Academic Journal
Analysis of molecular weight of mixed poly (lactide-co-glycolide) in Risperidone microspheres based on separation method.
| Τίτλος: | Analysis of molecular weight of mixed poly (lactide-co-glycolide) in Risperidone microspheres based on separation method. |
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| Συγγραφείς: | Chen S; Collaborative Innovation Center of Advanced Drug Delivery System and Biotech Drugs in Universities of Shandong, Key Laboratory of Molecular Pharmacology and Drug Evaluation, Ministry of Education, School of Pharmacy, Yantai University, Yantai, PR China., Ma J; Collaborative Innovation Center of Advanced Drug Delivery System and Biotech Drugs in Universities of Shandong, Key Laboratory of Molecular Pharmacology and Drug Evaluation, Ministry of Education, School of Pharmacy, Yantai University, Yantai, PR China., Ma Y; Collaborative Innovation Center of Advanced Drug Delivery System and Biotech Drugs in Universities of Shandong, Key Laboratory of Molecular Pharmacology and Drug Evaluation, Ministry of Education, School of Pharmacy, Yantai University, Yantai, PR China., Hu J; Collaborative Innovation Center of Advanced Drug Delivery System and Biotech Drugs in Universities of Shandong, Key Laboratory of Molecular Pharmacology and Drug Evaluation, Ministry of Education, School of Pharmacy, Yantai University, Yantai, PR China., Liu J; Collaborative Innovation Center of Advanced Drug Delivery System and Biotech Drugs in Universities of Shandong, Key Laboratory of Molecular Pharmacology and Drug Evaluation, Ministry of Education, School of Pharmacy, Yantai University, Yantai, PR China., Zhu L; Collaborative Innovation Center of Advanced Drug Delivery System and Biotech Drugs in Universities of Shandong, Key Laboratory of Molecular Pharmacology and Drug Evaluation, Ministry of Education, School of Pharmacy, Yantai University, Yantai, PR China., Xia Y; State Key Laboratory of Long-Acting and Targeting Drug Delivery System, Shandong Luye Pharmaceutical Co., Ltd, Yantai, Shandong, PR China., Jiang H; State Key Laboratory of Long-Acting and Targeting Drug Delivery System, Shandong Luye Pharmaceutical Co., Ltd, Yantai, Shandong, PR China., Shen L; State Key Laboratory of Long-Acting and Targeting Drug Delivery System, Shandong Luye Pharmaceutical Co., Ltd, Yantai, Shandong, PR China., Xue Y; State Key Laboratory of Long-Acting and Targeting Drug Delivery System, Shandong Luye Pharmaceutical Co., Ltd, Yantai, Shandong, PR China., Liu W; Collaborative Innovation Center of Advanced Drug Delivery System and Biotech Drugs in Universities of Shandong, Key Laboratory of Molecular Pharmacology and Drug Evaluation, Ministry of Education, School of Pharmacy, Yantai University, Yantai, PR China. Electronic address: wanhui@luye.cn., Xu L; Collaborative Innovation Center of Advanced Drug Delivery System and Biotech Drugs in Universities of Shandong, Key Laboratory of Molecular Pharmacology and Drug Evaluation, Ministry of Education, School of Pharmacy, Yantai University, Yantai, PR China. Electronic address: xulixiao78@163.com. |
| Πηγή: | Journal of pharmaceutical sciences [J Pharm Sci] 2026 Sep; Vol. 115 (9), pp. 104414. Date of Electronic Publication: 2026 Jul 12. |
| Τύπος έκδοσης: | Journal Article |
| Γλώσσα: | English |
| Στοιχεία περιοδικού: | Publisher: Elsevier Country of Publication: United States NLM ID: 2985195R Publication Model: Print-Electronic Cited Medium: Internet ISSN: 1520-6017 (Electronic) Linking ISSN: 00223549 NLM ISO Abbreviation: J Pharm Sci Subsets: MEDLINE |
| Imprint Name(s): | Publication: 2016- : New York, NY : Elsevier Original Publication: Easton, Pa., American Pharmaceutical Assn. |
| Ιατρικοί όροι (MeSH): | Risperidone*/chemistry , Polyglycolic Acid*/chemistry , Polyglactin 910*/chemistry , Lactic Acid*/chemistry , Microspheres*, Solvents/chemistry ; Molecular Weight ; Polylactic Acid-Polyglycolic Acid Copolymer ; Solubility ; Chromatography, Gel |
| Περίληψη: | Poly(lactide-co-glycolide) polymers (PLGAs) are indispensable biodegradable matrices for long-acting parenteral (injectable) microsphere formulations. To modulate drug release kinetics and mitigate burst release in these complex injectable systems, PLGAs with varying lactide:glycolide (L:G) ratios are often employed in combination. While essential for ensuring batch-to-batch consistency and developing generic long-acting injectables, characterizing the individual properties of mixed PLGAs remains technically challenging. This study establishes a simple and accurate method to separate and characterize PLGA 7525 5A and PLGA 5050 2.5A within risperidone microspheres based on their solubility differences (semi-solvent principle). Trichloroethylene was identified as the optimal separation solvent, with n-propyl acetate serving as the washing solvent. The method was optimized by investigating parameters such as solvent volume, temperature, and mechanical assistance, with the addition of glass beads proving critical for effective separation. Molecular weight (Mw) analysis was performed using Gel Permeation Chromatography (GPC) on Agilent PLgel columns (connected in series) with tetrahydrofuran (THF) as the mobile phase. The method demonstrated excellent linearity (R2 = 0.9998) within the calibration range of 1220-554,000 g·mol⁻¹ (Polystyrene equivalent). Precision was high, with RSD values of 0.33% (n = 6) for the supernatant Mw and 2.1% (n = 6) for the sediment Mw. The method's discriminatory ability was validated using simulated single-polymer degradation and mixed degraded microspheres. In conclusion, this method enables independent quality control of individual PLGA components within complex injectable matrices, providing a vital analytical tool for the key characteristic evaluation and bioequivalence assessment of complex generic parenteral formulations. (Copyright © 2026 American Pharmacists Association®. Published by Elsevier Inc. All rights reserved.) |
| Competing Interests: | Declaration of competing interest The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper. |
| Contributed Indexing: | Keywords: Complex microspheres; Deformulation; L:G ratios; PLGA molecular weight; Separation method |
| Substance Nomenclature: | L6UH7ZF8HC (Risperidone) 1SIA8062RS (Polylactic Acid-Polyglycolic Acid Copolymer) 0 (Solvents) 26009-03-0 (Polyglycolic Acid) 34346-01-5 (Polyglactin 910) 33X04XA5AT (Lactic Acid) |
| Entry Date(s): | Date Created: 20260712 Date Completed: 20260922 Latest Revision: 20260922 |
| Update Code: | 20260923 |
| DOI: | 10.1016/j.xphs.2026.104414 |
| PMID: | 42437590 |
| Βάση Δεδομένων: | MEDLINE |
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