For decades, scientists have pursued the production of nanoparticles to enhance the bioavailability and stability of drugs and cosmeceuticals. Owing to their vanishingly small particle sizes, so-called “nanomedicines” possess significantly higher dissolution rates than their macro analogues. This characteristic is especially desirable when the molecule in question suffers from poor water solubility. In recent years, drug and cosmetics manufacturers have worked to develop drug-delivery vehicles that can overcome many of the challenges related to stability, targeted delivery and bioavailability.
Nanoparticles are characterized by at least one dimension of 100 nm or less. They represent a link between the macro- and micro-scale worlds; straddling the shadowy realm between bulk objects and molecular or even atomic-scale structures. This proximity to the atomic scale accounts for some of the unique physiochemical properties of these nanostructures. By harnessing these properties, it’s possible to significantly enhance the delivery, efficacy, stability and even dosing of active pharmaceutical ingredients (APIs).
Case Study: Topical Delivery of CoQ10
For example, consider the topical delivery of the potent natural antioxidant molecule, coenzyme Q10 (CoQ10), which boosts cellular energy production. Present in virtually every cell in the body, this mitochondrial coenzyme is desirable for use in cosmeceutical formulations, as CoQ10 has been shown to penetrate the epidermis and reach the deep layers of the epidermis and dermis, where it helps combat aging and its effects at the cellular level.
CoQ10’s lipid solubility makes it especially desirable for topical antioxidant use. Water-soluble antioxidants are far less adept at crossing cells’ lipid bilayers to gain entry into the cytoplasm. Since oxidative stress occurs largely within cells, this ability to penetrate into cells is key. Levels of naturally produced CoQ10 (also known as ubiquinone) decline with age. Replenishment of this crucial antioxidant is highly desirable, therefore. Research has shown that topical application of suitably formulated CoQ10 results in “significant augmentation of energy metabolism,” a decline in potentially damaging free radicals, and an increase in antioxidant capacity.
Various methodologies have been explored for achieving nanoparticles suitable for use in the emerging and rapidly evolving field of nanomedicine. One popular solution involves the nanoencapsulation of nanoparticles in lipids, polymers or lipid bilayers. Nanostructured lipid carriers (NLCs) of about 230 nm have been shown to enhance delivery compared to equally sized nanoemulsions. More recently, ultra-small NLCs with particle sizes of about 80 nm were shown to further enhance delivery. Skin permeation and penetration increased, as did the physiochemical stability of the NLC.
Enhanced Oral Dosage Delivery
Of course, nanotechnology is also useful for the enhancement of oral drug delivery and performance. BioMed Research International details the development of an oral CoQ10 supplement with significantly enhanced bioavailability. CoQ10 is poorly absorbed from the gut, so enhancing bioavailability has been a long-term goal for nutraceutical manufacturers. Using “hot” high-pressure homogenizer technology, they formulated a lipid-free nano-CoQ10 system modified with surfactants to achieve “significantly improved CoQ10 bioavailability.”
Of course, the successful production of solid lipid nanoparticles depends on the ability to produce extremely tight particle size distributions in the target range. The high shear forces generated by the proprietary fixed-geometry interaction chamber at the heart of every Microfluidics high-pressure homogenizer deliver superior particle size reductions, under temperature controlled conditions, which helps eliminate API degradation, loss and uncertain lipid transitions.
For more information about our groundbreaking Microfluidizer® technology, contact Microfluidics today.