Poor absorption, short half-life and resistance development are some of the
major factors responsible for reduced drug efficacy. Lipophilic prodrugs can offer certain
advantages to overcome these challenges. Chemical derivatization of hydrophilic
agents with lipophilic pro-moieties can significantly elevate drug diffusion across absorptive
membranes. Moreover, the desired linkage (ester vs. amide) may be selected
to improve stability in vivo. Importantly, an appropriate selection of pro-moiety (targeting
ligand) may promote drug specificity and selectivity. In this review article, an
attempt has been made to summarize lipophilic prodrugs employed to improve delivery
and efficacy of a wide range of poorly permeable but highly potent therapeutic
agents. In addition, a brief overview on recent application of lipophilic prodrugs to
promote encapsulation of hydrophilic agents in nano-sized drug carriers has been provided.
Keywords: Absorption, formulation and delivery, lipophilic, lipids, linkages, prodrugs.
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