Some Multifunctional Lipid Excipients and Their Pharmaceutical Applications

Abstract

This review is generally focussed on lipid-based excipients in solid oral formulations which increase its bioavailability. Several approaches have been used to deliver the drug efficiently in the body, and lipid excipients are one of the promising drug delivery systems which address challenges like solubility and bioavailability of water-soluble drugs. Lipids excipients can be tailored to meet a wide range of product requirements like disease indication, route of administration, stability, toxicity, and efficacy. This review discusses novel lipids like Compritol 888 ATO, Dynasan 114, and Precirol ATO 5 and how these can be employed for devicing efficient drug delivery models and thereby have used in cosmetic and pharmaceutical industries.Lipids can be classified in many ways, due to their different composition, nature and origin. According to with Bloor's classification, lipids can be divided into simple lipids, compound lipids, and derived lipids. Individual characteristics are not discussed in this section because they are well known. Simple LipidsThese are those compounds which belong to heterogeneous class of predominantly nonpolar compounds such as Lecithin and Cephalins. Compound LipidsThese are esters of fatty acids with alcohols. Compounds molecules also contain additional functional groups such as a phosphate ion, simple sugar, amino acid, sulphate ion and oligopeptides. Examples are fatty acids, alcohols, monoglycerides and diglycerides, steroids, terpenes, carotenoids. Derived LipidsThese are those substances which are derived from simple and compound lipids by hydrolysis. Derived lipids include fatty acids, alcohols, monoglycerides and diglycerides, steroids, terpenes, carotenoids. Steroids, terpenes and carotenoids are the most common derived lipids. Some of the most important lipids are shown in table 1, [20][21][22][23][24][25].

Oleogel Formulations for the Topical Delivery of Betulin and Lupeol in Skin Injuries—Preparation, Physicochemical Characterization, and Pharmaco-Toxicological Evaluation

“…Glyceryl dibehenate, a biocompatible pharmaceutically approved excipient with GRAS status, is frequently used as an oil gelator due to its pronounced lipophilic character and its moderate melting point of 64–74 °C [ 53 ]. Furthermore, it has the ability to efficiently entrap active substances in its solid matrix formed in oleogels, consequently delaying their release [ 54 ].…”

Merging konjac glucomannan with other copolymeric hydrogels as a cutting-edge liquid raft system for dual delivery of etoricoxib and famotidine

“…Previously, the addition of lipids like Pr was known for their biodegradability, as a gelling agent (DEVI & Agarwal, 2019 ), and their ability to improve gelling capacity (Abou Youssef et al., 2015 ). The exact role of Pr in improving gelling ability and decreasing the gelation lag time is not clear.…”

Impact of solid lipid nanoparticles on 3T3 fibroblasts viability and lipid profile: The effect of curcumin and resveratrol loading

“…All the empty formulations did not show cytotoxic effect in 3T3 cells at long‐term exposure (24 h of incubation), independently of the lipid and TRC amount; therefore, this incubation time was chosen for all cell viability assessments. Components (Compritol®, TRC and Poloxamer 188) of empty SLN are safe and well‐tolerated compounds, used in many cosmetic and pharmaceutical products for skin and/or oral delivery (Björklund et al, 2016 ; Cortés et al, 2021 ; Devi & Agarwal, 2019 ).…”

“…TRC is a penetration enhancer, a safe and well‐tolerated solvent/vehicle used in the formulation or manufacturing process of pharmaceuticals, cosmetics, and food additives (Björklund et al, 2016 ; Sullivan et al, 2014 ). The observed significant increase in the cell level of S/M‐PL and MUFA, mainly 18:1 n‐9, after the treatment with empty‐TRC 4%‐SLN 4% could be probably ascribable to an enhanced cellular uptake of nanoparticles (Panariti et al, 2012 ) helped by TRC, coupled to the metabolism of behenic acid (22:0), the main FA of Compritol® (Devi & Agarwal, 2019 ). After SLN membrane interaction/uptake, behenic acid, derived from the lipolysis of its glyceryl derivatives, was possibly metabolized/oxidized by fibroblasts into the shorter‐chain FA 18:1 n‐9, which was then used for the synthesis of phospholipids.…”

“…Starting from all these considerations, the aim of this study was to evaluate the simultaneous impact of different types of unloaded and loaded SLN on cell viability and lipid metabolism in relation to their composition (lipid content, penetration enhancer, and encapsulated compounds). SLN were prepared with different amounts of Compritol® 888 ATO (monoesters, diesters, and triesters of behenic acid 22:0; the structure of glyceryl behenate is reported in Figure 1A ) as lipid matrix, Poloxamer 188 (P188) as nanoparticle stabilizer, and Transcutol® P (TRC) (Figure 1A ) as penetration enhancer, excipients amply used in cosmetic and pharmaceutical products for their tolerability (Björklund et al, 2016 ; Cortés et al, 2021 ; Devi & Agarwal, 2019 ). In a previous study, we demonstrated that the use of TRC in a SLN formulation containing 4% of Compritol 888 ATO could enhance the cellular uptake of nanoparticles and cell lipid modulation (Pitzanti et al, 2020 ).…”