Solubility Improvement and Bioavailability Enhancement

Poor water solubility and low bioavailability are two of the most common challenges in drug product development today. Over half of marketed APIs suffer from solubility challenges, and as many as 90% of new drug candidates will pose the same problems for formulators.

At LLS Health, we know that formulating BCS Class II and IV compounds is not one-size-fits-all. That is why we employ a range of techniques to achieve your goals. We are a full-service partner, offering formulation, manufacturing, and analytical support services for a range of dosage forms.

API Physical Modification Services

Nanomilling

A process by which the particle size of an API is reduced in a liquid vehicle (typically aqueous) via grinding using polymeric or ceramic beads to increase dissolution rate. This technique is also referred to as high energy media milling.

Learn more about Nanomilling services.

Micronization

Another particle size reduction technique that commonly uses pressurized air (jet milling) to achieve micron-scale particles with higher dissolution rates.

Co-Crystals

A technique where API molecules and co-crystal formers (AKA co-formers) form a single crystal lattice with higher solubility than the individual components.

Amorphous Solutions and Dispersions

A technique where API particles are dispersed in an excipient (via hot melt extrusion or spray drying) to stabilize the API in an amorphous state, leading to higher solubility.

API Chemical Modification Services

pH Modification

A technique where the solubility of ionizable APIs is increased through the addition of acidic of basic excipients to a formulation.

Salt Formation

A process where the salt form of an ionizable API is formed by coupling the API with a counterion and crystallization solvents. Salt forms often exhibit higher solubility.

PEGylation

A technique where polyethylene glycol (PEG) is covalently or non-covalently bound to the surface of a large molecule, small molecule, or liposomal carrier, improving solubility and half-life of an API.

PEGPLUS™ Technology

A proprietary, multifunctional excipient technology offered by LLS Health. PEGPLUS Technology improves adherence to mucous membranes, leading to increased bioavailability and protection/stabilization of APIs.

Learn more about PEGPLUS™ Technology.

Encapsulation Techniques

Micelles

Structures comprised of surfactants, which are amphiphilic compounds with a hydrophobic tail and hydrophilic head. Micelles are typically spherical and consist of a hydrophobic core for solubilizing API and a hydrophilic outer surface which faces the surrounding aqueous environment.

Liposomes

Structures comprised of one or more phospholipid bi-layers. Liposomes are typically spherical and are used to encapsulate water-soluble APIs in the core, oil-soluble APIs in the bilayer membrane(s), and, if made of cationic phospholipids, trap and deliver oligonucleotides for gene therapy.

LyoCell® Technology

A patented, proprietary drug delivery technology offered by LLS Health that is based on the use of reverse cubic phase lyotropic liquid crystals. LyoCells consist of nanoparticles containing both lipidic and aqueous regions, meaning they can solubilize a wide range of small and large molecule APIs.

Learn more about LyoCell® Technology.

Solid-Lipid Nanoparticles

Nano-scale particles comprised of lipidic materials (usually phospholipids, triglycerides, and natural waxes) which can solubilize a wide range of small and large molecule APIs.

Learn more about Solid-Lipid Nanoparticles.

Polymer Encapsulation

Micron-scale particles comprised of a bioresorbable polymer (typically PLGA) and an API. These particles are typically developed as microspheres for long-acting injectables.

Learn more about Polymer Encapsulation.

Inclusion Complexes

β-cyclodextrins

Torus-shaped structures with a hydrophilic outer surface and a hollow, hydrophobic core where poorly water-soluble APIs are entrapped and carried to their site of action.

Serum Albumin

A biocompatible, naturally-occurring protein which is complexed with APIs to form bioresorbable nanoparticles with improved dissolution rates.