Characterising lipid lipolysis and its implication in lipid-based formulation development
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Characterising lipid lipolysis and its implication in lipid-based formulation development. / Thomas, Nicky; Holm, Rene; Rades, Thomas; Müllertz, Anette.
In: The AAPS journal, Vol. 14, No. 4, 2012, p. 860-71.Research output: Contribution to journal › Journal article › Research › peer-review
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TY - JOUR
T1 - Characterising lipid lipolysis and its implication in lipid-based formulation development
AU - Thomas, Nicky
AU - Holm, Rene
AU - Rades, Thomas
AU - Müllertz, Anette
PY - 2012
Y1 - 2012
N2 - Facing the increasing number of poorly water-soluble drugs, pharmaceutical scientists are required to break new grounds for the delivery of these pharmaceutically problematic drugs. Lipid-based drug delivery systems (LBDDS) have received increased interest as a novel drug delivery platform during the last decades and several successfully marketed products have shown the potential for LBDDS. However, there exists a discrepancy between the clear need for innovative delivery forms and their rational design. In the case of LBDDS, this can be attributed to the complexity of LBDDS after administration. Unlike conventional formulations, LBDDS are susceptible to digestion in the gastrointestinal tract, the interplay of delivery system, drug and physiology ultimately effecting drug disposition. In vitro lipolysis has become an important technique to mimic the enzymatic degradation. For the better understanding of how LBDDS promote drug delivery, in vitro lipolysis requires advanced characterisation methods. In this review, the physiological background of lipid digestion is followed by a thorough summary of the techniques that are currently used to characterise in vitro lipolysis. It would be desirable that the increasing knowledge about LBDDS will foster their rationale development thereby increasing their broader application.
AB - Facing the increasing number of poorly water-soluble drugs, pharmaceutical scientists are required to break new grounds for the delivery of these pharmaceutically problematic drugs. Lipid-based drug delivery systems (LBDDS) have received increased interest as a novel drug delivery platform during the last decades and several successfully marketed products have shown the potential for LBDDS. However, there exists a discrepancy between the clear need for innovative delivery forms and their rational design. In the case of LBDDS, this can be attributed to the complexity of LBDDS after administration. Unlike conventional formulations, LBDDS are susceptible to digestion in the gastrointestinal tract, the interplay of delivery system, drug and physiology ultimately effecting drug disposition. In vitro lipolysis has become an important technique to mimic the enzymatic degradation. For the better understanding of how LBDDS promote drug delivery, in vitro lipolysis requires advanced characterisation methods. In this review, the physiological background of lipid digestion is followed by a thorough summary of the techniques that are currently used to characterise in vitro lipolysis. It would be desirable that the increasing knowledge about LBDDS will foster their rationale development thereby increasing their broader application.
U2 - 10.1208/s12248-012-9398-6
DO - 10.1208/s12248-012-9398-6
M3 - Journal article
C2 - 22956477
VL - 14
SP - 860
EP - 871
JO - A A P S Journal
JF - A A P S Journal
SN - 1550-7416
IS - 4
ER -
ID: 41889985