIC P123 in ratios of 2:1:5 and 5:2:20, respectively, were optimally obtained with a particle size of < 200 nm, an E.E. of >80%, and a D.L. of >10%. The formulated system efficiently stabilized curcumin in phosphate-buffered saline (PBS) at room temperature or 4 °C and in fetal bovine serum or PBS at 37 °C and delayed the in vitro curcumin release. In vivo results further demonstrated that the slow release of curcumin from micelles and prolonged duration increased the curcumin BA followed oral and intravenous administrations in rats. Thus, lecithin-based saMPMs represent an effective curcumin delivery system, and enhancing BA of curcumin can enable its wide applications for treating human disorders.

scholarly journals Polymeric Micelles for the Enhanced Deposition of Hydrophobic Drugs into Ocular Tissues, without Plasma Exposure

Pharmaceutics ◽  
2021 ◽  
Vol 13 (5) ◽  
pp. 744
Author(s):  
Ijeoma F. Uchegbu ◽  
Jan Breznikar ◽  
Alessandra Zaffalon ◽  
Uche Odunze ◽  
Andreas G. Schätzlein
Keyword(s):  
Polymeric Micelles ◽  
Rabbit Model ◽  
Penetration Enhancer ◽  
Hydrophobic Drugs ◽  
Ocular Tissues ◽  
Ocular Penetration ◽  
Self Assembling ◽  
Similar Dose ◽  
Oil In Water ◽  
The Stability

Commercial topical ocular formulations for hydrophobic actives rely on the use of suspensions or oil in water emulsions and neither of these formulation modalities adequately promote drug penetration into ocular tissues. Using the ocular relevant hydrophobic drug, cyclosporine A (CsA), a non-irritant ocular penetration enhancer is showcased, which may be used for the formulation of hydrophobic actives. The activity of this penetration enhancer is demonstrated in a healthy rabbit model. The Molecular Envelope Technology (MET) polymer (N-palmitoyl-N-monomethyl-N,N-dimethyl-N,N,N-trimethyl-6-O-glycolchitosan), a self-assembling, micelle-forming polymer, was used to formulate CsA into sterile filtered nanoparticulate eye drop formulations and the stability of the formulation tested. Healthy rabbits were dosed with a single dose of a MET–CsA (NM133) 0.05% formulation and ocular tissues analyzed. Optically clear NM133 formulations were prepared containing between 0.01–0.1% w/v CsA and 0.375–0.75% w/v MET polymer. NM133 0.01%, NM133 0.02% and NM133 0.05% were stable for 28 days when stored at refrigeration temperature (5–6 °C) and room temperature (16–23 °C), but there was evidence of evaporation of the formulation at 40 °C. There was no change in drug content when NM133 0.05% was stored for 387 days at 4 °C. On topical dosing to rabbits, corneal, conjunctival and scleral AUC0–24 levels were 25,780 ng.h g−1, 12,046 ng.h g−1 and 5879 ng.h g−1, respectively, with NM133 0.05%. Meanwhile, a similar dose of Restasis 0.05% yielded lower values of 4726 ng.h/g, 4813 ng.h/g and 1729 ng.h/g for the drug corneal, conjunctival and scleral levels, respectively. NM133 thus delivered up to five times more CsA to the ocular surface tissues when compared to Restasis. The MET polymer was non-irritant up to a concentration of 4% w/v. The MET polymer is a non-irritant ocular penetration enhancer that may be used to deliver hydrophobic drugs in optically clear topical ocular formulations.

scholarly journals The behavior of hydrophobic-core/hydrophilic-shell structured microgels at an interface: from Mickering emulsion to colloidosomes with dual-level controlled permeability

RSC Advances ◽  
2016 ◽  
Vol 6 (97) ◽  
pp. 95067-95072 ◽  
Author(s):  
Yi Gong ◽  
Mao Wang ◽  
Jianying He
Keyword(s):  
Hydrophobic Core ◽  
Coarse Level ◽  
Controllable Release ◽  
Model Drug ◽  
Hydrophilic Shell

The release of model drug FITC-Dex from colloidosomes was examined in selected media and the controllable release was achieved by adjusting the pH (coarse level) and the ratio of the shell to core in the microgels (fine level).

Strategies to improve insulin delivery through oral route: A review

2021 ◽  
Vol 18 ◽  
Author(s):  
Rohini Bhattacharya ◽  
Asha P. Johnson ◽  
Shailesh T. ◽  
Mohamed Rahamathulla ◽  
Gangadharappa H. V.
Keyword(s):  
Diabetes Mellitus ◽  
Drug Delivery ◽  
Drug Delivery Systems ◽  
Polymeric Micelles ◽  
Insulin Delivery ◽  
Peptide Hormone ◽  
Diabetes Mellitus Type 1 ◽  
Delivery Systems ◽  
Oral Insulin ◽  
Subcutaneous Route

