Lipid Excipients Development

Lipid excipients are an important component of drug delivery systems, providing multiple functions such as solubilization, stabilization, and controlled release of active pharmaceutical ingredients (APIs). BOC Sciences is a leading provider of lipid excipient development services, offering a broad range of lipid excipients and expertise to support pharmaceutical companies developing lipid-based drug delivery systems. Our lipid excipient development and cGMP manufacturing services are a resource for pharmaceutical and biotechnology companies seeking to develop and produce high-quality lipid formulations. As the demand for lipid formulations continues to grow, we are well-prepared to meet our customers' needs and support the development of lipid-based drug products in the pharmaceutical industry.

What is Lipid-Based Excipients?

Lipid drug delivery systems (LBDDS) are formulations consisting of drugs dissolved or suspended in lipid excipients. LBDDS have been widely explored for the delivery of lipophilic drugs, where lipids keep the drug in a dissolved form. LBDDS are typically formulated by dissolving the drug in a molten mixture of lipids and emulsifying with water to form a stable lipid system. Solubility screening is most commonly used to determine the optimal lipid excipient for a given drug. Surfactants are used to stabilize lipid particles by reducing the surface free energy or interfacial energy of solid particles, thereby inhibiting aggregation. Lipid excipients also facilitate the distribution of drugs within skin epidermal lipids, thus accelerating drug penetration in human skin.

Fig. 1. Research on lipid excipients in pharmaceutical formulations (International Journal of Pharmaceutics. 2022, 624: 122013).

Lipid excipients play a crucial role in drug delivery, especially for poorly water-soluble drugs. Lipid-based drug delivery systems can improve the solubility, bioavailability, and stability of APIs, thereby improving therapeutic efficacy. Lipid excipients can be used to formulate various types of drug delivery systems, including lipid nanoparticles, liposomes, emulsions, and solid lipid nanoparticles. These systems can be designed to deliver drugs through different routes of administration (e.g., oral, parenteral, and topical).

Lipid Excipient Development Services

BOC Sciences provides comprehensive lipid excipient development services to support pharmaceutical companies in formulating and optimizing lipid drug delivery systems. Our expertise in lipid excipient development covers a broad range of lipid excipients, including natural and synthetic lipids, surfactants and co-solvents. Our lipid excipient development services include:

Lipid Excipient Screening

BOC Sciences offers screening of the most suitable lipid excipients for specific drug compounds and delivery requirements. Our team of lipid experts can provide advice and screening synthesis services on lipid excipient selection based on the excipient's solubilizing ability, compatibility with the API, and desired drug release profile.

Pre-formulation Studies

After a suitable excipient is synthesized or screened, BOC Sciences can also conduct pre-formulation studies to evaluate the physical and chemical properties of the excipient and its interaction with the API. These studies provide valuable information for the selection and optimization of excipients in pharmaceutical formulations. Our lipid analysis and characterization services can characterize lipid composition in detail and identify and quantify the various lipid classes present in a sample.

Formulation Development Services

BOC Sciences provides formulation development services for lipid drug delivery systems, including lipid nanoparticles, liposomes, and emulsions. Our formulation scientists can develop optimized drug formulations using a variety of lipid products to achieve desired drug delivery properties.

Analytical Method Development

The quality of lipid components, including modified lipids (e.g., polyethylene glycol-modified lipids, Lipid PEG), may affect the quality and performance of lipid-based drug products. When using novel lipid formulations, the nature of the excipients in the drug system should also be clearly analyzed. BOC Sciences develops and validates analytical methods for characterizing lipid drug delivery systems, including lipid excipient analysis, drug release studies, and stability testing.

