Polystyrene Sulfonate Resin as an Ophthalmic Carrier for Enhanced Bioavailability of Ligustrazine Phosphate Controlled Release System.
J Pharm Sci
; 113(9): 2786-2794, 2024 Sep.
Article
em En
| MEDLINE
| ID: mdl-38986870
ABSTRACT
Topical ocular sustained-release drug delivery systems represent an effective strategy for the treatment of ocular diseases, for which a suitable carrier has yet to be sufficiently developed. Herein, an eye-compatible sodium polystyrene sulfonate resin (SPSR) was synthesized with a uniform particle size of about 3 µm. Ligustrazine phosphate (LP) was adsorbed to SPSR by cation exchange to form LP@SPSR. LP@SPSR suspension eye drops were further developed using the combination of Carbopol 934P and xanthan gum as suspending agents. The LP@SPSR suspension showed a sustained release in vitro, which was consistent with the observed porcine corneal penetration ex vivo. Pharmacokinetics in tear fluid of rabits indicated that LP@SPSR suspension led to prolonged ocular retention of LP and a 2-fold improved the area under the drug concentration-time curve (AUC0-t). Pharmacokinetics in the aqueous humor of rabbits showed 2.8-fold enhancement in the AUC0-t compared to LP solution. The LP@SPSR suspension exhibited no cytotoxicity to human corneal epithelial cells, nor irritation was observed in rabbit eyes. Thus, the LP@SPSR suspension has been validated as a safe and sustained release system leading to enhanced ophthalmic bioavailability for treating ocular diseases.
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Base de dados:
MEDLINE
Assunto principal:
Poliestirenos
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Pirazinas
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Portadores de Fármacos
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Disponibilidade Biológica
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Preparações de Ação Retardada
Limite:
Animals
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Humans
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Male
Idioma:
En
Revista:
J Pharm Sci
Ano de publicação:
2024
Tipo de documento:
Article
País de afiliação:
China