Fundamental Aspects of Lipid-Based Excipients in Lipid-Based Product Development

Deepa Nakmode; Valamla Bhavana; Pradip Thakor; Jitender Madan; Pankaj Kumar Singh; Shashi Bala Singh; Jessica M. Rosenholm; Kuldeep K. Bansal; Neelesh Kumar Mehra

doi:10.3390/pharmaceutics14040831

Fundamental Aspects of Lipid-Based Excipients in Lipid-Based Product Development

Deepa Nakmode, Valamla Bhavana, Pradip Thakor, Jitender Madan, Pankaj Kumar Singh, Shashi Bala Singh, Jessica M. Rosenholm, Kuldeep K. Bansal, Neelesh Kumar Mehra

Research output: Contribution to journal › Review Article or Literature Review › peer-review

23 Citations (Scopus)

154 Downloads (Pure)

Abstract

Poor aqueous solubility of drugs is still a foremost challenge in pharmaceutical product development. The use of lipids in designing formulations provides an opportunity to enhance the aqueous solubility and consequently bioavailability of drugs. Pre-dissolution of drugs in lipids, surfactants, or mixtures of lipid excipients and surfactants eliminate the dissolution/dissolving step, which is likely to be the rate-limiting factor for oral absorption of poorly water-soluble drugs. In this review, we exhaustively summarize the lipids excipients in relation to their classification, absorption mechanisms, and lipid-based product development. Methodologies utilized for the preparation of solid and semi-solid lipid formulations, applications, phase behaviour, and regulatory perspective of lipid excipients are discussed.

Original language	English
Article number	831
Number of pages	28
Journal	Pharmaceutics
Volume	14
Issue number	4
DOIs	https://doi.org/10.3390/pharmaceutics14040831
Publication status	Published - 11 Apr 2022
MoE publication type	A2 Review article in a scientific journal

Keywords

Lipid based drug delivery systems
bioavailability
Poorly soluble drugs
oral drug administration
computational modeling
lipid excipients
oral absorption
lipid-based nanosystems
Poorly water-soluble drugs

UN SDGs

This output contributes to the following UN Sustainable Development Goals (SDGs)

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10.3390/pharmaceutics14040831Licence: CC BY

pharmaceutics-14-00831Final published version, 0.99 MBLicence: CC BY

Jasmine PRO: A versatile platform for drug delivery
Rosenholm, J., Wilen, C., Soidinsalo, S., Bansal, K. & Monaco, E.
Business Finland
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abstract = "Poor aqueous solubility of drugs is still a foremost challenge in pharmaceutical product development. The use of lipids in designing formulations provides an opportunity to enhance the aqueous solubility and consequently bioavailability of drugs. Pre-dissolution of drugs in lipids, surfactants, or mixtures of lipid excipients and surfactants eliminate the dissolution/dissolving step, which is likely to be the rate-limiting factor for oral absorption of poorly water-soluble drugs. In this review, we exhaustively summarize the lipids excipients in relation to their classification, absorption mechanisms, and lipid-based product development. Methodologies utilized for the preparation of solid and semi-solid lipid formulations, applications, phase behaviour, and regulatory perspective of lipid excipients are discussed.",

keywords = "Lipid based drug delivery systems, bioavailability, Poorly soluble drugs, oral drug administration, computational modeling, lipid excipients, oral absorption, lipid-based nanosystems, Poorly water-soluble drugs",

author = "Deepa Nakmode and Valamla Bhavana and Pradip Thakor and Jitender Madan and Singh, {Pankaj Kumar} and Singh, {Shashi Bala} and Rosenholm, {Jessica M.} and Bansal, {Kuldeep K.} and Mehra, {Neelesh Kumar}",

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TY - JOUR

T1 - Fundamental Aspects of Lipid-Based Excipients in Lipid-Based Product Development

AU - Nakmode, Deepa

AU - Bhavana, Valamla

AU - Thakor, Pradip

AU - Madan, Jitender

AU - Singh, Pankaj Kumar

AU - Singh, Shashi Bala

AU - Rosenholm, Jessica M.

AU - Bansal, Kuldeep K.

AU - Mehra, Neelesh Kumar

PY - 2022/4/11

Y1 - 2022/4/11

N2 - Poor aqueous solubility of drugs is still a foremost challenge in pharmaceutical product development. The use of lipids in designing formulations provides an opportunity to enhance the aqueous solubility and consequently bioavailability of drugs. Pre-dissolution of drugs in lipids, surfactants, or mixtures of lipid excipients and surfactants eliminate the dissolution/dissolving step, which is likely to be the rate-limiting factor for oral absorption of poorly water-soluble drugs. In this review, we exhaustively summarize the lipids excipients in relation to their classification, absorption mechanisms, and lipid-based product development. Methodologies utilized for the preparation of solid and semi-solid lipid formulations, applications, phase behaviour, and regulatory perspective of lipid excipients are discussed.

AB - Poor aqueous solubility of drugs is still a foremost challenge in pharmaceutical product development. The use of lipids in designing formulations provides an opportunity to enhance the aqueous solubility and consequently bioavailability of drugs. Pre-dissolution of drugs in lipids, surfactants, or mixtures of lipid excipients and surfactants eliminate the dissolution/dissolving step, which is likely to be the rate-limiting factor for oral absorption of poorly water-soluble drugs. In this review, we exhaustively summarize the lipids excipients in relation to their classification, absorption mechanisms, and lipid-based product development. Methodologies utilized for the preparation of solid and semi-solid lipid formulations, applications, phase behaviour, and regulatory perspective of lipid excipients are discussed.

KW - Lipid based drug delivery systems

KW - bioavailability

KW - Poorly soluble drugs

KW - oral drug administration

KW - computational modeling

KW - lipid excipients

KW - oral absorption

KW - lipid-based nanosystems

KW - Poorly water-soluble drugs

U2 - 10.3390/pharmaceutics14040831

DO - 10.3390/pharmaceutics14040831

M3 - Review Article or Literature Review

SN - 1999-4923

VL - 14

JO - Pharmaceutics

JF - Pharmaceutics

IS - 4

M1 - 831

ER -

Fundamental Aspects of Lipid-Based Excipients in Lipid-Based Product Development

Abstract

Keywords

UN SDGs

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