Why is lipids important in targeted drug delivery system?
Lipid nanoparticles protect the drug against chemical degradation and achieve controlled drug release, once the drug is entrapped in a biocompatible lipid core surrounded by a surfactant at the outer surface.
How does lipid solubility affect drug distribution?
Drug absorption depends on the lipid solubility of the drug, its formulation and the route of administration. A drug needs to be lipid soluble to penetrate membranes unless there is an active transport system or it is so small that it can pass through the aqueous channels in the membrane.
How does lipid solubility affect bioavailability?
Both the lipid solubility of the drug and the pH of the gastric tissues affect drug absorption from the GI tract. Lipid-soluble drugs are absorbed more rapidly than non–lipid-soluble drugs.
What is lipid-based drug delivery system?
Lipid-based drug delivery systems (LBDDS) is a wide-ranging designation for formulations containing a dissolved or suspended drug in lipidic excipients. Lipids are esters of fatty acids – lipophilic hydrocarbon chains linked to a hydrophilic group like glycerol, polyglycerol, or polyalcohol (Figure 1).
What are water soluble drugs?
Drugs that dissolve in water (water-soluble drugs), such as the antihypertensive drug atenolol, tend to stay within the blood and the fluid that surrounds cells (interstitial space). Drugs that dissolve in fat (fat-soluble drugs), such as the antianxiety drug clorazepate, tend to concentrate in fatty tissues.
Why does water solubility matter for a drug molecule?
Solubility is one of the important parameters to achieve desired concentration of drug in systemic circulation for achieving required pharmacological response [12]. Poorly water soluble drugs often require high doses in order to reach therapeutic plasma concentrations after oral administration.
Why is water solubility an important factor in drug design?
Why is water solubility important in drugs?
Solubility plays a critical role in drug effectiveness. Without it, a drug substance cannot be absorbed, leading to low bioavailability. Poor solubility of drugs also leads to other issues, such as challenges with metabolism or permeability, interactions with other drugs or the need to extend drug release.
Which drug is lipid-soluble?
Propranolol, oxprenolol, metoprolol, and timolol are the most lipid-soluble beta-adrenoceptor antagonists, and atenolol, nadolol, and sotalol are the most water-soluble; acebutolol and pindolol are intermediate [14].
What are lipid soluble drugs?
Why are lipids insoluble in water?
Lipids are a large and diverse class of biological molecules marked by their being hydrophobic, or unable to dissolve in water. The hydrophobic nature of lipids stems from the many nonpolar covalent bonds. Water, on the other hand, has polar covalent bonds and mixes well only with other polar or charged compounds.
Which method of delivery has the fastest absorption?
Intravenous (IV) It is the fastest and most certain and controlled way. It bypasses absorption barriers and first-pass metabolism. It is used when a rapid effect is required, continuous administraction and large volumes.
Why is the solubility of lipids important?
In regard to lipid solubility, it is an important measure of the relative safety of chemicals because cells have lipid membrane/cell wall barriers, and so movement of chemicals across membranes and into organs and cells is dependent on its lipophilicity (lipid-solubility).
Why is solubility important in industry?
Apart from key separation issues like extraction and crystal- lization, in pharmaceutical industries, solubility is also an essential property for the design of new drugs. Aqueous solubility gives valuable indications about the biological activity of a drug, and therefore, is most important in pre- formulation studies.
What is lipid solubility of drugs?
Lipid solubility [13] determines the extent to which a drug partitions between an organic solvent and water.
What is the difference between water soluble and lipid soluble drugs?
Which drugs are water soluble?
Disodium cromoglycate, diclofenac sodium, dopamine hydrochloride, isoproterenol hydrochloride, diltiazem hydrochloride and papaverine hydrochloride were selected as water-soluble drugs.
What is a water-soluble drug?
What are the excipients in lipids?
The simplest lipid-based formulations contain only one excipient such as oleic acid, α-tocopherol, corn oil, peanut oil, sesame oil, medium chain triglycerides, or medium chain mono- and diglycerides. All such oral formulations are marketed in soft gelatin capsules.
What is a lipid-based drug delivery system?
Lipid-based drug delivery systems (LBDDS) are one of the emerging technologies designed to address challenges like the solubility and bioavailability of poorly water-soluble drugs.
What are the advantages of lipid formulations of water soluble drugs?
Lipid formulations can reduce the inherent limitation of slow and incomplete dissolution of poorly water-soluble drugs and facilitate formation of solubilised phases from which absorption may occur [ 3 ]. The solubilised phases most likely arise from intralaminal processing after lipid absorption.
Are lipids the future of drug delivery?
The use of lipids in drug delivery is no more a new trend now but is still the promising concept. Lipid-based drug delivery systems (LBDDS) are one of the emerging technologies designed to address challenges like the solubility and bioavailability of poorly water-soluble drugs.