Title:Lipid Microparticles for Oral Bioavailability Enhancement
Volume: 5
Issue: 2
Author(s): Afzal Hussain, Abdus Samad, Mohd Usman Mohd Siddique and Sarwar Beg
Affiliation:
Keywords:
Bioavailability, drug delivery, lipid microparticles, poor soluble drugs.
Abstract: A variety of potent lipophilic drugs exhibits low oral bioavailability due to poor water solubility of
drugs. These drugs are challenging for the formulation scientists with regard to solubility and bioavailability
(BA). Extensive efforts are ongoing to enhance oral BA of these types of drugs to increase clinical efficacies.
The most common approach is the use of highly developed lipid-based drug delivery systems. This is a
strategy to incorporate drug into the safe and biodegradable lipids (natural, semi-synthetic, vegetable oils or
hydrolyzed solid lipids) with improved oral bioavailability. Lipid microparticles (LM) are efficient lipid based
drug delivery system which might be prudent attempt to increase the oral bioavailability of poor aqueous
soluble drugs. Lipid based systems are recognized as a potential approach for the improved oral absorption
which ultimately caused to enhanced BA. Wide variety and range of substances have been reported to be
entrapped into lipid microparticles including lipophilic and hydrophilic molecules as well as labile proteins
and peptides. Moreover, LM can protect drugs from in vitro and in vivo degradation. Several authors reported
numerous techniques and methods to enhance drug solubility by exploiting lipids while formulation
development. The use of LM is a novel carrier to enhance oral BA of poor aqueous soluble drug. Lipids are
well known to deliver a number of drugs with profound systemic availability either through portal vein or
lymphatic absorption from gastro-intestinal tract. These lipids are belonging to triglycerides (short chain,
medium chain and long chain) with or without double bond in their hydrocarbon chain length. The present
chapter discusses the physico-chemical properties, processing techniques necessary to obtain lipid-based
microparticles formulations for oral delivery along with a brief discussion of lipid excipients and their
characterization. The chapter provided related patents with valuable informations for pharmaceutical research
groups which would be very informative and instructive.
