Lipid & Drug Delivery Solutions

Lipid drug delivery systems are well suited for low water solubility, lipophilic, and hydrophobic drugs. Generally, lipid delivery systems contain one or more excipients, which can be oily formulations, self-emulsifying formulations (SEDDS), self-microemulsifying formulations (SMEDDS) formulations, or micellar solutions. Lipid-based drug delivery systems can be classified into liposomes, lipid nanoparticles, solid lipid nanoparticles, and lipid-based micelles. Lipid-based formulations have revolutionized drug delivery, offering a multifaceted approach to enhancing the solubility and stability of poorly soluble drugs. This groundbreaking advancement not only amplifies bioavailability and therapeutic efficacy but also introduces a paradigm shift in controlled release and targeted delivery, effectively mitigating dosing frequency and ameliorating adverse effects. Moreover, the inherent biocompatibility and exceptional tolerability of lipid-based drug delivery systems render them a versatile and indispensable asset across diverse pharmaceutical applications.

Fig. 1. Lipid nanodelivery systems enhance absorption mechanisms (Adv Food Nutr Res. 2017, 81: 1-30).

Lipid Based Drug Delivery Systems

BOC Sciences is a leading provider of lipid & drug delivery solutions to the pharmaceutical, biotechnology and research industries. Our lipid support services are designed to help customers overcome drug delivery challenges and accelerate the development of lipid-based drug delivery systems. Our broad service categories include formulation development, analytical testing and process optimization, supporting customers at every stage of the drug development process. Here are the lipid-based drug delivery systems we support:

Liposomes

Liposomes are hollow spheres composed of lipid bilayer membranes. In the aqueous phase, lipid molecules usually aggregate spontaneously, with hydrophobic tails "tail-to-tail" and hydrophilic heads "side-by-side". It forms a double-layered hollow vesicle, the hollow part of which can be loaded with hydrophilic drugs, and at the same time, the lipid bilayer can be loaded with lipophilic drugs. Due to this characteristic of liposomes, it is considered to be a good drug carrier. In addition, liposomes have many other advantages, such as adjustable particle size, good stability, sustained release, low toxicity, good biocompatibility, non-immunogenicity, and low cost. Therefore, liposomes, as drug carriers, can well protect drugs from external media and reduce side effects caused by drugs.

Lipid Nanoparticles (LNPs)

Lipid nanoparticles (LNPs) are nanoparticles composed of lipids, an organic molecule that is soluble in fat. LNPs are usually spherical with an average diameter between 10 and 1000 nm. They consist of a lipid core that dissolves lipophilic molecules and a surfactant layer that stabilizes the particles and protects the nucleic acid payload. The lipid core can be solid or liquid, depending on the type and composition of the lipid used. The surfactant layer can be composed of various biomembrane lipids, such as phospholipids, cholesterol, bile salts, or sterols. Optionally, LNPs can also have targeting molecules, such as antibodies or peptides, attached to their surface to enhance their specificity and uptake by certain cells. We generally support lipid nanoparticles composed of the following four main components:

• Cationic or ionizable lipids that complex with negatively charged genetic material and aid in endosomal escape.
• Phospholipids used to form particulate structures.
• Cholesterol for stability and membrane fusion.
• Pegylated lipids for improved stability and circulation.

Lipid nanoparticles are widely used in personalized gene therapy due to their nucleic acid delivery ability, simple synthesis, small size and high serum stability. Among them, ionizable lipid nanoparticles are ideal tools for nucleic acid therapy, which are close to neutral at physiological pH and have charge in acidic endosomes, thereby promoting endosomal escape for intracellular delivery.

Lipid Nanoemulsions (LNEs)

Lipid nanoemulsions (LNEs) are surfactant-stabilized oil-in-water emulsions with small droplet sizes, typically less than 100 nm. These nanoemulsions are colloidal dispersions or heterogeneous mixtures of two liquids. The two liquids are immiscible and one liquid disperses into the other in the form of small droplets. These two liquids are primarily oil and water, giving rise to the two main forms of emulsions, water-in-oil and oil-in-water emulsions. Lipid-based nanoemulsions can alter the absorption, bioaccessibility, and stability of low-solubility compounds and improve bioavailability. Therefore, lipid nanoemulsions are widely used to encapsulate hydrophobic bioactive compounds, including carotenoids, flavonoids, triglycerides, polyphenols, tocopherols, and fat-soluble vitamins.

Solid Lipid Nanoparticles (SLNs)

Solid lipid nanoparticles (SLNs) are submicron-sized spherical vesicles with a unilamellar shell of surfactant and a solid lipid core. The lipid component of SLNs is solid at body and ambient temperatures. The structure of SLNs is amphipathic substances arranged on the outside, a solid lipid matrix on the inside, and drugs in the core. There are three main forms of distribution of related drugs in SLNs, namely solid solution type, lipid core type and drug core type. Judging from the overall characteristics of SLNs, this drug delivery system has physiological compatibility that far exceeds traditional pharmaceutical dosage forms. In addition, SLNs can also significantly improve the stability of drugs during the application process, preventing the drugs from being affected by enzymes or other substances in the body after entering the human body, thereby ensuring that they can fully exert their effectiveness. Drugs in SLN will also show significant sustained-controlled release and targeting characteristics.

Nanostructured Lipid Carriers (NLCs)

Nanostructured lipid carriers (NLCs), also known as second-generation lipid nanocarriers, are one such efficient and targeted drug delivery system. NLCs are lipid formulations with a solid matrix at room temperature. Compared with other traditional lipid nanocarriers (such as nanoemulsions and solid lipid nanoparticles), NLCs have strong stability, low toxicity, extended shelf life, high drug loading capacity and biocompatibility and other advantages. Currently, NLCs are used as important carriers of drugs for brain targeting, cancer and gene therapy.

What Can We Offer?

• Research on the control of phase transition temperature
• Stability studies of lipid formulations
• Supported by specifically charged lipid formulations
• Ready-to-use lipid blend supplies
• Lipid nanoparticle development and manufacturing
• Lipid carrier toxicity testing

Advantages of Lipid Drug Delivery

• Lipid-based drug delivery can protect drugs from degradation and enhance their stability, thereby improving the bioavailability of poorly soluble drugs.
• The versatility of lipid formulations enables controlled release of drugs, providing a more targeted and effective delivery method.
• The custom design of lipid-based drug delivery systems enables them to target specific tissues or cells while mitigating off-target effects.
• Lipid-based drug delivery can be used for drug delivery of a variety of bioactive substances such as nucleic acids, small molecules, peptides, and proteins.

BOC Sciences can partner with customers to develop and optimize lipid formulations for a variety of pharmaceutical compounds, including selecting the most suitable lipids, surfactants and cosolvents, and optimizing formulations to achieve the desired drug release curve, stability and bioavailability. In addition to formulation development, BOC Sciences offers comprehensive analytical testing services to support lipid-based drug delivery systems, such as testing drug content, particle size distribution, zeta potential and drug release kinetics, as well as stability testing of lipid formulations and representation.

Reference

1. Jafari, S.M. et al. Nanotechnology Approaches for Increasing Nutrient Bioavailability. Adv Food Nutr Res. 2017, 81: 1-30.