Abstract
An important step in oral drug development is to identify drug candidates that show sufficient aqueous solubility and could resist or bypass first-pass metabolism in order to overcome bioavailability problems. Aqueous solubility is characteristically low for Biopharmaceutical Classification System (BCS) class II and class IV drug candidates. Several formulation approaches are being identified to overcome the low solubility aspect of a drug candidate such as particle size manipulation, solid dispersions, inclusion complexes and several of nanoparticle-based options. However, the formulation for drug candidates that in addition to low aqueous solubility shows high intestinal and first-pass metabolism is challenging. The self-emulsifying lipid formulations (SELF) provide a mean for sidestepping these factors and improve the bioavailability of lipophilic and highly first- pass metabolised drugs. Nevertheless, formulation of a successful SELF requires an exhaustive understanding of the component used to formulate them, the behaviour of the formulation within the gastrointestinal (GI) milieu and the mechanism by which the drug is released and absorbed. This review gives a brief description of the formulation aspects of SELF and their potential role to mitigate the bioavailability problem related to lipophilic and highly first- pass metabolised drugs.
Keywords: BCS, lipidic excipients, lymphatic absorption, precipitation, SELF, supersaturation.
Current Drug Delivery
Title:Self-Emulsifying Lipid Formulation: An Overview
Volume: 12 Issue: 2
Author(s): Vikrant Saluja, Sunnia Arora and Suman Goyal
Affiliation:
Keywords: BCS, lipidic excipients, lymphatic absorption, precipitation, SELF, supersaturation.
Abstract: An important step in oral drug development is to identify drug candidates that show sufficient aqueous solubility and could resist or bypass first-pass metabolism in order to overcome bioavailability problems. Aqueous solubility is characteristically low for Biopharmaceutical Classification System (BCS) class II and class IV drug candidates. Several formulation approaches are being identified to overcome the low solubility aspect of a drug candidate such as particle size manipulation, solid dispersions, inclusion complexes and several of nanoparticle-based options. However, the formulation for drug candidates that in addition to low aqueous solubility shows high intestinal and first-pass metabolism is challenging. The self-emulsifying lipid formulations (SELF) provide a mean for sidestepping these factors and improve the bioavailability of lipophilic and highly first- pass metabolised drugs. Nevertheless, formulation of a successful SELF requires an exhaustive understanding of the component used to formulate them, the behaviour of the formulation within the gastrointestinal (GI) milieu and the mechanism by which the drug is released and absorbed. This review gives a brief description of the formulation aspects of SELF and their potential role to mitigate the bioavailability problem related to lipophilic and highly first- pass metabolised drugs.
Export Options
About this article
Cite this article as:
Saluja Vikrant, Arora Sunnia and Goyal Suman, Self-Emulsifying Lipid Formulation: An Overview, Current Drug Delivery 2015; 12 (2) . https://dx.doi.org/10.2174/1567201811666140924130224
DOI https://dx.doi.org/10.2174/1567201811666140924130224 |
Print ISSN 1567-2018 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5704 |
Call for Papers in Thematic Issues
Advances of natural products, bio-actives and novel drug delivery system against emerging viral infections
Due to the increasing prevalence of viral infections and the ability of these human pathogens to develop resistance to current treatment strategies, there is a great need to find and develop new compounds to combat them. These molecules must have low toxicity, specific activity and high bioavailability. The most suitable ...read more
Electrospun Fibers as Drug Delivery Systems
In recent years, electrospun fibers have attracted considerable attention as potential platforms for drug delivery due to their distinctive properties and adaptability. These fibers feature a notable surface area-to-volume ratio and can be intentionally designed with high porosity, facilitating an increased capacity for drug loading and rendering them suitable for ...read more
Emerging Nanotherapeutics for Mitigation of Neurodegenerative Disorders
Conditions affecting the central nervous system (CNS) present a significant hurdle due to limited access of both treatments and diagnostic tools for the brain. The blood-brain barrier (BBB) acts as a barrier, restricting the passage of molecules from the bloodstream into the brain. The most formidable challenge facing scientists is ...read more
Nanotechnology Based Chemotherapy for the treatment of Head & Neck Cancer
The escalating recurrence rates observed in Head and Neck cancer, particularly within the chemo-therapeutically treated cohort (50-60%), can be attributed to the non-selective nature of current anticancer drug delivery modalities. In this context, nanotechnology-based drug delivery systems emerge as a promising avenue for achieving precise localization of therapeutic agents to ...read more
- Author Guidelines
- Graphical Abstracts
- Fabricating and Stating False Information
- Research Misconduct
- Post Publication Discussions and Corrections
- Publishing Ethics and Rectitude
- Increase Visibility of Your Article
- Archiving Policies
- Peer Review Workflow
- Order Your Article Before Print
- Promote Your Article
- Manuscript Transfer Facility
- Editorial Policies
- Allegations from Whistleblowers
Related Articles
-
Anti-Cancer Phytometabolites Targeting Cancer Stem Cells
Current Genomics Interactome Analysis of the Differentially Expressed Proteins in Uterine Leiomyoma
Anti-Cancer Agents in Medicinal Chemistry Laboratory Techniques for Human Viral Encephalitis Diagnosis
Infectious Disorders - Drug Targets Ribonucleases, Nucleases and Antiangiogenins in Antiproliferative Activities
Current Signal Transduction Therapy Cathepsin D as a Promising Target for the Discovery of Novel Anticancer Agents
Current Cancer Drug Targets Retinal Ganglion Cell Gene Therapy and Visual System Repair
Current Gene Therapy Advances in Cancer Stem Cell Therapy: Targets and Treatments
Recent Patents on Regenerative Medicine Polypharmacology of <i>Aconitum</i> and <i>Delphinium</i> sp. Diterpene Alka loids: Antiarrhythmic, Analgesic and Anti-Inflammatory Effects
Mini-Reviews in Organic Chemistry HTLV-1-Associated Myelopathy/Tropical Spastic Paraparesis (HAM/TSP): Still an Obscure Disease
Central Nervous System Agents in Medicinal Chemistry Multiple Metamorphoses of CD38 from Prognostic Marker to Disease Modifier to Therapeutic Target in Chronic Lymphocytic Leukemia
Current Topics in Medicinal Chemistry CXXC5 Associates with Smads to Mediate TNF-α Induced Apoptosis
Current Molecular Medicine Central Nervous System Abnormalities in Fibromyalgia and Chronic Fatigue Syndrome: New Concepts in Treatment
Current Pharmaceutical Design Antibody Therapy of Acute and Chronic Leukemias
Current Pharmaceutical Biotechnology Sauropus androgynus Leaves for Health Benefits: Hype and the Science
The Natural Products Journal Anti-Cancer Drugs of Today and Tomorrow: Are we Close to Making the Turn from Treating to Curing Cancer?
Current Pharmaceutical Design Dual Inhibition of Cdc7 and Cdk9 by PHA-767491 Suppresses Hepatocarcinoma Synergistically with 5-Fluorouracil
Current Cancer Drug Targets Inflammation and Anemia
Anti-Inflammatory & Anti-Allergy Agents in Medicinal Chemistry Functional and Structural Roles of GPI Moieties in Mammalian Plasma Membranes
Current Organic Chemistry Latest Advancements on Serotonin and Dopamine Transporters in Lymphocytes
Mini-Reviews in Medicinal Chemistry Cardioprotection by Targeting the Pool of Resident and Extracardiac Progenitors
Current Drug Targets