Evaluation of the oral delivery of a peptide with Pheroid® technology

Abstract

Goserelin is a type of hormone therapy used in addition to standard adjuvant therapy. Currently, goserelin is only available as a slow releasing subcutaneous implant but this is an invasive and generally not well- tolerated method of administration. By using a drug delivery system (DDS), peptides can be protected from the harsh environment of the gastrointestinal (GI) tract. Pheroid® technology is one such example of a drug delivery system. This delivery system is a patented, colloidal drug delivery system and is capable of targeting specific areas for treatment, transportation of genetic material to the cellular nucleus and the decrease of drug resistance, all this while improving the delivery of dynamic complexes [1,2]. The prospect of changing to a less invasive administration method will yield a great advantage. Goserelin was investigated in female Balb/c mice. Pheroid® technology was used as a drug delivery system (DDS) to compare the bioavailability of goserelin subcutaneous depot against a peroral formulation with goserelin pro-Pheroid® formulation. The mice were divided into three groups; group one received goserelin subcutaneously, group 2 received an oral dose of 4 mg/kg pro-Pheroid®-goserelin and group 3 being the control group which received only pro- Pheroid®. Vaginal cytology was evaluated to track the disruption of the oestrus cycle Vaginal cytology results indicated a disruption in the oestrus cycle in the subcutaneous groups and the pro- Pheroid®-goserelin oral group. No disruption in the cycle was observed for the pro-Pheroid® oral group. Entrapment in Pheroid® resulted in oral bioavailability of goserelin as indicated by the related effect on the oestrus cycle. No disruption of the cycle was observed in the pro-pheroid® oral group, thus, goserelin was successfully absorbed in the blood after the peroral administration with pro-Pheroid. In conclusion, Pheroid® technology seemed to protect goserelin from the harsh environment of the gastrointestinal tract and could thus be a helpful DDS