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

Liu, Xingzheng; Fan, Rongrong; Lu, B; Le, Yuan

doi:10.3390/pharmaceutics10040230

Cited by 9 publications

(5 citation statements)

References 30 publications

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“…Thorough dialysis method has been widely used in polymer micelles prepared for simple operating processors ( Nah et al, 1998 ; Liu et al, 2018 ; Zhao et al, 2020 ). We successfully prepared the AS-loaded TC‒mPEG‒PLGA micelle (TC‒mPEG‒PLGA/AS), which was formed spontaneously in aqueous solution.…”

Section: Resultsmentioning

confidence: 99%

Tetracycline-grafted mPEG-PLGA micelles for bone-targeting and osteoporotic improvement

et al. 2022

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Aim: We aimed to create a nano drug delivery system with tetracycline (TC)-grafted methoxy poly-(ethylene-glycol)‒poly-(D, L-lactic-co-glycolic acid) (mPEG‒PLGA) micelles (TC‒mPEG‒PLGA) with TC and mPEG‒PLGA for potential bone targeting. Prospectively, TC‒mPEG‒PLGA aims to deliver bioactive compounds, such as astragaloside IV (AS), for osteoporotic therapy.Methods: Preparation and evaluation of TC‒mPEG‒PLGA were accomplished via nano-properties, cytotoxicity, uptake by MC3T3-E1 cells, ability of hydroxyapatite targeting and potential bone targeting in vivo, as well as pharmacodynamics in a rat model.Results: The measured particle size of AS-loaded TC‒mPEG‒PLGA micelles was an average of 52.16 ± 2.44 nm, which exhibited a sustained release effect compared to that by free AS. The TC‒mPEG‒PLGA demonstrated low cytotoxicity and was easily taken by MC3T3-E1 cells. Through assaying of bone targeting in vitro and in vivo, we observed that TC‒mPEG‒PLGA could effectively increase AS accumulation in bone. A pharmacodynamics study in mice suggested potentially increased bone mineral density by AS-loaded TC‒mPEG‒PLGA in ovariectomized rats compared to that by free AS.Conclusion: The nano drug delivery system (TC‒mPEG‒PLGA) could target bone in vitro and in vivo, wherein it may be used as a novel delivery method for the enhancement of therapeutic effects of drugs with osteoporotic activity.

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Section: Resultsmentioning

confidence: 99%

Tetracycline-grafted mPEG-PLGA micelles for bone-targeting and osteoporotic improvement

et al. 2022

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“…Table summarizes all the results. Since m - THPP is a water-insoluble drug, it was believed that the more hydrophobic part leads to the higher loading capacity for the nanoparticles . However, too high content of P(NADA) in P(Glu 70 - b -NADA 90 ) defeated the hydrophobic-hydrophilic balance, resulting in instability and consequently the low solubilizing effect of m - THPP .…”

Section: Resultsmentioning

confidence: 99%

“…Since m - THPP is a water-insoluble drug, it was believed that the more hydrophobic part leads to the higher loading capacity for the nanoparticles . However, too high content of P(NADA) in P(Glu 70 - b -NADA 90 ) defeated the hydrophobic-hydrophilic balance, resulting in instability and consequently the low solubilizing effect of m - THPP . Therefore, the loading capacity of P(Glu 55 - b -NADA 20 ), with 27% hydrophobic content, was higher than that of P(Glu 70 - b -NADA 90 ) with almost double the hydrophobic content, 60%.…”

Section: Resultsmentioning

confidence: 99%

“…46 However, too high content of P(NADA) in P(Glu 70 -b-NADA 90 ) defeated the hydrophobichydrophilic balance, resulting in instability and consequently the low solubilizing effect of m-THPP. 46 Therefore, the loading capacity of P(Glu 55 -b-NADA 20 ), with 27% hydrophobic content, was higher than that of P(Glu 70 -b-NADA 90 ) with almost double the hydrophobic content, 60%. Therefore, P(Glu 55 -b-NADA 20 ) with moderate hydrophobic content, 27%, and consequently the highest loading capacity was chosen as the best candidate for the further investigations in this study.…”

Section: ■ Results and Discussionmentioning

confidence: 99%

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Amphiphilic Co-polypeptides Self-Assembled into Spherical Nanoparticles for Dermal Drug Delivery

Ahmadi

Zabihi

Rancan

et al. 2021

ACS Appl. Nano Mater.

