pH Modulation as a Key Strategy for Developing a Stable Lyotropic Liquid Crystal Formulation of Octreotide Acetate
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Le résumé fourni par la source
Background: Lyotropic liquid crystal (LLC) systems provide sustained release and convenient administration for peptide delivery. Octreotide, a first-line somatostatin analogue, has previously been formulated into LLC systems mainly using the hydrochloride salt. Here, we investigated the acetate salt, which is widely used in marketed products, but presents unique challenges in LLC formulation due to poor stability. Methods: We demonstrate that pH adjustment is a critical determinant for successfully incorporating octreotide acetate into a stable LLC system. By employing 3M HCl–EtOH to adjust pH to approximately 5.7, we obtained a formulation that maintained >90% drug content after 3 months at 40 °C and >98% after 12 months at 4 °C. Results: Structural analyses confirmed the coexistence of cubic and hexagonal mesophases, supporting controlled release. In vivo pharmacokinetic studies in rats further demonstrated sustained-release behavior, as evidenced by prolonged systemic exposure and an extended half-life. Pharmacokinetic profiles were comparable to those of an octreotide hydrochloride LLC. Conclusions: These findings highlight pH modulation as an essential strategy for stabilizing octreotide acetate in LLC systems, providing a foundation for extending LLC technology to clinically relevant salt forms of peptide therapeutics.
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Le contrôle bibliographique ouvert
DOI retrouvé dans Crossref DOI retrouvé ; titre concordant.
- Titre Crossref
- pH Modulation as a Key Strategy for Developing a Stable Lyotropic Liquid Crystal Formulation of Octreotide Acetate
- Date Crossref
- 13/02/2026
- Éditeur
- MDPI AG
- Type
- journal-article
Ce recoupement confirme des métadonnées liées au DOI. Il ne confirme ni la méthode ni les conclusions de l’étude, et il ne compte pas comme une seconde source scientifique indépendante.
Où se fait cette recherche
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Hebei Medical University pays non établi dans la noticeUniversité ou école supérieure
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Shijiazhuang Yiling Pharmaceutical (China) pays non établi dans la noticeEntreprise
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School of Pharmacy pays non établi dans la noticeUniversité ou école supérieure
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Ltd. CSPC Pharmaceutical Group Co. pays non établi dans la noticeEntreprise
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Hebei Key Laboratory of Innovative Drug Research and Evaluation pays non établi dans la noticeStructure de recherche
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State Key Laboratory of New Pharmaceutical Preparations and Excipients pays non établi dans la noticeStructure de recherche
Hebei Medical University, Shijiazhuang Yiling Pharmaceutical (China) et School of Pharmacy, avec 3 autres affiliations.
Une affiliation ne permet pas de déduire la nationalité d’un auteur.