Dithiol-PEG-PDLLA Micelles: Preparation and Evaluation as Potential Topical Ocular Delivery Vehicle

Yang, Jian; Yan, Jing; Zhou, Zheng; Amsden, Brian G.

doi:10.1021/bm4018879

Cited by 46 publications

(26 citation statements)

References 32 publications

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“…Instead, the product mixture was directly used for the subsequent polymerization step, since HOOC-PEG-COOH was inert under the ring-open polymerization conditions. As a result, a monocarboxyl-terminated block-polymer HOOC-PEG-PLA was obtained in the presence of unreacted HOOC-PEG-COOH, which was able to be removed by hot water washing [25]. Finally, HEMI was connected to HOOC-PEG-PLA via an esterification reaction, affording Mal-PEG-PLA.…”

Section: Synthesis Of Mal-peg-plamentioning

confidence: 99%

Cell-Penetrating Peptide Modified PEG-PLA Micelles for Efficient PTX Delivery

Shuai

Cai

Zhao

et al. 2020

IJMS

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On account of their excellent capacity to significantly improve the bioavailability and solubility of chemotherapy drugs, amphiphilic block copolymer-based micelles have been widely utilized for chemotherapy drug delivery. In order to further improve the antitumor ability and to also reduce undesired side effects of drugs, cell-penetrating peptides have been used to functionalize the surface of polymer micelles endowed with the ability to target tumor tissues. Herein, we first synthesized functional polyethylene glycol-polylactic acid (PEG-PLA) tethered with maleimide at the PEG section of the block polymer, which was further conjugated with a specific peptide, the transactivating transcriptional activator (TAT), with an approved capacity of aiding translocation across the plasma membrane. Then, TAT-conjugated, paclitaxel-loaded nanoparticles were self-assembled into stable nanoparticles with a favorable size of 20 nm, and displayed a significantly increased cytotoxicity, due to their enhanced accumulation via peptide-mediated cellular association in human breast cancer cells (MCF-7) in vitro. But when further used in vivo, TAT-NP-PTX showed an acceleration of the drug's plasma clearance rate compared with NP-PTX, and therefore weakened its antitumor activities in the mice model, because of its positive charge, its elimination by the endoplasmic reticulum system more quickly, and its targeting effect on normal cells leading towards being more toxic. So further modification of TAT-NP-PTX to shield TAT peptide's positive charges may be a hot topic to overcome the present dilemma.

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Section: Synthesis Of Mal-peg-plamentioning

confidence: 99%

Cell-Penetrating Peptide Modified PEG-PLA Micelles for Efficient PTX Delivery

Shuai

Cai

Zhao

et al. 2020

IJMS

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“…5 Mucoadhesivity of micelles can be improved by incorporating the functional groups, which are capable of binding to the chemical groups present within mucosa. 77 Thiol is a good example of these functional groups that can interact with cysteine that is available in abundance in the mucin layer. 78 Therefore, materials containing thiol groups can be easily attached to the mucin‏ layer and thus enhance the residence time.…”

Section: Introductionmentioning

confidence: 99%

Novel Pentablock Copolymers as Thermosensitive Self-Assembling Micelles for Ocular Drug Delivery

Alami-Milani¹,

Zakeri–Milani²,

Valizadeh³

et al. 2017

Adv Pharm Bull

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Many studies have focused on how drugs are formulated in the sol state at room temperature leading to the formation of in situ gel at eye temperature to provide a controlled drug release. Stimuli-responsive block copolymer hydrogels possess several advantages including uncomplicated drug formulation and ease of application, no organic solvent, protective environment for drugs, site-specificity, prolonged and localized drug delivery, lower systemic toxicity, and capability to deliver both hydrophobic and hydrophilic drugs. Self-assembling block copolymers (such as diblock, triblock, and pentablock copolymers) with large solubility variation between hydrophilic and hydrophobic segments are capable of making temperature-dependent micellar assembles, and with further increase in the temperature, of jellifying due to micellar aggregation. In general, molecular weight, hydrophobicity, and block arrangement have a significant effect on polymer crystallinity, micelle size, and in vitro drug release profile. The limitations of creature triblock copolymers as initial burst release can be largely avoided using micelles made of pentablock copolymers. Moreover, formulations based on pentablock copolymers can sustain drug release for a longer time. The present study aims to provide a concise overview of the initial and recent progresses in the design of hydrogel-based ocular drug delivery systems.

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“…In comparison to our systems, other polymeric micelles recently used for Dex encapsulation exhibited lower loading capacities. A loading capacity in the range 0.5–3% was observed for Dex-loaded micelles composed of poly(ethylene glycol) (PEG) as a hydrophilic part, and poly(butyl methacrylate) 53 , poly(D,L-lactide) 54 , poly(ε-caprolactone) (PCL) 55 , 56 and poly(propylene glycol) 57 , respectively, as a hydrophobic core. Slightly higher loading capacities (from 7 to 12%) were reported for PEG-PCL micelles loaded with Dex-acetate.…”

Section: Resultsmentioning

confidence: 99%

Investigation of drug release modulation from poly(2-oxazoline) micelles through ultrasound

Salgarella

Zahoranová

Šrámková

et al. 2018

Sci Rep

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Among external stimuli used to trigger release of a drug from a polymeric carrier, ultrasound has gained increasing attention due to its non-invasive nature, safety and low cost. Despite this attention, there is only limited knowledge about how materials available for the preparation of drug carriers respond to ultrasound. This study investigates the effect of ultrasound on the release of a hydrophobic drug, dexamethasone, from poly(2-oxazoline)-based micelles. Spontaneous and ultrasound-mediated release of dexamethasone from five types of micelles made of poly(2-oxazoline) block copolymers, composed of hydrophilic poly(2-methyl-2-oxazoline) and hydrophobic poly(2-n-propyl-2-oxazoline) or poly(2-butyl-2-oxazoline-co-2-(3-butenyl)-2-oxazoline), was studied. The release profiles were fitted by zero-order and Ritger-Peppas models. The ultrasound increased the amount of released dexamethasone by 6% to 105% depending on the type of copolymer, the amount of loaded dexamethasone, and the stimulation time point. This study investigates for the first time the interaction between different poly(2-oxazoline)-based micelle formulations and ultrasound waves, quantifying the efficacy of such stimulation in modulating dexamethasone release from these nanocarriers.

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Dithiol-PEG-PDLLA Micelles: Preparation and Evaluation as Potential Topical Ocular Delivery Vehicle

Cited by 46 publications

References 32 publications

Cell-Penetrating Peptide Modified PEG-PLA Micelles for Efficient PTX Delivery

Cell-Penetrating Peptide Modified PEG-PLA Micelles for Efficient PTX Delivery

Novel Pentablock Copolymers as Thermosensitive Self-Assembling Micelles for Ocular Drug Delivery

Investigation of drug release modulation from poly(2-oxazoline) micelles through ultrasound

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