: Diabetes mellitus is found to be among the most suffered and lethal diseases for mankind. Diabetes mellitus type-1 is caused by the demolition of pancreatic islets responsible for the secretion of insulin. Insulin is the peptide hormone (anabolic] that regulates the metabolism of carbohydrates, fats, and proteins. Upon the breakdown of the natural process of metabolism, the condition leads to hyperglycemia (increased blood glucose levels]. Hyperglycemia demands outsourcing of insulin. The subcutaneous route was found to be the most stable route of insulin administration but faces patient compliance problems. Oral Insulin delivery systems are the patient-centered and innovative novel drug delivery system, eliminating the pain caused by the subcutaneous route of administration. Insulin comes in contact across various barriers in the gastrointestinal tract, which has been discussed in detail in this review. The review describes about the different bioengineered formulations, including microcarriers, nanocarriers, Self-Microemulsifying drug delivery systems (SMEDDs), Self-Nanoemulsifying drug delivery systems (SNEDDs), polymeric micelles, cochleates, etc. Surface modification of the carriers is also possible by developing ligand anchored bioconjugates. A study on evaluation has shown that the carrier systems facilitate drug encapsulation without tampering the properties of insulin. Carrier-mediated transport by the use of natural, semi-synthetic, and synthetic polymers have shown efficient results in drug delivery by protecting insulin from harmful environment. This makes the formulation readily acceptable for a variety of populations. The present review focuses on the properties, barriers present in the GI tract, overcome the barriers, strategies to formulate oral insulin formulation by enhancing the stability and bioavailability of insulin.

Polymeric micelles as drug delivery systems in cancer: challenges and opportunities

Nanomedicine ◽  
2021 ◽  
Author(s):  
Swati Biswas
Keyword(s):  
Drug Delivery ◽  
Drug Delivery Systems ◽  
Polymeric Micelles ◽  
Delivery Systems ◽  
Clinical Translation ◽  
Current Status ◽  
Chemotherapeutic Drugs ◽  
Challenges And Opportunities

Tweetable abstract Micelles are nanocarriers for hydrophobic chemotherapeutic drugs. This editorial discusses the current status of preclinical micellar research and sheds light on the possibility of their clinical translation.

scholarly journals Novel polymeric micelles for insect pest control: encapsulation of essential oil monoterpenes inside a triblock copolymer shell for head lice control

PeerJ ◽  
2017 ◽  
Vol 5 ◽  
pp. e3171 ◽  
Author(s):  
Alejandro Lucia ◽  
Ariel Ceferino Toloza ◽  
Eduardo Guzmán ◽  
Francisco Ortega ◽  
Ramón G. Rubio
Keyword(s):  
Essential Oil ◽  
Pest Control ◽  
Polymeric Micelles ◽  
Ex Vivo ◽  
Insect Pest ◽  
Immersion Test ◽  
Poloxamer 407 ◽  
Head Lice ◽  
Hydrophobic Core ◽  
Micellar Systems

BackgroundEssential oil components (EOCs) are molecules with interesting application in pest control, these have been evaluated against different insect pest from more than 100 years, but their practical use is rather limited. Thus, the enhancement of their bioavailability and manageability due to their dispersion in water can open new perspective for the preparation of formulations for the control of insect pest. In this work, we studied the encapsulation of different monoterpenes in a poloxamer shell in order to prepare aqueous formulations that can be used for the development of platforms used in pest control.MethodsMicellar systems containing a 5 wt% of poloxamer 407 and 1.25 wt% of the different monoterpenes were prepared. Dynamic Light Scattering (DLS) experiments were carried out to characterize the dispersion of the EOCs in water. The pediculicidal activity of these micellar systems was tested on head lice using anex vivoimmersion test.ResultsThe poloxamers allowed the dispersion of EOCs in water due to their encapsulation inside the hydrophobic core of the copolymer micelles. From this study, we concluded that it is possible to make stable micellar systems containing water (>90 wt%), 1.25 wt% of different monoterpenes and a highly safe polymer (5wt% Poloxamer 407). These formulations were effective against head lice with mortality ranging from 30 to 60%, being the most effective emulsions those containing linalool, 1,8-cineole,α-terpineol, thymol, eugenol, geraniol and nonyl alcohol which lead to mortalities above 50%.DiscussionSince these systems showed good pediculicidal activity and high physicochemical stability, they could be a new route for the green fabrication of biocompatible and biosustainable insecticide formulations.

scholarly journals Cross-plane transport in a single-molecule two-dimensional van der Waals heterojunction

2020 ◽  
Vol 6 (22) ◽  
pp. eaba6714 ◽  
Author(s):  
Shiqiang Zhao ◽  
Qingqing Wu ◽  
Jiuchan Pi ◽  
Junyang Liu ◽  
Jueting Zheng ◽  
...  
Keyword(s):  
Charge Transport ◽  
Single Molecule ◽  
Density Functional ◽  
Electronic Materials ◽  
2D Materials ◽  
Molecular Layer ◽  
Van Der Waals ◽  
Density Functional Theory Calculations ◽  
Two Dimensional ◽  
Guest Molecules

Two-dimensional van der Waals heterojunctions (2D-vdWHs) stacked from atomically thick 2D materials are predicted to be a diverse class of electronic materials with unique electronic properties. These properties can be further tuned by sandwiching monolayers of planar organic molecules between 2D materials to form molecular 2D-vdWHs (M-2D-vdWHs), in which electricity flows in a cross-plane way from one 2D layer to the other via a single molecular layer. Using a newly developed cross-plane break junction technique, combined with density functional theory calculations, we show that M-2D-vdWHs can be created and that cross-plane charge transport can be tuned by incorporating guest molecules. The M-2D-vdWHs exhibit distinct cross-plane charge transport signatures, which differ from those of molecules undergoing in-plane charge transport.

Sign in / Sign up

Export Citation Format

Share Document