Lipids

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Lipids reagents play important roles in mRNA delivery system development, especially in lipid nanoparticle-formulated drugs. Creative Biolabs has a comprehensive platform for custom delivery vehicle for mRNA and thus provides reliable relevant products that have been proven by our practice.

  • Fatty Acids (FA)

In the field of drug delivery by FA-drug conjugates, there has been rising attention in the use of nanostructured delivery systems to improve drug bioavailability, prolong systemic circulation time, control drug release, increase drug accumulation at the site of action, decrease the risk of adverse reactions, and eventually enhance therapeutic responses. Therefore, a great deal of effort is currently underway to develop nano-vehicles to transport diverse types of drug molecules safely and to effectively release their payload in the right place within the host body. Therefore, combining prodrug technology with the nanostructured delivery systems has been presented by liposomes, emulsions, micelles, SLNs, nanoassemblies, and polymeric NPs to achieve a maximum therapeutic effect with minimal adverse reactions.

  • Monoglycerides

Monoglycerides are swelling amphiphiles as well as liquid crystals. Due to their amphiphilic structure, they can incorporate water and form several distinct physical phases known as mesophases. Mesophases are physical states that have characteristics of two physical states simultaneously (e.g., a semiliquid semisolid phase). The most biologically relevant example of a mesophase is the phospholipid bilayer referred to as the lamellar phase. Liquid crystal refers to the organization of the structures that monoglycerides may assume. As in a crystal, the individual molecules pack into repeatable units, however, portions of the molecule, such as the acyl chains, may exhibit liquid-like traits.

  • Diglycerides

Diglycerides (DG) constitute the main backbone for all naturally occurring glycerolipids. Individual glycerolipid species exhibit their characteristic composition of saturated and unsaturated fatty acids. For example, PIP2 is enriched in arachidonate at the sn-2 position with stearate predominating in the sn-1 position. 1-Ether linkages associated with glycerolipids occur in nature primarily as 1-O-alkyl and 1-O-alk-1-enyl moieties (designated as glycerol ethers and plasmalogens, respectively).

Typical structure of a triglyceride.
  • Triglycerides

Triglycerides are characterized by a typical tendency to crystallize as polymorphs, meaning that they can form different crystalline structures depending on several factors that include chemical composition, presence of impurities, thermal history, and measurement conditions (such as the heating or cooling rate in dynamic conditions), and the dwell time under isothermal conditions.

  • Waxes

Waxes are found in nature as coatings on leaves and stems. Waxes consistently serves a critical role in restricting nonstomatal water loss. It also protects the plant against other environmental stresses, including desiccation, UV radiation, microorganisms, and insects. Waxes consist of a long-chain fatty acid linked through ester oxygen to long-chain alcohol. These molecules are completely water-insoluble and generally solid at biological temperatures.

  • Liquid Lipids

Polymorphic transitions of the lipid may occur with time due to the crystalline structure of solid lipid. At nano-scale, crystallization behavior is different as the solidification temperature decreases in comparison with bulk lipid. The formation of less ordered lipid modification is more pronounced compared with bulk lipid. Therefore, the expulsion of encapsulated drug molecules may be observed during storage, especially when the solid lipid nanoparticles (SLN) matrix is composed of a highly purified lipid, which leads to the limited drug-loading capacity of SLNs. Liquid lipid can overcome the limitations of SLN such as limited drug loading capacity, drug expulsion during storage, and so forth.

  • Cationic lipids

Cationic lipids, one of the most studied classes of compounds for delivery, have attracted much attention as transfection reagents and carriers for gene therapy. Many reviews and book chapters focusing on the application of cationic liposomes for gene delivery have been published. The transfection activity of cationic lipids is determined by their chemical structures, colloidal properties in aqueous solution, and the charge ratio between the cationic lipids and DNA in the complexes. The rationale for the use of cationic lipids for gene therapy relies on their potential to deliver genes into selected cells without inducing significant toxicity.

General structure of cationic lipids or co-lipids for DNA delivery.Fig. 2 General structure of cationic lipids or co-lipids for DNA delivery. (Nicolazzi, 2003)

Lipids Reagents for mRNA Delivery

As a professional mRNA-based therapeutics services provider, Creative Biolabs offers not only custom delivery vehicle services for mRNA, but also relevant products. Our platform is now capable of offering a variety of lipids reagents to help our customers with all kinds of problems. The types of lipids our platform provides include but are not limited to:

If you are working on mRNA-based therapeutics, or you are looking for the assistance of custom delivery vehicle services for mRNA, please feel free to contact us for more information.

References

  1. Ravotti, R.; et al. Triglycerides as Novel Phase-Change Materials: A Review and Assessment of Their Thermal Properties. Molecules. 2020, 25(23).
  2. Nicolazzi, C.; et al. Cationic lipids for transfection. Curr Med Chem. 2003, 10(14): 1263-77.
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