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Bioavailability is a critical pharmacological concept that measures the extent and rate at which an active drug ingredient or therapeutic moiety enters the systemic circulation, remaining unchanged. It's a pivotal factor in determining a drug's efficacy and safety.The Biopharmaceutics Classification System (BCS) plays an essential role in drug development by categorizing drugs into four classes based on their solubility and permeability. This classification aids in understanding drug absorption...
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Methodological advances in liposomal encapsulation efficiency determination: systematic review and analysis.

Jin-Ping Wang1,2,3, Zi-Rui Huang1,2,3, Cheng Zhang1,2,3

  • 1Third-grade Pharmacological Laboratory on Traditional Chinese Medicine, State Administration of Traditional Chinese Medicine, China Three Gorges University, Yichang, China.

Journal of Drug Targeting
|March 24, 2025
PubMed
Summary

Accurately measuring liposomal drug encapsulation efficiency (EE) is crucial for formulation development. This review analyzes analytical methods for quantifying encapsulated and free drug concentrations, aiding in optimization and quality control.

Keywords:
Liposomesdrug deliveryencapsulation efficiencypharmaceutical compoundsseparation methods

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Area of Science:

  • Pharmaceutical Sciences
  • Drug Delivery Systems
  • Analytical Chemistry

Background:

  • Liposomes are versatile drug delivery vehicles with broad pharmaceutical applications.
  • Encapsulation efficiency (EE) is a critical quality attribute for liposomal formulations, directly impacting efficacy and safety.
  • Accurate EE determination requires quantifying total drug, encapsulated drug, and free drug concentrations, which is analytically challenging due to liposome complexity.

Purpose of the Study:

  • To provide a comprehensive review of analytical techniques for determining liposomal encapsulation efficiency (EE).
  • To analyze the methodological characteristics, applicable ranges, advantages, and limitations of various EE determination methods.
  • To propose detection strategies for EE assessment tailored to laboratory capabilities and compound properties.

Main Methods:

  • Review of analytical techniques including (reverse) dialysis, ultrafiltration centrifugation, differential centrifugation, and size exclusion chromatography.
  • Emphasis on the challenges posed by liposome physicochemical properties (flexibility, charge, composition) for direct drug fraction measurement.
  • Discussion of strategies for quantifying free and total drug concentrations to enable reliable EE evaluation.

Main Results:

  • Various analytical methods exist for EE determination, each with specific strengths and weaknesses.
  • Accurate quantification of free and total drug is essential for reliable EE assessment.
  • Liposome characteristics complicate direct measurement of encapsulated and free drug fractions.

Conclusions:

  • Precise EE determination is vital for guiding liposomal formulation optimization and ensuring manufacturing quality.
  • The choice of analytical technique should consider laboratory resources and the specific physicochemical properties of the drug and liposome.
  • This review offers guidance for selecting appropriate methods for robust encapsulation efficiency assessment.