Recent advances in oral delivery of drugs and bioactive natural products using solid lipid nanoparticles as the carriers

Chemical and enzymatic barriers in the gastrointestinal (GI) tract hamper the oral delivery of many labile drugs. The GI epithelium also contributes to poor permeability for numerous drugs. Drugs with poor aqueous solubility have difficulty dissolving in the GI tract, resulting in low bioavailabilit...

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Published inYàowu shi͡p︡in fenxi Vol. 25; no. 2; pp. 219 - 234
Main Authors Lin, Chih-Hung, Chen, Chun-Han, Lin, Zih-Chan, Fang, Jia-You
Format Journal Article
LanguageEnglish
Published China (Republic : 1949- ) Elsevier B.V 01.04.2017
Food and Drug Administration
Taiwan Food and Drug Administration
Subjects
Acids
Administration, Oral
adverse effects
Bioavailability
Biocompatibility
Biological Availability
Biological Products
Biomedical materials
Central nervous system
diabetes
Diabetes mellitus
Disease
drug
Drug Carriers
Drug delivery
Drug delivery systems
Drugs
encapsulation
engineering
Epithelium
Formulations
gastrointestinal system
Gastrointestinal tract
half life
Humans
Lipids
Lymphatic system
Medical treatment
medicinal properties
Metabolism
Migraine
Mucosa
nanomedicine
Nanoparticles
Nanotechnology
natural compound
Natural products
neoplasms
Oral administration
oral delivery
Organic chemistry
Osteoporosis
Permeability
Pharmacology
Physicochemical properties
Psychosis
Review
Side effects
solid lipid nanoparticles
Solubility
Tropical diseases
gastrointestinal tract
natural compound
oral delivery
solid lipid nanoparticles
drug
Online AccessGet full text

