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Self-Nanoemulsification of Healthy Oils to Enhance the Solubility of Lipophilic Drugs
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Liquid and Solid Self-Emulsifying Drug Delivery Systems (SEDDs) as Carriers for the Oral Delivery of Azithromycin:

Reem Abou Assi1,2, Ibrahim M Abdulbaqi1,2, Toh Seok Ming1

  • 1The Discipline of Pharmaceutical Technology, School of Pharmaceutical Sciences, Universiti Sains Malaysia, Penang 11800, Malaysia.

Pharmaceutics
|November 7, 2020
PubMed

Insights

This study developed novel liquid and solid self-emulsifying drug delivery systems (SEDDs) to enhance azithromycin (AZM) oral bioavailability. The optimized SEDDs demonstrated improved AZM release and stability, offering a promising approach for antibiotic delivery.

Area of Science:

  • Pharmaceutical Sciences
  • Drug Delivery Systems
  • Macrolide Antibiotics

Background:

  • Azithromycin (AZM) exhibits low oral bioavailability (37%) due to poor solubility and absorption.
  • Challenges include high molecular weight, low dissolution rate, and incomplete intestinal absorption.
  • Self-emulsifying drug delivery systems (SEDDs) offer a potential solution to improve AZM oral delivery.

Purpose of the Study:

  • To develop and optimize liquid (L) and solid (S) SEDDs for azithromycin (AZM).
  • To evaluate the physicochemical properties and in vitro performance of the developed AZM SEDDs.
  • To assess the potential of SEDDs to enhance the oral bioavailability of azithromycin.

Main Methods:

  • Construction of pseudo-ternary diagrams to identify optimal SEDDs excipient ratios.
  • Formulation and optimization of liquid and solid SEDDs based on droplet size, dispersity, and transmittance.
  • In vitro drug release studies in distilled water (DW), 0.1 mM HCl, and simulated intestinal fluids (SIF).
  • Cytocompatibility and tight junction modulation assessments.

Main Results:

  • Optimized liquid (L-F1(H)) and solid (S-F1(H)) SEDDs met all selection criteria (DS < 150 nm, Đ ≤ 0.7, T% > 85).
  • Both formulations were cytocompatible and demonstrated the ability to open cellular epithelial tight junctions.
  • Significantly enhanced azithromycin release was observed: >90% from L-SEDDs and 52.22% from S-SEDDs within 5 min in DW, compared to 11.27% for pure AZM.
  • Formulations exhibited stability under refrigerator storage conditions.

Conclusions:

  • Developed liquid and solid SEDDs effectively encapsulate azithromycin.
  • The optimized SEDDs significantly improve azithromycin dissolution rate compared to the pure drug.
  • These findings suggest that AZM-loaded SEDDs hold considerable promise for enhancing oral drug delivery and therapeutic efficacy.
Keywords:
Caco-2 cellMTT assaycytotoxicitydrug deliveryliquid SEDDsself-emulsifyingsolid SEDDsstabilitytight junctions

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