What are Lipid Excipients and Their Applications?

Lipid excipients are a class of materials widely used in drug delivery applications in the pharmaceutical industry. They are used to enhance the solubility, stability, and bioavailability of drugs, as well as to control drug release in the body. Lipid excipients are derived from natural sources, such as vegetable oils and animal fats, or are synthesized in the laboratory. They are biocompatible and biodegradable, making them suitable for use in drug delivery systems.

Lipid excipients play a key role in drug delivery by improving the solubility, stability, and bioavailability of drugs and controlling their release kinetics in the body. They are widely used in oral, parenteral and topical drug delivery systems to enhance the effectiveness of pharmaceutical formulations. In addition, lipid excipients can improve the pharmacokinetics and biodistribution of drugs, thereby improving treatment outcomes and reducing side effects for patients. Their biocompatibility and biodegradability make them suitable for use in the human body, making them an important component of modern drug delivery systems.

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Lipid Excipients in Drug Delivery

Lipid excipients play a key role in the development of lipid drug delivery systems. They can be used as carriers for drugs, as well as stabilizers and modulators of drug release. Lipid excipients can improve the solubility and stability of drugs and control their release kinetics in the body. They can also enhance the biocompatibility and biodegradability of drug delivery systems, making them safe and effective for use in humans. Lipid excipients are commonly used in oral, parenteral, and topical drug delivery systems.

• In oral drug delivery, they are used to improve the solubility and absorption of poorly water-soluble drugs. Lipid excipients can form lipid-based drug delivery systems, such as lipid nanoparticles, liposomes, and solid lipid nanoparticles, which enhance the bioavailability of drugs by improving their solubility and stability in the gastrointestinal tract. Lipid-based drug delivery systems can also protect drugs from degradation and metabolism, thereby improving therapeutic efficacy.
• In parenteral drug delivery, lipid excipients are used to formulate lipid emulsions and lipid nanocarriers for the delivery of poorly soluble drugs. Lipid emulsions are used as carriers for intravenous drugs such as propofol and intravenous nutrients. Lipid-based nanocarriers, such as liposomes and lipid nanoparticles, are used for targeted delivery of drugs to specific tissues or cells in the body. These lipid-based nanocarriers can improve the pharmacokinetics and biodistribution of drugs, thereby enhancing therapeutic efficacy and reducing side effects.
• In topical drug delivery, lipid excipients are used to formulate lipid formulations such as creams, ointments, and gels for delivering drugs to the skin and mucous membranes. Lipid-based formulations can improve drug penetration into the skin and enhance their retention in target tissues, thereby improving therapeutic efficacy. Lipid excipients can also improve the stability and shelf life of topical pharmaceutical formulations, making them suitable for commercial use.

What Can We Offer at BOC Sciences?

• Lipid Excipients Development
• Lipid cGMP Manufacturing
• Lipid Formulation Development
• Lipid Analysis and Characterization
• Lipid Synthesis Services
• Lipid Adjuvant Development
• Lipid Nanoparticles Development
• Lipid Extraction Services
• Liposome Encapsulation Services

Lipid Excipients for Pharmaceutical Applications

Glyceryl Dibehenate

Glyceryl dibehenate is obtained by esterification of glycerin and behenic acid. It is widely used in the development of lipid-based nanocarriers such as solid lipid nanoparticles (SLNs), nanostructured lipid carriers (NLCs), and nanoparticles. For example, Abdelbary and Fahmy prepared SLNs containing varying concentrations of glyceryl dibehenate and glyceryl stearate using a modified high-shear homogenization process and ultrasonic technology. Glyceryl behenate and glyceryl stearate were added as lipid components. It was concluded that glyceryl dibehenate formed SLNs of larger size and resulted in higher encapsulation efficiency of diazepam and significantly sustained release compared to the glyceryl stearate formulation.

Dynasan

These pure monotriglycerides are glyceryl esters of saturated, even-numbered and unbranched monofatty acids, such as plant-derived trimyristate (Dynasan® 114), tristearin (Dynasan® 118) and glycerol Tripalmitin (Dynasan® 116). Dynasan® can also be used as an ingredient to modulate the release rate, depending on the concentration. Studies have used different grades of dyanasan114,116 and 118 to prepare SLN. All six SLNs were prepared using three lipids, with two different concentrations of each lipid. By formulating rosuvastatin calcium solid lipid nanoparticles, a 2.2-fold increase in oral bioavailability compared to the control suspension was observed due to bypassing the effects of first-pass metabolism through the lymphatic transport pathway.