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Abstract Chemical and enzymatic barriers in the gastrointestinal (GI) tract hamper the oral delivery of many labile drugs. The GI epithelium also contributes to poor permeability for numerous drugs. Drugs with poor aqueous solubility have difficulty dissolving in the GI tract, resulting in low bioavailability. Nanomedicine provides an opportunity to improve the delivery efficiency of orally administered drugs. Solid lipid nanoparticles (SLNs) are categorized as a new generation of lipid nanoparticles consisting of a complete solid lipid matrix. SLNs used for oral administration offer several benefits over conventional formulations, including increased solubility, enhanced stability, improved epithelium permeability and bioavailability, prolonged half-life, tissue targeting, and minimal side effects. The nontoxic excipients and sophisticated material engineering of SLNs tailor the controllable physicochemical properties of the nanoparticles for GI penetration via mucosal or lymphatic transport. In this review, we highlight the recent progress in the development of SLNs for disease treatment. Recent application of oral SLNs includes therapies for cancers, central nervous system-related disorders, cardiovascular-related diseases, infection, diabetes, and osteoporosis. In addition to drugs that may be active cargos in SLNs, some natural compounds with pharmacological activity are also suitable for SLN encapsulation to enhance oral bioavailability. In this article, we systematically introduce the concepts and amelioration mechanisms of the nanomedical techniques for drug- and natural compound-loaded SLNs. [Display omitted] •SLNs are nanosystems for the delivery of drugs with controlled release kinetics.•We highlight the recent progress in the study of oral SLNs for disease treatment.•SLNs are developed by solid lipids and emulsifiers generally recognized as safe.•Both drugs and natural compounds are suitable to be orally delivered by SLNs.
AbstractList Chemical and enzymatic barriers in the gastrointestinal (GI) tract hamper the oral delivery of many labile drugs. The GI epithelium also contributes to poor permeability for numerous drugs. Drugs with poor aqueous solubility have difficulty dissolving in the GI tract, resulting in low bioavailability. Nanomedicine provides an opportunity to improve the delivery efficiency of orally administered drugs. Solid lipid nanoparticles (SLNs) are categorized as a new generation of lipid nanoparticles consisting of a complete solid lipid matrix. SLNs used for oral administration offer several benefits over conventional formulations, including increased solubility, enhanced stability, improved epithelium permeability and bioavailability, prolonged half-life, tissue targeting, and minimal side effects. The nontoxic excipients and sophisticated material engineering of SLNs tailor the controllable physicochemical properties of the nanoparticles for GI penetration via mucosal or lymphatic transport. In this review, we highlight the recent progress in the development of SLNs for disease treatment. Recent application of oral SLNs includes therapies for cancers, central nervous system-related disorders, cardiovascular-related diseases, infection, diabetes, and osteoporosis. In addition to drugs that may be active cargos in SLNs, some natural compounds with pharmacological activity are also suitable for SLN encapsulation to enhance oral bioavailability. In this article, we systematically introduce the concepts and amelioration mechanisms of the nanomedical techniques for drug- and natural compound-loaded SLNs.
Chemical and enzymatic barriers in the gastrointestinal (GI) tract hamper the oral delivery of many labile drugs. The GI epithelium also contributes to poor permeability for numerous drugs. Drugs with poor aqueous solubility have difficulty dissolving in the GI tract, resulting in low bioavailability. Nanomedicine provides an opportunity to improve the delivery efficiency of orally administered drugs. Solid lipid nanoparticles (SLNs) are categorized as a new generation of lipid nanoparticles consisting of a complete solid lipid matrix. SLNs used for oral administration offer several benefits over conventional formulations, including increased solubility, enhanced stability, improved epithelium permeability and bioavailability, prolonged half-life, tissue targeting, and minimal side effects. The nontoxic excipients and sophisticated material engineering of SLNs tailor the controllable physicochemical properties of the nanoparticles for GI penetration via mucosal or lymphatic transport. In this review, we highlight the recent progress in the development of SLNs for disease treatment. Recent application of oral SLNs includes therapies for cancers, central nervous system-related disorders, cardiovascular-related diseases, infection, diabetes, and osteoporosis. In addition to drugs that may be active cargos in SLNs, some natural compounds with pharmacological activity are also suitable for SLN encapsulation to enhance oral bioavailability. In this article, we systematically introduce the concepts and amelioration mechanisms of the nanomedical techniques for drug- and natural compound-loaded SLNs. [Display omitted] •SLNs are nanosystems for the delivery of drugs with controlled release kinetics.•We highlight the recent progress in the study of oral SLNs for disease treatment.•SLNs are developed by solid lipids and emulsifiers generally recognized as safe.•Both drugs and natural compounds are suitable to be orally delivered by SLNs.
Author Chen, Chun-Han
Fang, Jia-You
Lin, Zih-Chan
Lin, Chih-Hung
AuthorAffiliation b Division of General Surgery, Department of Surgery, Chang Gung Memorial Hospital at Chiayi, Chiayi, Taiwan
h Department of Anesthesiology, Chang Gung Memorial Hospital, Kweishan, Taoyuan, Taiwan
a Center for General Education, Chang Gung University of Science and Technology, Kweishan, Taoyuan, Taiwan
d Graduate Institute of Biomedical Sciences, Chang Gung University, Kweishan, Taoyuan, Taiwan
f Chinese Herbal Medicine Research Team, Healthy Aging Research Center, Chang Gung University, Kweishan, Taoyuan, Taiwan
g Research Center for Food and Cosmetic Safety and Research Center for Chinese Herbal Medicine, Chang Gung University of Science and Technology, Kweishan, Taoyuan, Taiwan
c Graduate Institute of Clinical Medical Sciences, College of Medicine, Chang Gung University, Kweishan, Taoyuan, Taiwan
e Pharmaceutics Laboratory, Graduate Institute of Natural Products, Chang Gung University, Kweishan, Taoyuan, Taiwan
AuthorAffiliation_xml – name: f Chinese Herbal Medicine Research Team, Healthy Aging Research Center, Chang Gung University, Kweishan, Taoyuan, Taiwan
– name: g Research Center for Food and Cosmetic Safety and Research Center for Chinese Herbal Medicine, Chang Gung University of Science and Technology, Kweishan, Taoyuan, Taiwan
– name: h Department of Anesthesiology, Chang Gung Memorial Hospital, Kweishan, Taoyuan, Taiwan
– name: b Division of General Surgery, Department of Surgery, Chang Gung Memorial Hospital at Chiayi, Chiayi, Taiwan
– name: e Pharmaceutics Laboratory, Graduate Institute of Natural Products, Chang Gung University, Kweishan, Taoyuan, Taiwan
– name: a Center for General Education, Chang Gung University of Science and Technology, Kweishan, Taoyuan, Taiwan
– name: c Graduate Institute of Clinical Medical Sciences, College of Medicine, Chang Gung University, Kweishan, Taoyuan, Taiwan
– name: d Graduate Institute of Biomedical Sciences, Chang Gung University, Kweishan, Taoyuan, Taiwan
Author_xml – sequence: 1
  givenname: Chih-Hung
  surname: Lin
  fullname: Lin, Chih-Hung
  organization: Center for General Education, Chang Gung University of Science and Technology, Kweishan, Taoyuan, Taiwan
– sequence: 2
  givenname: Chun-Han
  surname: Chen
  fullname: Chen, Chun-Han
  organization: Division of General Surgery, Department of Surgery, Chang Gung Memorial Hospital at Chiayi, Chiayi, Taiwan
– sequence: 3
  givenname: Zih-Chan
  surname: Lin
  fullname: Lin, Zih-Chan
  organization: Graduate Institute of Biomedical Sciences, Chang Gung University, Kweishan, Taoyuan, Taiwan
– sequence: 4
  givenname: Jia-You
  surname: Fang
  fullname: Fang, Jia-You
  email: fajy@mail.cgu.edu.tw
  organization: Pharmaceutics Laboratory, Graduate Institute of Natural Products, Chang Gung University, Kweishan, Taoyuan, Taiwan
BackLink https://www.ncbi.nlm.nih.gov/pubmed/28911663$$D View this record in MEDLINE/PubMed
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Keywords gastrointestinal tract
natural compound
oral delivery
solid lipid nanoparticles
drug
Language English
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Snippet Chemical and enzymatic barriers in the gastrointestinal (GI) tract hamper the oral delivery of many labile drugs. The GI epithelium also contributes to poor...
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SubjectTerms Acids
Administration, Oral
adverse effects
Bioavailability
Biocompatibility
Biological Availability
Biological Products
Biomedical materials
Central nervous system
diabetes
Diabetes mellitus
Disease
drug
Drug Carriers
Drug delivery
Drug delivery systems
Drugs
encapsulation
engineering
Epithelium
Formulations
gastrointestinal system
Gastrointestinal tract
half life
Humans
Lipids
Lymphatic system
Medical treatment
medicinal properties
Metabolism
Migraine
Mucosa
nanomedicine
Nanoparticles
Nanotechnology
natural compound
Natural products
neoplasms
Oral administration
oral delivery
Organic chemistry
Osteoporosis
Permeability
Pharmacology
Physicochemical properties
Psychosis
Review
Side effects
solid lipid nanoparticles
Solubility
Tropical diseases
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Title Recent advances in oral delivery of drugs and bioactive natural products using solid lipid nanoparticles as the carriers
URI https://dx.doi.org/10.1016/j.jfda.2017.02.001
https://www.ncbi.nlm.nih.gov/pubmed/28911663
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Volume 25
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