Chapter 5
Catanionic Hybrid Lipid Nanovesicles for Improved
Bioavailability and Efficacy of Chemotherapeutic Drugs
Xuemei Xie, Dan He, Yan Wu, Tingting Wang, Cailing Zhong,
and Jingqing Zhang
Abstract
Catanionic nanovesicles are attractive as a novel class of delivery vehicle because they can increase the
stability, adsorption, and cellular uptake of a broad range of drugs. These hybrid lipid nanocarriers consist of
solid and liquid lipids, which are biocompatible and biodegradable. Since liquid lipid is added to the
nanocarrier, the lipids are present in a crystalline defect or amorphous structure state. As a result, hybrid
lipid nanocarriers have a higher drug loading capability and suffer less drug leakage during preparation and
storage compared to the pure lipid nanocarriers. Catanionic nanovesicles have been shown to increase
stability, adsorption, cellular uptake, apoptosis induction, tumor cell cytotoxicity, and antitumorigenic
effect, making it a highly desirable vehicle for drug delivery. For example, the anticancer compound
curcumin (CC) have shown great promise to cure cancers such as lung cancer, breast cancer, stomach
cancer, and colon cancer. However, like many potential antitumor drugs, CC on its own has poor water
solubility, easy photodegradation, chemical instability, low bioavailability, rapid metabolism, and fast
systematic clearance, which severely limits its clinical applications. In this chapter, we demonstrate the use
of catanionic nanovesicles to improve the bioavailability and efficacy of CC for anticancer applications. This
technique can be easily adapted for delivery and evaluation of other bioactive compounds.
Key words Catanionic nanovesicle, Hybrid lipid nanovesicle, Effective delivery, Bioavailability, Anticancer efficacy
1 Introduction
Lipid-based drug delivery systems enhance bioavailability of poorly
water-soluble drugs by facilitating dissolution, enhancing the
uptake and inhibiting the efflux transporters [1–3]. First-generation lipid carrier [4] were originally composed of pure solid lipids.
Due to the intact crystal structure of solid lipid, the drug loading
capacity of this type of nanoparticles is low, resulting in drug
leakage during storage and limiting its usefulness as a drug delivery
Kumaran Narayanan (ed.), Bio-Carrier Vectors: Methods and Protocols, Methods in Molecular Biology, vol. 2211,
https://doi.org/10.1007/978-1-0716-0943-9_5, © Springer Science+Business Media, LLC, part of Springer Nature 2021
Xuemei Xie and Dan He contributed equally to this work.
57
Catanionic Hybrid Lipid Nanovesicles for Improved
Bioavailability and Efficacy of Chemotherapeutic Drugs
Xuemei Xie, Dan He, Yan Wu, Tingting Wang, Cailing Zhong,
and Jingqing Zhang
Abstract
Catanionic nanovesicles are attractive as a novel class of delivery vehicle because they can increase the
stability, adsorption, and cellular uptake of a broad range of drugs. These hybrid lipid nanocarriers consist of
solid and liquid lipids, which are biocompatible and biodegradable. Since liquid lipid is added to the
nanocarrier, the lipids are present in a crystalline defect or amorphous structure state. As a result, hybrid
lipid nanocarriers have a higher drug loading capability and suffer less drug leakage during preparation and
storage compared to the pure lipid nanocarriers. Catanionic nanovesicles have been shown to increase
stability, adsorption, cellular uptake, apoptosis induction, tumor cell cytotoxicity, and antitumorigenic
effect, making it a highly desirable vehicle for drug delivery. For example, the anticancer compound
curcumin (CC) have shown great promise to cure cancers such as lung cancer, breast cancer, stomach
cancer, and colon cancer. However, like many potential antitumor drugs, CC on its own has poor water
solubility, easy photodegradation, chemical instability, low bioavailability, rapid metabolism, and fast
systematic clearance, which severely limits its clinical applications. In this chapter, we demonstrate the use
of catanionic nanovesicles to improve the bioavailability and efficacy of CC for anticancer applications. This
technique can be easily adapted for delivery and evaluation of other bioactive compounds.
Key words Catanionic nanovesicle, Hybrid lipid nanovesicle, Effective delivery, Bioavailability, Anticancer efficacy
1 Introduction
Lipid-based drug delivery systems enhance bioavailability of poorly
water-soluble drugs by facilitating dissolution, enhancing the
uptake and inhibiting the efflux transporters [1–3]. First-generation lipid carrier [4] were originally composed of pure solid lipids.
Due to the intact crystal structure of solid lipid, the drug loading
capacity of this type of nanoparticles is low, resulting in drug
leakage during storage and limiting its usefulness as a drug delivery
Kumaran Narayanan (ed.), Bio-Carrier Vectors: Methods and Protocols, Methods in Molecular Biology, vol. 2211,
https://doi.org/10.1007/978-1-0716-0943-9_5, © Springer Science+Business Media, LLC, part of Springer Nature 2021
Xuemei Xie and Dan He contributed equally to this work.
57