Glyceryl Distearate

Glyceryl distearate consists of stearate and palmitate. It has excellent anti-friction properties and is ideal for capsule filling and taste masking. Currently, glyceryl distearate is widely used for taste masking, mainly using melt granulation technology and matrix encapsulation. Glyceryl distearate can also prevent dissolution by forming a physical barrier to dissolution, known as matrix encapsulation, where the drug is encapsulated in a lipid matrix with very small amounts of the drug retained on the surface, which is tolerable on dissolution into the saliva.

Glyceryl Caprylate

These mono- and diglyceride emulsifiers are prepared by glycerolysis of specific oils, fats and fractionated vegetable oil fatty acids used in lipid formulations. For example, medium-chain glycerides (glyceryl caprylate) are used as the lipid phase, ethanol is added as a co-surfactant, and polyoxyethylene ester of 12-hydroxystearic acid is added as a surfactant. Microemulsions showed significantly enhanced dissolution and oral bioavailability of the active drug without any intestinal toxicity.

Non-Ionic Surfactant (Lauroyl Polyoxyl-32 Glycerides)

The lauroyl polyoxyl-32 glycerides are carriers for a series of mixtures of mono-, di- and triglycerides derived from fatty acid PEG esters. Lauroyl polyoxyl-32 glycerides forms microemulsions, which emulsify into fine dispersions on contact with an aqueous medium. It is a nonionic surfactant that is dispersible in water. Due to its surface-active properties, it can promote enhanced solubility and wetting ability of APIs in vitro and in vivo. For topical formulations, it is used as a coagulant (thickening agent).

Caprylocaproyl Macrogol-8 Glyceride

Caprylocaproyl macrogol-8 glyceride is a nonionic oil-in-water surfactant that is both oil and water soluble. Due to its emulsifying and absorption-enhancing properties, it has a wide range of applications in topical and transdermal formulations. Zhou and colleagues observed that the oral bioavailability of resveratrol was increased due to the use of caprylocaproyl macrogol-8 glyceride (labrasol) as an auxiliary emulsifier, which inhibited intestinal glucuronidation. The nanoemulsion was prepared by using soybean oil as oil phase, soybean lecithin as emulsifier and caprylocaproyl macrogol-8 glyceride as co-emulsifier. In vitro absorption studies were conducted in the everted bursa, and the results showed that the inhibition of UDP-glucuronosyltransferase by caprylic acid decanoic acid polyethylene glycol glyceride increased the transfer rate of resveratrol in the everted bursa. Compared with the negative control nanoemulsion, the AUC of caprylic acid decanoic acid polyethylene glycol glyceride nanoemulsion in vivo increased by 2.92 and 5.60 times respectively. The superior output of the nanoemulsions was attributed to the inhibition of intestinal glucuronidation in the presence of UDP-glucuronosyltransferase inhibitory excipients.

Medium Chain Triglycerides

Medium chain triglycerides have excellent spreadability on the skin and better skin absorption. Caprylic/capric triglycerides are used as emollient, penetration enhancer, pharmaceutical carrier, solvent, and in oral and dermal formulations. In addition, the composition of the self-emulsifying drug delivery system (SEDDS) blend (oil phase) generally also contains CsA, polyoxyethylene castor oil, diethylene glycol monoethyl ether, and capric triglyceride.

Glyceryl Stearate

Glyceryl stearate typically contains about 40%–55% monoesters and is commonly used as a co-emulsifier and consistency enhancer in oil-in-water emulsions. It helps stabilize the lotion and improves the texture and feel of the final product. Prombutara et al. prepared nisin-filled SLNs using high-pressure homogenization to protect them from the food environment and prolong their effects in the body (slow release). The antimicrobial activity of nisin-loaded SLN against L. monocytogenes DMST 2871 and L. plantarum TISTR 850 was observed for up to 20 and 15 days, compared with only 1 and 3 days for free nisin, respectively.

Application of Lipid Excipients^[1]

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Reference

1. Nakmode D. et al. Fundamental aspects of lipid-based excipients in lipid-based product development. Pharmaceutics. 2022,14(4): 831.