Lipid & Preparation Solutions

Lipid preparations, after nearly half a century of research, the technology has been relatively mature. The preclinical prescription screening process of this dosage form has a short cycle, a small amount of compounds, and obvious cost control advantages. It has become one of the best candidate dosage forms for early intervention in preclinical drug development. Lipid-based drug delivery systems ( LBDDS ) are the most widely studied of all technologies for improving bioavailability, and are used as a formulation technology to solve the problems of solubility and permeability. BOC Sciences is a leading supplier of lipids. We support the formulation development of a variety of lipid pharmaceutical preparations, including unilamellar liposomes (ULV), multivesicular liposomes (MVL), multilamellar liposomes (MLV), giant vesicles and bicelle.

Fig. 1. Lipid formulation of ibrutinib (Journal of Drug Delivery Science and Technology. 2022, 77: 103912).

Types of Lipid Preparations

The formulation composition of lipid preparations usually contains oils, and/or surfactants, and/or small molecule co/co-solvents, etc. Types of lipid preparations are generally divided into 4 categories:

• Category I: Pure oil phase composition. The dispersion process of this type of preparation in the gastrointestinal tract basically does not affect the solubilization of the drug, but the digestion process usually has a greater impact on the solubilization of the drug.
• Class II: Composition of oil + water-insoluble surfactant. The dispersion process of this type of preparation in the gastrointestinal tract basically does not affect the solubilization of the drug, but the digestion process may have an impact on the solubilization of the drug.
• Class III: Composition of oil + water-soluble surfactant + solvent. This type of preparation has the ability to self-emulsify, usually forming nanoparticles with small particle size and uniform distribution, which can be directly absorbed by intestinal epithelial cells. During the dispersion and digestion process in the gastrointestinal tract, it may affect the solubilization and absorption of the drug.
• Category IV: Water-soluble surfactant + solvent (without grease). This type of preparation does not contain fat, and the dispersion process may have a greater impact on the solubilization of the drug, but the impact on the digestion process is relatively small.

Our Lipid Preparation Srevices

The component selection of lipid preparations needs to fully consider the physical and chemical properties of the drug, the affinity of the drug and lipid excipients, pharmacokinetic requirements, and the dosage form of the future drug (oral milk/liquid soft capsule/hard capsule), etc.

Lipid Preparation Excipients

There are many types of excipients used in lipid preparations, and factors that need to be considered are regulatory acceptance, safety, dispersion characteristics, etc. Excipient safety is a major consideration because the vast majority of FDA-approved drugs are intended for long-term use. According to the classification of Lipid Formulation Classification System (LFCS), excipients of lipid preparations can be divided into three categories: (1) oil phase; (2) surfactants; (3) cosolvents. Among them, surfactants can be divided into surfactants greater than 12 and less than 12 according to the hydrophilic-lipophilic balance value. BOC Sciences can support the selection of excipients, including surfactants and cosolvents, based on drug formulations. Our surfactants work to improve drug solubility and the self-emulsifying properties of the vehicle, thereby reducing reliance on the patient's digestive function. Additionally, we support the screening and optimization of cosolvents aimed at improving drug solubility and dispersion rates in lipid formulations.

Lipid Preparation APIs

When developing lipid formulations such as lipid-based drug delivery systems (LBDDS), there are many factors that need to be considered, such as excipients, solubility, stability, scale-up and production. Typically, the key to LBDDS development is dissolution and preventing the drug from leaching out in the body. In addition to this, data based on the physicochemical properties of drug molecules are also needed to help researchers predict the most promising formulation route for a given compound. For lipid preparations, the closely related physical and chemical properties include fat solubility, solubility, molecular weight, etc. Based on the selection of formulations based on the physical and chemical properties of the compounds, BOC Sciences' experienced R&D team can customize the development process of lipid formulations based on the molecular weight, stability, solubility, pH, melting point and other properties of the compounds. We have expertise in designing lipid drug delivery systems for various routes of administration, including oral, parenteral and topical delivery. Our R&D team can also optimize lipid formulations for targeted delivery to specific tissues or cells, as well as sustained-release or controlled-release applications.

What Can We Offer?

• Lipid support for liposome formulation
• Liposome formulation development
• Preparation of unilamellar vesicles (ULV)
• Preparation of multivesicular liposomes (MVL)
• Preparation of multilamellar vesicles (MLV)
• Preparation of giant vesicle
• Preparation of bicelle

Lipid Characterization Services

• Particle size distribution
• Liposome morphology and/or structure
• Surface charge (zeta potential)
• Thermodynamic properties of liposome membranes
• In vitro release characteristics of active substances in liposomal drug products
• Weight molar osmotic pressure concentration
• pH testing
• Aggregation detection
• Loading efficiency of active substances
• Impurity detection
• The physical state of the encapsulated active substance
• For drugs whose liposome surface is modified with targeting molecules (such as ligands)

Advantage of Our Lipid Preparations

Lipid preparation solutions from BOC Sciences support the delivery of poorly water-soluble compounds, liquid lipid-soluble drugs, or volatile drugs. Building on our expertise in lipid formulation development and drug delivery, our lipid preparation offer a range of advantages:

• Improving drug dissolving and dissolving: Our lipid preparations are designed to improve drug dissolution and dissolution to increase drug absorption.
• Maintain the soluble stability of the drug: We support lipid preparations with a variety of particulate structures, including vesicles, mixed micelles, etc., to stabilize the dissolution state of the drug throughout the digestion process, thereby achieving sustained drug absorption over a long period of time.
• Increasing intestinal permeability: We usually use medium-chain fatty acids (C8-C10) and some surfactants to promote the intestinal epithelial cells' ability to bypass absorption and transcellular transport, thereby improving the intestinal permeability of the drug.
• Reducing liver metabolic effect: Using solubilizing excipients such as unsaturated long-chain fatty acid esters (such as C16-C18) to promote lymphatic absorption of the drug, thereby reducing hepatic first-pass metabolism.
• Reducing food effect: We can also design the formulation of lipid preparations to reduce the impact of a high-fat diet on absorption.

Reference

1. Song, P. et al. Preparation and evaluation of ibrutinib lipid-based formulations. Journal of Drug Delivery Science and Technology. 2022, 77: 103912.