Liposome Encapsulated Small Molecule Development Service

Through the intelligent delivery of drugs, liposomes provide a solid foundation for the sustainable development of various commercial products for the treatment of medical diseases. It has been proven that sterically stabilized liposomes can extend the circulation time of small molecule drugs by reducing the clearance of the reticuloendothelial system (RES).

Background of Small Molecule Drugs

In the field of molecular biology and pharmacology, the small molecule is a kind of organic compound with low molecular weight (< 900 Da), which can regulate biological processes, and its size is about 1 nm. Small molecule drugs can be enzyme inhibitors, receptor ligands or allosteric modulators. They are widely used in the diagnosis and chemotherapy of cancer, vaccinology, ophthalmology, pulmonology and other pathologies. Small molecule drugs are widely used in the clinic, but their therapeutic effects are limited by their fast clearance, poor biological distribution, low intracellular absorption rate and low toxicity in vivo. These shortcomings can be overcome by loading drugs into the drug delivery system, especially liposomes.

Fig.1 Two major methods for liposomal drug loading

Liposome Encapsulated Small Molecule Drugs Development

The unique feature of liposomes is that they can naturally separate and solubilize hydrophilic and hydrophobic materials. This unique function, coupled with biocompatibility and biodegradability, makes liposomes attractive as drug delivery media.

At present, Creative Biolabs has enough mature technology platform to encapsulate many kinds of small molecule drugs into liposomes.

• Liposomal Hydrophilic Small Molecule Drugs Development

Hydrophilic small molecule drugs are encapsulated in the aqueous internal volume formed by lipid bilayers. These molecules generally do not interact with the lipid moiety of the vesicle. Polyethylene glycol (PEG) modified long-circulating liposomes and other formulations containing cytotoxic drugs such as doxorubicin, paclitaxel and vincristine are clinically approved chemotherapeutic liposome formulations.

Fig.2 Hydrophilic drug encapsulation methods

• Liposomal Hydrophobic Small Molecule Drugs Development

Hydrophobic drugs are solubilized in the lipid bilayer of liposomes that mainly provide a hydrophobic environment. Once captured, they remain in the bilayer membrane of the liposome because of their low affinity for the internal or external aqueous regions of the liposome. During the preparation of liposomes, the hydrophobic drugs and phospholipids were dissolved in organic solvents. In the subsequent hydration stage, the hydrophobic drugs were still wrapped in the hydrophobic double-layer region.

What We Can Do about Liposome Encapsulated Small Molecule Drugs Development?

Creative Biolabs provides contract services for the development of liposome pharmaceutical formulations for the pharmaceutical/biotechnology industry. We have strong and extensive expertise and years of experience in the field of drug delivery and lipid biophysics.

By selecting a suitable preparation method to affect the final amount of the encapsulated drug, we provide liposomes of various sizes, lamellae and physicochemical properties to which hydrophilic and hydrophobic small-molecule drugs can be encapsulated, so as to improve the defects of these drugs. For more details about our services, please directly contact us.

For Research Use Only. Not For Clinical Use