For a drug to have a therapeutic effect, it has to reach its site of action in sufficient quantities. The Pheroid drug delivery system enhances the absorption of drugs in various pharmacological categories and is the focus of this study. A number of patents are registered in various countries to protect its application. Pheroid technology is trademarked, but may for ease of reading, be called Pheroid(s) only. The Pheroid itself is composed of an organic carbon backbone composed of unsaturated fatty acids with some side-chain interactions that result in self-emulsifying characteristics. The resulting vesicles and nano-sponges can entrap hydrophilic, hydrophobic or amphiphilic compounds for biomedical and agricultural application and can be manipulated as to loading ability, mechanical resistance, permeability, size and solubility. Pheroid was investigated for its potential use in the areas of vaccines, peptide drugs, topical products and cosmeceuticals, antimicrobial treatments and agriculture. In all of these areas, the Pheroid has indeed shown applicability: the results showed improved uptake and/or efficacy of the entrapped chemical or biological compounds after administration by a number of administration routes. For oral administration, a precursor format, the pro-Pheroid, was used, wherein the vesicles and/or sponges are formed post-administration. Proof of concept studies on the in vivo absorption and bioavailability, as well as studies on in vitro efficacy of Pheroid-based formulations were carried out for antimicrobials, such as tuberculosis drugs, antimalarials and antiretrovirals. In all cases, the in vitro efficacy of the active compounds was increased, compared to well-known standard drug treatments. In a phase I bio-equivalence study, a Pheroid-containing combination formulation was compared against the comparative market leader. The results demonstrated that the bioavailability of the active compounds in the Pheroid was at least as good but mostly significantly better than that of the comparative medication. In addition, the incidence of side-effects was decreased in the case of the Pheroid formulations. Furthermore, in vitro results indicate that drug resistance can at least partially be negated. Pheroid technology may also be capable of protecting labile drugs such as peptides against degradation and increasing efficacy so that lower dosages can be administered less frequently and with fewer side effects. Based on in vitro and in vivo results, a number of products are currently in development. The application of Pheroid technology is potentially limitless and includes such areas as TB, malaria, cancer, AIDS, gene delivery, vaccines, patented medicines and generics and agriculture. / Thesis (Ph.D. (Pharmaceutics))--North-West University, Potchefstroom Campus, 2010.
| Identifer | oai:union.ndltd.org:netd.ac.za/oai:union.ndltd.org:nwu/oai:dspace.nwu.ac.za:10394/6701 |
| Date | January 2009 |
| Creators | Grobler, Anne Frederica |
| Publisher | North-West University |
| Source Sets | South African National ETD Portal |
| Detected Language | English |
| Type | Thesis |
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