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Lipid Nanoparticles: Effect on Bioavailability and Pharmacokinetic Changes

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Book cover Drug Delivery

Part of the book series: Handbook of Experimental Pharmacology ((HEP,volume 197))

Abstract

The main aim of pharmaceutical technology research is the design of successful formulations for effective therapy, taking into account several issues including therapeutic requirements and patient compliance. In this regard, several achievements have been reported with colloidal carriers, in particular with lipid nanoparticles, due to their unique physicochemical properties. For several years these carriers have been showing potential success for several administration routes, namely oral, dermal, parenteral, and, more recently, for pulmonary and brain targeting. The present chapter provides a review of the use of solid lipid nanoparticles (SLN) and nanostructured lipid carriers (NLC) to modify the release profile and the pharmacokinetic parameters of active pharmaceutical ingredients (APIs) incorporated in these lipid matrices, aiming to modify the API bioavailability, either upwards or downwards depending on the therapeutic requirement. Definitions of the morphological characteristics, surface properties, and polymorphic structures will also be given, emphasizing their influence on the incorporation parameters of the API, such as yield of production, loading capacity, and encapsulation efficiency.

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Abbreviations

AFM:

Atomic force microscopy

API:

Active pharmaceutical ingredient

AUC:

Area under the curve

BBB:

Blood–brain barrier

BSC:

Biopharmaceutical classification system

CNS:

Central nervous system

DSC:

Differential scanning calorimetry

EE:

Encapsulation efficiency

ESR:

Electron spin resonance

FFF:

Field flow fractionation

GIT:

Gastrointestinal tract

HLB:

Hydrophilic–lipophilic balance

HPH:

High pressure homogenization

IES:

Inter-endothelial cell slits

LC:

Loading capacity

LD:

Laser diffractometry

LDL:

Low density lipoproteins

LHRH:

Luteinizing hormone releasing hormone

MPS:

Mononuclear phagocytic system

NLC:

Nanostructured lipid carriers

NMR:

Nuclear magnetic resonance

PCS:

Photon correlation spectroscopy

PEG:

Polyethylene glycol

RES:

Reticulo-endothelial system

SAXS:

Small angle X-ray scattering

SEM:

Scanning electron microscopy

SFEE:

Supercritical fluid extraction of emulsion

SLN:

Solid lipid nanoparticles

TEM:

Transmission electron microscopy

TPGS:

d-α-Tocopheryl polyethylene glycol 1,000 succinate

WAXS:

Wide angle X-ray scattering

YP:

Yield of production

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  1. Faculty of Health Sciences, Fernando Pessoa University, Rua Carlos da Maia, 296, P-4200-150, Porto, Portugal

    Eliana B. Souto

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  1. Eliana B. Souto
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  2. Rainer H. Müller
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Correspondence to Eliana B. Souto .

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  1. FB Biologie, Chemie, Pharmazie, Inst. Pharmazie, FU Berlin, Königin-Luise-Str. 2-4, Berlin, 14195, Berlin, Germany

    Monika Schäfer-Korting

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Souto, E.B., Müller, R.H. (2010). Lipid Nanoparticles: Effect on Bioavailability and Pharmacokinetic Changes. In: Schäfer-Korting, M. (eds) Drug Delivery. Handbook of Experimental Pharmacology, vol 197. Springer, Berlin, Heidelberg. https://doi.org/10.1007/978-3-642-00477-3_4

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