Novel insights on the encapsulation mechanism of PLGA terminal groups on ropivacaine

Li, Xun; Yi, Wei; Wen, Kang; Han, Qingzhen; Ogino, Kenji; Ma, Guanghui

doi:10.1016/j.ejpb.2021.01.015

Cited by 28 publications

(12 citation statements)

References 21 publications

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“…The safety of PLGA has been recognized by the United States Food and Drug Administration(FDA) and the European Medicines Agency, and has now been officially included by the FDA as a pharmaceutical excipient (Han et al, 2016;Ruman et al, 2020;Stefani et al, 2020). The properties of PLGA can be changed by adjusting the monomer ratio (LA/GA), molecular weight (M W ), concentration, and terminal group, which will affect the encapsulation efficiency (EE%) and drug release kinetics of PLGA microspheres (Li et al, 2021). The polymer PLGA retains some properties of the two monomers, such as the rigidity, hydrophobicity, and slow degradation of LA and the extensibility, relatively less hydrophobicity, and faster degradation of GA (Essa et al, 2020).…”

Section: Plga As Biodegradable Microsphere Carrier Materialsmentioning

confidence: 99%

“…The properties of PLGA can be changed by adjusting the monomer ratio (LA/GA), molecular weight (M W ), concentration, and terminal group, which will affect the encapsulation efficiency (EE%) and drug release kinetics of PLGA microspheres (Li et al, 2021 ). The polymer PLGA retains some properties of the two monomers, such as the rigidity, hydrophobicity, and slow degradation of LA and the extensibility, relatively less hydrophobicity, and faster degradation of GA (Essa et al, 2020 ).…”

Section: Plga As Biodegradable Microsphere Carrier Materialsmentioning

confidence: 99%

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PLGA-based biodegradable microspheres in drug delivery: recent advances in research and application

Zhang²,

Sun³

et al. 2021

Drug Delivery

310

106

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Biodegradable microspheres have been widely used in the field of medicine due to their ability to deliver drug molecules of various properties through multiple pathways and their advantages of low dose and low side effects. Poly (lactic-co-glycolic acid) copolymer (PLGA) is one of the most widely used biodegradable material currently and has good biocompatibility. In application, PLGA with a specific monomer ratio (lactic acid and glycolic acid) can be selected according to the properties of drug molecules and the requirements of the drug release rate. PLGA-based biodegradable microspheres have been studied in the field of drug delivery, including the delivery of various anticancer drugs, protein or peptide drugs, bacterial or viral DNA, etc. This review describes the basic knowledge and current situation of PLGA biodegradable microspheres and discusses the selection of PLGA polymer materials. Then, the preparation methods of PLGA microspheres are introduced, including emulsification, microfluidic technology, electrospray, and spray drying. Finally, this review summarizes the application of PLGA microspheres in drug delivery and the treatment of pulmonary and ocularrelated diseases.

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Section: Plga As Biodegradable Microsphere Carrier Materialsmentioning

confidence: 99%

Section: Plga As Biodegradable Microsphere Carrier Materialsmentioning

confidence: 99%

PLGA-based biodegradable microspheres in drug delivery: recent advances in research and application

Zhang²,

Sun³

et al. 2021

Drug Delivery

310

106

View full text Add to dashboard Cite

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“…The model of subcutaneous infiltration anesthesia has been commonly used to evaluate the duration of LAs. [41][42][43] As shown in Figure 4A, all formulations achieved complete nociceptive blockade (score of 100%) within 15 minutes, which corresponded with the onset time of ropivacaine. 44 The score for 0.75% RH group rapidly decreased to 61% after 4 hours and reached 0 within 8 hours, which corresponded with the clinic fact that effective anesthesia caused by soluble RH can only last for several hours.…”

Section: Prolonged Nociceptive Blockade Effectsmentioning

confidence: 71%

Interaction Between Ropivacaine and a Self-Assembling Peptide: A Nanoformulation for Long-Acting Analgesia

