Phospholipid-based solid drug formulations for oral bioavailability enhancement: A meta-analysis

Area of Science:

• Pharmaceutics and Drug Delivery Systems
• Biopharmaceutics
• Materials Science

Background:

• Low oral bioavailability poses a significant challenge in developing effective drug dosage forms.
• Solid phospholipid (PL) formulations, also known as proliposomes, offer a promising strategy to improve drug absorption.
• These formulations form multilamellar liposomes upon hydration, enhancing drug solubility and permeability.

Purpose of the Study:

• To systematically analyze and quantitatively assess the efficacy of solid PL formulations in enhancing oral bioavailability.
• To provide an overview of research progress and the potential of proliposomes for oral drug delivery.
• To identify correlations between drug properties and formulation effectiveness.

Main Methods:

• Systematic literature search of Medline, Embase, and SciFinder databases (1985-March 2015).
• Identification and summarization of 54 studies utilizing solid PL formulations for bioavailability enhancement of 43 drugs.
• Meta-analysis of in vitro and animal study data to quantify improvements in solubility, permeability, and oral bioavailability.

Main Results:

• Solid PL formulations significantly enhanced drug solubility (127.4%), permeability (59.6%), and oral bioavailability (18.5%) on average.
• The review identified 112 research articles and 82 patents related to solid PL formulations for oral delivery.
• No clinical studies were identified, indicating a gap in clinical translation.

Conclusions:

• Solid phospholipid formulations represent a viable and effective approach for overcoming oral bioavailability challenges.
• The meta-analysis provides quantitative evidence supporting the use of proliposomes for poorly soluble and permeable drugs.
• Further research, including clinical trials, is warranted to fully realize the therapeutic potential of this drug delivery system.