Separation and identification of acylated leuprorelin inside PLGA microspheres

Guo, Ningzi; Zhang, Qi; Sun, Yue; Hua-xin, Yang

doi:10.1016/j.ijpharm.2019.01.061

Cited by 10 publications

(6 citation statements)

References 28 publications

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“…It is difficult to achieve efficient bioavailability with the pulmonary delivery of macromolecules because of local toxicity, immunogenicity, large size of macromolecules, humidity, mucociliary clearance, presence of hydrolytic enzymes, and macrophage clearance (Agrahari et al 2016). Furthermore, the stability issue of peptides incorporated into PLGA MPs needs to be considered because several peptide drugs such as calcitonin, octreotide, goserelin, and leuprolide are acylated by their interaction with PLGA structures (Ahn et al 2011;Guo et al 2019;Na and DeLuca 2005;Na et al 2003Na et al , 2007Park et al 2007;Shirangi et al 2016).…”

Section: Protein and Peptide Deliverymentioning

confidence: 99%

Poly(lactic acid)/poly(lactic-co-glycolic acid) particulate carriers for pulmonary drug delivery

Emami

Yazdi

2019

J. Pharm. Investig.

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Background Pulmonary route is an attractive target for both systemic and local drug delivery, with the advantages of a large surface area, rich blood supply, and absence of first-pass metabolism. Numerous polymeric micro/nanoparticles have been designed and studied for controlled and targeted drug delivery to the lung. Area covered Among the natural and synthetic polymers for polymeric particles, poly(lactic acid) (PLA) and poly(lacticco-glycolic acid) (PLGA) have been widely used for the delivery of anti-cancer agents, anti-inflammatory drugs, vaccines, peptides, and proteins because of their highly biocompatible and biodegradable properties. This review focuses on the characteristics of PLA/PLGA particles as carriers of drugs for efficient delivery to the lung. Furthermore, the manufacturing techniques of the polymeric particles, and their applications for inhalation therapy were discussed. Expert opinion Compared to other carriers including liposomes, PLA/PLGA particles present a high structural integrity providing enhanced stability, higher drug loading, and prolonged drug release. Adequately designed and engineered polymeric particles can contribute to a desirable pulmonary drug delivery characterized by a sustained drug release, prolonged drug action, reduction in the therapeutic dose, and improved patient compliance.

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Section: Protein and Peptide Deliverymentioning

confidence: 99%

Poly(lactic acid)/poly(lactic-co-glycolic acid) particulate carriers for pulmonary drug delivery

Emami

Yazdi

2019

J. Pharm. Investig.

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“…Acylation of peptides incorporated into PLGA microparticles has been shown to account for a significant portion of the drug instability problem in drug release process of PLGA microparticles [ 122 , 123 , 124 , 125 , 126 , 127 , 128 , 129 ]. Nucleophilic groups of peptides, mainly the primary amines of the N-terminus or Lys residue, are the major targets for peptide acylation [ 36 , 124 , 130 ] ( Figure 6 ) and the peptide acylation can affect the release properties, biological activity, pharmacological effect, and toxicity of peptide drugs in PLGA microparticles [ 131 , 132 , 133 ].…”

Section: Stability Of Drugs In Plga Particulate Formulationsmentioning

confidence: 99%

“…Nucleophilic groups of peptides, mainly the primary amines of the N-terminus or Lys residue, are the major targets for peptide acylation [ 36 , 124 , 130 ] ( Figure 6 ) and the peptide acylation can affect the release properties, biological activity, pharmacological effect, and toxicity of peptide drugs in PLGA microparticles [ 131 , 132 , 133 ]. In addition to primary amines, arginine residue has also been identified as acylation site in goserelin and leuprolide having no primary amines [ 128 , 129 ]. Several strategies have been proposed and studied to prevent and minimize peptide acylation in PLGA formulations [ 134 , 135 , 136 , 137 , 138 , 139 , 140 , 141 , 142 , 143 , 144 , 145 ].…”

Section: Stability Of Drugs In Plga Particulate Formulationsmentioning

confidence: 99%

Recent Progress in Drug Release Testing Methods of Biopolymeric Particulate System

et al. 2021

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Biopolymeric microparticles have been widely used for long-term release formulations of short half-life chemicals or synthetic peptides. Characterization of the drug release from microparticles is important to ensure product quality and desired pharmacological effect. However, there is no official method for long-term release parenteral dosage forms. Much work has been done to develop methods for in vitro drug release testing, generally grouped into three major categories: sample and separate, dialysis membrane, and continuous flow (flow-through cell) methods. In vitro drug release testing also plays an important role in providing insight into the in vivo performance of a product. In vitro release test with in vivo relevance can reduce the cost of conducting in vivo studies and accelerate drug product development. Therefore, investigation of the in vitro–in vivo correlation (IVIVC) is increasingly becoming an essential part of particulate formulation development. This review summarizes the principles of the in vitro release testing methods of biopolymeric particulate system with the recent research articles and discusses their characteristics including IVIVC, accelerated release testing methods, and stability of encapsulated drugs.

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“…Biodegradable poly(lactide-co-glycolide) (PLGA) has become one of the most widely used biological scaffold materials (23)(24)(25)(26). Compared with other scaffold materials, PLGA possesses good biological properties (27)(28)(29).…”

Section: Introductionmentioning

confidence: 99%

Effects of Smad4 on the expression of caspase‑3 and Bcl‑2 in human gingival fibroblasts cultured on 3D PLGA scaffolds induced by compressive force

Zhao

Wang

et al. 2021

Int J Mol Med

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Human gingival fibroblasts (HGFs) are the main cells that comprise gingival tissue, where they transfer mechanical signals under physiological and pathological conditions. The exact mechanism underlying gingival tissue reconstruction under compressive forces remains unclear. The present study aimed to explore the effects of Smad4, caspase-3 and Bcl-2 on the proliferation of HGFs induced by compressive force. HGFs were cultured on poly(lactide-co-glycolide) (PLGA) scaffolds under an optimal compressive force of 25 g/cm 2 . Cell viability was determined via Cell Counting Kit-8 assays at 0, 12, 24, 48 and 72 h. The expression levels of Smad4, caspase-3 and Bcl-2 were measured via reverse transcription-quantitative PCR and western blotting. The application of compressive force on HGFs for 24 h resulted in a significant increase in cell proliferation and Bcl-2 expression, but a significant decrease in the expression of Smad4 and caspase-3; however, inverse trends were observed by 72 h. Subsequently, a lentivirus was used to overexpress Smad4 in HGFs, which attenuated the effects of compressive force on HGF proliferation and Bcl-2 expression, but enhanced caspase-3 expression, suggesting that Smad4 may regulate compressive force-induced apoptosis in HGFs. In conclusion, these findings increased understanding regarding the mechanisms of compressive force-induced HGF proliferation and apoptosis, which may provide further insight for improving the efficacy and stability of orthodontic treatment.

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Separation and identification of acylated leuprorelin inside PLGA microspheres

Cited by 10 publications

References 28 publications

Poly(lactic acid)/poly(lactic-co-glycolic acid) particulate carriers for pulmonary drug delivery

Poly(lactic acid)/poly(lactic-co-glycolic acid) particulate carriers for pulmonary drug delivery

Recent Progress in Drug Release Testing Methods of Biopolymeric Particulate System

Effects of Smad4 on the expression of caspase‑3 and Bcl‑2 in human gingival fibroblasts cultured on 3D PLGA scaffolds induced by compressive force

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