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Poly(l-glutamic acid)-b-poly(N γ-acetyl-l-2,4-diaminobutyric acid), P(Glu-b-NADA), amphiphilic block-co-polypeptides with different hydrophobic/hydrophilic ratios were synthesized as drug carriers for dermal delivery. The block-co-polypeptides were prepared using ring-opening polymerization (ROP) of γ-benzyl l-glutamate N-carboxyanhydride and polycondensation of the activated urethane derivative of N γ-acetyl-l-2,4-diaminobutyric acid. Structures and conjugations of two blocks were successfully confirmed by 1H NMR, FTIR, DOSY NMR, GPC, and TGA. The nanocarriers were loaded with 5,10,15,20-tetrakis(3-hydroxyphenyl)porphyrin (m-THPP), a close congener of the approved photosensitizer 5,10,15,20-tetrakis(3-hydroxyphenyl)chlorin (m-THPC, temoporfin), and the loading capacity was found to be dependent on the composition of the block-co-polypeptides. Among the synthesized polymers, P(Glu55-b-NADA20) with moderate hydrophobic content showed the highest drug loading capacity of 4 wt % and self-aggregated into spherical nanoparticles with a size of 180–200 nm, which was confirmed by TEM and DLS. In an in vitro drug release study, P(Glu55-b-NADA20) could release m-THPP in a controllable manner. Furthermore, the synthesized polymer P(Glu55-b-NADA20) did not show high toxicity against HaCaT and HeLa cells up to 1000 and 500 μg mL–1, respectively, in an in vitro cell viability assay. Finally, it was shown in an ex vivo skin penetration study that the ionic amphiphilic block co-polypeptide enhanced the m-THPP penetration into human skin compared to base cream up to a factor of 12. m-THPP was released from P(Glu55-b-NADA20) to the viable epidermis while the polymer was deposited in the skin’s stratum corneum. Taking advantage of its excellent biodegradability, the low cytotoxcity, and efficient skin penetration, the synthesized block-co-polypeptide has the potential for future topical delivery systems.

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“…In the past decades, nanotechnology has been well developed to construct drug delivery systems, including but not limited to micelles, liposomes, and nanoparticles [1][2][3][4][5][6][7][8][9][10]. Compared with conventional formulations, these nanoscaled drug delivery systems (DDS) exhibit great potential in improving drug stability, preventing premature drug release, altering drug distribution, and prolonging the half-life of drugs [11].…”

Section: Introductionmentioning

confidence: 99%

Poly(Ethylene Glycol) Crosslinked Multi-Armed Poly(l-Lysine) with Encapsulating Capacity and Antimicrobial Activity for the Potential Treatment of Infection-Involved Multifactorial Diseases

et al. 2020

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With the development of modern medical technology, common diseases usually can be treated by traditional medicines and their formulation, while diseases with multiple etiologies still remain a great challenge in clinic. Nanoformulation was widely explored to address this problem. However, due to limited drug loading space of nanocarriers, co-delivery strategy usually fails to achieve sufficient loading of multiple drugs simultaneously. In this research, we explored the potential of poly(ethylene glycol) (PEG) crosslinked alternating copolymers MPLL-alt-PEG as both an anionic drug carrier and antimicrobial agent. The high cationic charge density of multi-armed poly(l-lysine) (MPLL) segments in MPLL-alt-PEG could endow the electrostatic encapsulation of anionic model drugs through the formation of polyion complex micelles with a MPLL/drug complex core and crosslinked PEG outer shell, enabling pH-sensitive drug release. Meanwhile, the MPLL-alt-PEG copolymer exhibits a broad spectrum of antimicrobial activities against various clinically relevant microorganisms with low hemolytic activity. Studies on antibacterial mechanism revealed that MPLL-alt-PEG attacked bacteria through the membrane disruption mechanism which is similar to that of typical antimicrobial peptides. Taken together, the present study shed light on the possibility of endowing a polymeric carrier with therapeutic effect and thus offered a promising strategy for achieving a comprehensive treatment of bacterial infection-involved multifactorial diseases.

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

Cited by 9 publications

References 30 publications

Tetracycline-grafted mPEG-PLGA micelles for bone-targeting and osteoporotic improvement

Tetracycline-grafted mPEG-PLGA micelles for bone-targeting and osteoporotic improvement

Amphiphilic Co-polypeptides Self-Assembled into Spherical Nanoparticles for Dermal Drug Delivery

Poly(Ethylene Glycol) Crosslinked Multi-Armed Poly(l-Lysine) with Encapsulating Capacity and Antimicrobial Activity for the Potential Treatment of Infection-Involved Multifactorial Diseases

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