Classification of Our Lipid Excipients

Manufacturing of Lipid Excipients

BOC Sciences' pharmaceutical grade lipid excipients are manufactured in cGMP compliant facilities and are of high quality and compliance. We provide scale-up and manufacturing support for lipid delivery systems, helping pharmaceutical companies transition from lab-scale formulations to commercial production. Our lipid excipient manufacturing services are supported by robust quality assurance and control systems. Facilities are regularly audited and inspected by regulatory agencies to ensure compliance with cGMP regulations. In addition, BOC Sciences' quality control team performs rigorous testing and analysis of lipid excipients to ensure their purity, potency and stability. Our lipids have a reliable source of raw materials to support a variety of pharmaceutical dosage form needs:

• Lipid solvents
• Structural agents
• Lubricants
• Cream bases
• Emollients
• Penetration accelerators
• Emulsifiers
• Surfactants
• Solubilizers

Why Choose BOC Sciences?

• Expertise in lipid excipient selection and formulation development: BOC Sciences' team of lipid experts provides valuable expertise in excipient selection and formulation development to help pharmaceutical companies optimize the performance of their drug products.
• Comprehensive lipid excipient development services: BOC Sciences offers comprehensive lipid excipient development services, from pre-formulation studies to scale-up and production support.
• One-stop customized solutions: BOC Sciences works closely with pharmaceutical companies to develop custom lipid drug delivery systems that fit their specific drug compounds and delivery requirements.
• Quality and regulatory compliance: BOC Sciences adheres to the highest quality standards and regulatory requirements in the development and manufacturing of lipid delivery systems to ensure the safety and effectiveness of pharmaceutical products.
• Cost-effective and time-efficient solutions: BOC Sciences' excipient development services are designed to provide cost-effective and time-efficient solutions to help pharmaceutical companies accelerate the development of their drug products.

Case Study

Mancini and colleagues explored the use of glyceryl dibehenate in preparing SLNs for topical application. Using glyceryl dibehenate as solid lipid and polyoxyethylene sorbitan monooleate as surfactant, SLN was prepared by melt emulsification method. Liquid (etofenamate) and solid (ibuprofen) drug molecules were loaded into hydrogels prepared by gelation of SLN suspension using 2% hydroxypropyl methylcellulose gel. Encapsulating drugs in lipid nanoparticles prevents drug leakage and protects them from the external environment. The prepared formulation was found to have suitable particle size (<250 nm) with an encapsulation efficiency of 90%. Furthermore, SLN-containing hydrogels showed increased drug permeability compared to commercially available hydrogel formulations.^[3]

Fig. 2. (A) Encapsulation efficiency of etofenamate (a) and ibuprofen (b) in SLN. (B) Release profiles of etofenamate (a) and ibuprofen (b) incorporated in SLN and SLN-gels (Pharmaceutics. 2021, 13: 328).

FAQ

1. What are the excipients in lipid nanoparticles?

Excipients in lipid nanoparticles include surfactants, stabilizers, and co-solvents. Some common excipients used in lipid nanoparticles include phospholipids, cholesterol, polyethylene glycol (PEG), and other nonionic surfactants. These excipients help stabilize lipid nanoparticles, improve their drug-loading capacity and control their release profile.

2. What are lipid based drugs examples?

Lipid pharmaceutical system refers to a type of pharmaceutical preparation in which one or more API are encapsulated in a lipid bilayer or/and in an aqueous phase to form a drug-loaded system. Currently, approved drugs based on lipid formulations include Amprenavir, Ranitidine, Topotecan, Sirolimus, Saquinavir, Tipranavir, Dutasteride, and Cyclosporine.

References

1. Abdelhamid, M. et al. Filament-based 3D-printing of placebo dosage forms using brittle lipid-based excipients. International Journal of Pharmaceutics. 2022, 624: 122013.
2. Nakmode D. et al. Fundamental aspects of lipid-based excipients in lipid-based product development. Pharmaceutics. 2022,14(4): 831.
3. Mancini G. et al. Increased Therapeutic Efficacy of SLN Containing Etofenamate and Ibuprofen in Topical Treatment of Inflammation. Pharmaceutics. 2021, 13: 328.