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Literature review demonstrates the drug encapsulation and controlled-release capabilities of self-assembled ascorbic acid derivatives, highlighting their broad therapeutic versatility.
INTRODUCTION: The chemical instability and low liposolubility of ascorbic acid have driven the development of hydrophobic derivatives that not only enhance its stability but also enable the formation of self-assembled systems for controlled drug delivery. These systems have garnered increasing interest due to their potential to improve drug administration by enhancing solubility, protecting against degradation, and enabling controlled or targeted release. AREAS COVERED: This review critically explores the development and application of self-assembled systems derived from ascorbic acid compounds, including micelles, microemulsions, aspasomes, and other nanostructures. A comprehensive literature search was conducted across PubMed, Scopus, and ScienceDirect databases, covering publications from January 2000 to February 2025. The discussion focuses on the physicochemical characteristics, biological behavior, and relevance of these systems in the delivery of both hydrophilic and hydrophobic drugs. EXPERT OPINION: Self-assembled drug delivery systems based on hydrophobic ascorbic acid derivatives represent a promising strategy in the field of pharmaceutical development. These platforms combine biocompatibility with functional versatility, offering enhanced membrane permeability, reduced systemic toxicity, and the potential for sustained or targeted drug release. Their suitability for oral, ophthalmic, and parenteral administration further highlights their applicability across a range of therapeutic areas, including immunological, anti-inflammatory, anti-infective, and oncological treatments.
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Brignone et al. (2025) studied this question.
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