Peng¹,

Liu²,

Zhang³

et al. 2022

IJN

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Introduction Ropivacaine as a conventional local anesthetic has been used more and more frequently in the treatment of postoperative pain, but its analgesic effect can only last for several hours. In order to fulfill the clinic requirement for long-term analgesia, a long-acting ropivacaine nanocrystal formulation was fabricated through the interaction between ropivacaine and a self-assembling peptide. Methods Transmission electron microscopy, dynamic light scattering, circular dichroism and fluorescence spectrometry were used to examine the structural changes caused by the interaction between ropivacaine and the peptide. Scanning electron microscopy, dynamic light scattering, Fourier transform infrared spectrometry, X-ray diffraction and optical microscopy were used to characterize the ropivacaine-peptide nanocrystal. In vitro drug release and pharmacokinetics study were conducted to evaluate the slow-release profile of the nanocrystal formulation. A rodent cutaneous trunci muscle reflex model was used to evaluate the nociceptive blockade effects, and histological analysis was used to evaluate the local toxicity. A rodent plantar incisional pain model was used to evaluate the analgesic effect. Results Soluble ropivacaine monomers interacted with the Q11 peptide through π-π stacking and remolded its self-assembling structure, leading to the formation of drug/peptide nanoparticles which could be mineralized to form drug/peptide nanocrystals by adjusting the pH. Under physiological condition, the nanocrystals could release free ropivacaine slowly. As evaluated in rodent models, the anesthetic and analgesic effects of this formulation were significantly extended without causing toxicity. Conclusion Based on the interaction between ropivacaine and Q11, a controllable biomineralization process could be induced to obtain homogeneous nanocrystals, which could be used as an injectable long-acting analgesic formulation. This crystallization strategy utilizing the peptide-drug interaction also provided a promising pathway to fabricate long-acting formulations for many other small molecular drugs.

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“…The PEG2000-DSPE/ PLGA1:1 group showed higher mucus permeability, lower macrophage uptake and a longer lung retention time than the 0.25:1 group. PLGA has free end groups that can be modified into hydroxyl end groups (PLGA-OH), carboxyl end groups (PLGA-COOH) or ester end groups (PLGA-COOR); the encapsulation efficiency and sustained drug release characteristics of PLGA derivatives change with the presence of different modified end groups [51].…”

Section: Poly(lactide-co-glycolide) and Its Derivativesmentioning

confidence: 99%

Advances in therapeutic nanodrug delivery systems for infectious lung diseases: a review

Sheng

Tian

Duan

et al. 2022

Acta Materia Medica

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Infectious lung diseases are inflammatory diseases of the lungs caused by infectious agents such as bacteria, viruses or fungi. Oral or intravenous administration of antibiotics is the most common method of treatment, but some drugs have poor release stability, high systemic toxicity and susceptibility to drug resistance. Nanodrug delivery systems are promising alternatives for the treatment of infectious lung diseases, because they provide the advantages of enhancing the stability and solubility of delivered drugs, increasing pulmonary accumulation, decreasing systemic toxicity and ameliorating drug resistance. This review provides a brief overview of recent advances in approaches and ideas in pulmonary drug delivery methods. We believe that nano-based therapeutic strategies offer great potential to broaden the scope of treatment of infectious lung diseases and enhance therapeutic efficacy.

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Novel insights on the encapsulation mechanism of PLGA terminal groups on ropivacaine

Cited by 28 publications

References 21 publications

PLGA-based biodegradable microspheres in drug delivery: recent advances in research and application

PLGA-based biodegradable microspheres in drug delivery: recent advances in research and application

Interaction Between Ropivacaine and a Self-Assembling Peptide: A Nanoformulation for Long-Acting Analgesia

Advances in therapeutic nanodrug delivery systems for infectious lung diseases: a review

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