FORMULATION DEVELOPMENT FOR POORLY SOLUBLE DRUGS

Ascendia specializes in the development of market suitable formulations for poorly water soluble drug substances. Based on the pre-formulation data package and the delivery requirements for the product, we recommend a comprehensive formulation development strategy. We understand that each formulation is unique and must address the specific challenges associated with poor solubility, inadequate bioavailability, and/or unacceptable physical/chemical stability. We also understand the urgency companies have for progressing their pipeline, and our approach maximizes the probability of success by exploring multiple formulation options in parallel if necessary.

Our experienced formulation development team can overcome these issues. Our services will provide you with a formulation that you can be confident will be suitable for clinical scale-up. Ascendia provides these expert contract formulation development services rapidly and cost-effectively - let us help bring your molecule to market.

Oral Formulations

We develop and evaluate oral formulations for preclinical and early human studies. In addition to traditional granulation approaches, we offer a wide range of advanced technologies for your drug delivery challenges.

Our nano-emulsion formulations are prepared by high shear homogenization and then incorporated into either solid or liquid dosage forms.

Our amorphous solid dispersions can be processed by hot-melt extrusion, solvent evaporation, or spray drying, and then granulated and tableted.

Our nano-particle formulations are prepared by bead-milling, microfluidization, or homogenization, and then incorporated into a solid dosage form.

Our controlled-release formulations can provide enteric protection, colon targeting, sustained release with pH-independence, pulsed release or combinations thereof. Dosage forms can be either a capsule or tablet.
 

Parenteral Formulations

We develop and evaluate parenteral formulations for preclinical and early human studies. There are a couple of key considerations for the development of a parenteral pharmaceutical product: the administration route (intravenous, intramuscular, or subcutaneous) and the requirement for a sterile, pyrogen-free dosage form.

During development, the formulation is optimized via pH adjustments, co-solvents, complexation, surfactants and combinations of these methods. Different dosage-form concepts can be developed: solutions, suspensions, emulsions, or a lyophilized powder for reconstitution (if stability is an issue).

Topical Formulations

We design and evaluate topical formulations for administration to the skin or eye. There are a number of factors that must be considered during the development of a topical pharmaceutical product: viscosity, taste, ease-of-administration, skin sensitivity, and color to name a few. In particular, for ocular delivery, a formulation must not irritate the eye, and transparent drops are a key benefit.

ASD-004: OPHTHALMIC NANO-EMULSION CASE STUDY

ASD-004 is an ophthalmic drop formulation of cyclosporine intended for treatment of dry eye syndrome. Unlike the current marketed product (Restasis®),

ASD-004 is an optically clear nano-emulsion (see photo below).





Optically Clear Nano-Emulsion
Relative Droplet Size of ASD-004 Nano-Emulsion vs. Restasis


The droplet size of the ASD-004 nano-emulsion is approximately 40nm compared to the 100-200 nm of the Restasis formulation. This reduced particle size may enhance drug bioavailability in the eye tissue and thus improve efficacy. An optically clear product is preferred to prevent transient blurring of vision following administration of the drop. In addition, the ASD-004 formulation contains minimal surfactant and solvent, and has the potential to demonstrate reduced eye irritation - a frequent complaint.
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