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核心技术专利:CN118964589B侵权必究
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Lipid Nanocapsule-Chitosan and Iota-Carrageenan Hydrogel Composite for Sustained Hydrophobic Drug Delivery.

作者信息

Mukubwa Grady K, Safari Justin B, Tetana Zikhona N, Jones Caroline N, Walker Roderick B, Krause Rui W M

机构信息

Rhodes University.

University of South Africa.

出版信息

Res Sq. 2025 Aug 20:rs.3.rs-7078136. doi: 10.21203/rs.3.rs-7078136/v1.


DOI:10.21203/rs.3.rs-7078136/v1
PMID:40894010
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC12393483/
Abstract

Hydrophobic drug delivery via oral or pulmonary routes presents significant challenges for clinical translation, particularly for poorly soluble antiviral drugs. Physiological barriers-such as enzymatic degradation, harsh pH, and rapid transit in the gastrointestinal tract, or mucociliary clearance and alveolar macrophage uptake in the lungs-can severely limit therapeutic efficacy. To address these challenges, we developed a novel lipid nanocapsule (LNC) and chitosan/iota-carrageenan hydrogel composite tailored for sustained delivery of hydrophobic antiviral agents. This composite system was designed to encapsulate and deliver Efavirenz (EFV) under simulated gastrointestinal conditions. EFV was first encapsulated in LNCs, which were subsequently embedded within a mucoadhesive hydrogel matrix to form the EFV-LNC hydrogel composite. The LNCs significantly enhanced EFV solubility compared to water alone (p < 0.0001), and droplet size was controlled (57.4 ± 0.5 nm). The hydrogel composite exhibited an optimized swelling ratio (~ 300 g water per 1 g hydrogel) and achieved an encapsulation efficiency of approximately 53%. Importantly, EFV release from the composite was significantly prolonged under various gastrointestinal pH conditions compared to the unformulated drug (p < 0.0001). Cytotoxicity assays confirmed the composite's cytocompatibility, supporting its potential safety for future mucosal administration. These findings suggest that the LNC-hydrogel composite enhances solubility, enables controlled release, and may improve mucosal retention, supporting its utility as a versatile platform for oral and pulmonary delivery of hydrophobic antiviral drugs.

摘要
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/19ee/12393483/ee95b3cd20ca/nihpp-rs7078136v1-f0008.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/19ee/12393483/855f23518f61/nihpp-rs7078136v1-f0001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/19ee/12393483/0d399ff86f09/nihpp-rs7078136v1-f0002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/19ee/12393483/92ec88ad158e/nihpp-rs7078136v1-f0003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/19ee/12393483/11589341012a/nihpp-rs7078136v1-f0005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/19ee/12393483/cb0db3e07b17/nihpp-rs7078136v1-f0006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/19ee/12393483/b64c5abbf226/nihpp-rs7078136v1-f0007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/19ee/12393483/ee95b3cd20ca/nihpp-rs7078136v1-f0008.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/19ee/12393483/855f23518f61/nihpp-rs7078136v1-f0001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/19ee/12393483/0d399ff86f09/nihpp-rs7078136v1-f0002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/19ee/12393483/92ec88ad158e/nihpp-rs7078136v1-f0003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/19ee/12393483/11589341012a/nihpp-rs7078136v1-f0005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/19ee/12393483/cb0db3e07b17/nihpp-rs7078136v1-f0006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/19ee/12393483/b64c5abbf226/nihpp-rs7078136v1-f0007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/19ee/12393483/ee95b3cd20ca/nihpp-rs7078136v1-f0008.jpg

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本文引用的文献

[1]
Lipid-based oral formulation in capsules to improve the delivery of poorly water-soluble drugs.

Front Drug Deliv. 2023-8-24

[2]
-Carrageenan/Chitosan Nanoparticles via Coacervation: Achieving Stability for Tiny Particles.

Nanomaterials (Basel). 2025-1-22

[3]
New Horizons in Antiretroviral Drug Delivery Systems for HIV Management.

Curr Med Chem. 2024-8-9

[4]
Lecithin and cardiovascular health: a comprehensive review.

Egypt Heart J. 2024-7-13

[5]
A Comprehensive Review of Hydrogel-Based Drug Delivery Systems: Classification, Properties, Recent Trends, and Applications.

AAPS PharmSciTech. 2024-3-21

[6]
pH stimuli-responsive hydrogels from non-cellulosic biopolymers for drug delivery.

Front Bioeng Biotechnol. 2023-9-12

[7]
Diffusion-Limited Processes in Hydrogels with Chosen Applications from Drug Delivery to Electronic Components.

Molecules. 2023-8-7

[8]
Polymer-Based Hydrogels Applied in Drug Delivery: An Overview.

Gels. 2023-6-27

[9]
Rheological Considerations of Pharmaceutical Formulations: Focus on Viscoelasticity.

Gels. 2023-6-7

[10]
Bioassay-Guided Isolation of Antiplasmodial Compounds from Lam. (Hypericaceae) and Their Cytotoxicity and Molecular Docking.

Biomed Res Int. 2023

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