In vitro and in vivo correlation for lipid-based formulations: Current status and future perspectives

Autor: Zhongjian Chen, Yi Lu, Yanping Huang, Quangang Zhu, Wei Wu, Qin Yu
Rok vydání: 2021
Předmět:
LBF
lipid-based formulation

Computer science
Review
AUC
area under the curve

SLS
sodium lauryl sulfate

0302 clinical medicine
IVIVC
SIF
simulated intestinal fluid

SCT
short-chain triglyceride

General Pharmacology
Toxicology and Pharmaceutics

SEDDS
self-emulsifying drug delivery system

In silico prediction
0303 health sciences
FDA
US Food and Drug Administration

DDS
drug delivery system

GI
gastrointestinal

SMEDDS
self-microemulsifying drug delivery system

In vitro and in vivo correlations
CETP
cholesterol ester transfer protein

Oral delivery
030220 oncology & carcinogenesis
LCT
long-chain triglyceride

Perspectives
HLB
hydrophilic–lipophilic balance

Lipolysis
MCT
medium-chain triglyceride

RM1-950
Computational biology
PK
pharmacokinetic

Absorption
Gastrointestinal digestion
03 medical and health sciences
In vivo
PBPK
physiologically based pharmacokinetic

SGF
simulated gastric fluid

TIM
TNO gastrointestinal model

030304 developmental biology
BCS
biopharmaceutics classification system

IVIVC
in vitro and in vivo correlation

SNEDDS
self-nanoemulsifying drug delivery system

ANN
artificial neural network

TNO
Netherlands Organization for Applied Scientific Research

IVIVR
in vitro and in vivo relationship

Therapeutics. Pharmacology
Cmax
peak plasma concentration

BE
bioequivalence

Oral retinoid
Tmax
time to reach the peak plasma concentration

Lipid-based formulation
Model
Zdroj: Acta Pharmaceutica Sinica B, Vol 11, Iss 8, Pp 2469-2487 (2021)
Acta Pharmaceutica Sinica. B
ISSN: 2211-3835
DOI: 10.1016/j.apsb.2021.03.025
Popis: Lipid-based formulations (LBFs) have demonstrated a great potential in enhancing the oral absorption of poorly water-soluble drugs. However, construction of in vitro and in vivo correlations (IVIVCs) for LBFs is quite challenging, owing to a complex in vivo processing of these formulations. In this paper, we start with a brief introduction on the gastrointestinal digestion of lipid/LBFs and its relation to enhanced oral drug absorption; based on the concept of IVIVCs, the current status of in vitro models to establish IVIVCs for LBFs is reviewed, while future perspectives in this field are discussed. In vitro tests, which facilitate the understanding and prediction of the in vivo performance of solid dosage forms, frequently fail to mimic the in vivo processing of LBFs, leading to inconsistent results. In vitro digestion models, which more closely simulate gastrointestinal physiology, are a more promising option. Despite some successes in IVIVC modeling, the accuracy and consistency of these models are yet to be validated, particularly for human data. A reliable IVIVC model can not only reduce the risk, time, and cost of formulation development but can also contribute to the formulation design and optimization, thus promoting the clinical translation of LBFs.
Graphical abstract In vitro and in vivo correlations (IVIVCs) are powerful tools for preparation development. Constructing IVIVCs for lipid-based formulations is rather challenging. This article reviews the current status and future perspectives in this field.Image 1
Databáze: OpenAIRE