Producing Nano-particles for formulation: the alternative approach
Formulation issues might hamper the therapeutic possibilities of Active Pharmaceutical Ingredients and their commercial success.
Several traditional approaches have been developed to create nano-particles, with different degrees of success. Using Carbon Dioxide as an alternative for organic solvents typically used to make nano-particles opens a new world of possibilities.
Solvent free nano-particles can be processed further to achieve the optimal bio-availability profile.
Pharmacokinetics, bioavailability and the interaction of pharmaceuticals are important features in drug formulation and dosage determination. It is estimated that 40 to 60% of newly discovered Active Ingredients are difficult to formulate as a result of their lack of significant solubility in water. Drug formulation can crucially influence pharmaceutical properties, potentially preventing an effective drug to enter the market if the drug cannot reach its target.
To increase bioavailability of the API, formation of nano-particles as a drug-delivery approach has been a viable option. Nano-particles can be designed to form de novo when exposed to the appropriate solvent or the Active is combined with selected excipients. The thought behind the formation of nano-particles is to increase the particle’s surface area and thereby to enhance the dissolution rate.
Using solvents in the process of producing nano sized particles introduces process steps which complicate production of the API. Furthermore they are often difficult to remove, leaving a residue in the final product. A novel alternative solubilization technology for producing nano-particles is using supercritical fluid (SCF) processes. Under pressure and (ambient) temperature, gas (for example Carbon Dioxide) exhibits fluid-like properties in which Actives can be dissolved. Solubility is influenced by pressure and temperature, resulting in an easily tunable process that caters to the needs of the specific API. Once the drug particles are solubilized within SCF, they may be recrystallized at greatly reduced particle sizes. The flexibility and precision offered by SCF processes allows micro- or nanonization of drug particles in a predictable and controlled manner, thus limiting the need for further manipulation. Operational benefits include ambient temperature processing, absence of solvent residues in products, the near elimination of waste streams and easy recycling of solvents.
Creating nano-particles is an important step towards achieving the desired bioavailability profile. Once a nano-particulate platform is established, further particle design can be applied through encapsulation. This technology will be described in a following article.
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