Customized Lipospheres Drug Delivery Formulation Services

Lipospheres are lipid-based, water-dispersible solid particles with particle sizes ranging from 0.01 to 100 microns, consisting of a solid hydrophobic lipid core containing active drug molecules dissolved or dispersed in a solid lipid matrix, which is stabilized by a layer of phospholipid molecules as a coat. Liposphere systems improve drug stability in formulation, lyophilization and reconstitution properties, controlled particle size, high drug loading, good drug release control and no carrier toxicity. CD Formulation can provide professional liposphere formulation development services, including liposphere physical and chemical analysis, in vivo and in vitro evaluation, etc., to provide customers with the best product solution in all aspects.

Fig.1 Characters of lipospheres. (Ma et al., 2014)

Liposphere Drug Delivery System

Lipospheres are a novel lipid-based encapsulation system for parenteral and topical delivery of biologically active compounds and have been used for delivery of anti-inflammatory compounds, as well as antibiotics, anticancer agents, anthelmintics, vaccines, proteins, and peptides. Lipospheres differ from microspheres of homogeneously dispersed substances in homogeneous polymers because they consist of two layers, with the inner solid particles containing the encapsulated drug.

• Advantages of Lipospheres

• Lipospheres exhibit enhanced physical stability due to the avoidance of agglomeration.
• High dispersibility in aqueous media.
• Low feedstock cost.
• Easy preparation and scale-up.
• High retention of hydrophobic drugs.
• Controlled particle size.
• Extended release of encapsulated drug after a single injection.
• Static interface facilitates surface modification of carrier particles after lipid matrix.

Customized Lipospheres Drug Delivery Formulation

CD Formulation provides customization services for liposphere drug delivery formulations, including regulation of drug and excipient formulation, content, and ratio to obtain the target drug delivery lipospheres.

• Size Analysis

Particle size and particle size distribution studies can be performed using Coulter counter methods to correlate particle size and drug release from lipospheres. The morphology of lipid spheres is characterized by transmission electron microscopy, where the interaction of electrons with the lipid surface produces images, and SEM characterizes the jumping of electrons with the particle surface to produce images.

• In vitro evaluation

The encapsulation rate is defined as the drug encapsulated in the lipid-based particles, relative to the total amount of drug added, i.e., the percentage of drug contained in the particles versus the percentage of drug remaining in the dispersion medium. The loading capacity (LC) is the percentage of drug incorporated into the lipid particles relative to the total weight of the lipid phase (drug + lipid). LC is an important parameter for characterization and optimization of lipid-based drug carriers depends mainly on the solubility of the drug under study in the core lipid/lipid mixture, miscibility of the drug melt and lipid melt, chemical and physical properties of the SLM and polycrystalline state of the lipid.

• In vivo evaluation

The efficiency of target/site-specific delivery of lipid sphere systems is supported by in vivo studies. CD Formulation provides in vivo evaluation of loaded drug lipid spheres.

Applications of Lipospheres

1) Parenteral route

Lipospheres can be used for delivery of anesthetics, parenteral delivery of antibiotics, and parenteral administration of vaccines and adjuvants.

2) Oral drug delivery

Several classes of drugs such as antibiotics, anti-inflammatory compounds, vasodilators, anticancer agents, proteins and peptides are being formulated as oral lipospheres.

Reference

1. Ma, T., et al. (2014) PLGA - lipid liposphere as a promising platform for oral delivery of proteins. Colloids and Surfaces B: Biointerfaces, 117, 512-519.