In some specific fields of application (e.g., cosmetics, pharmacy), textile substrates need to incorporate sensible molecules (active principles) that can be affected if they are sprayed freely on the surface of fabrics. The effect is not controlled and sometimes this application is consequently neglected. Microencapsulation and functionalization using biocompatible vehicles and polymers has recently been demonstrated as an interesting way to avoid these problems. The use of defined structures (polymers) that protect the active principle allows controlled drug delivery and regulation of the dosing in every specific case. Many authors have studied the use of three different methodologies to incorporate active principles into textile substrates, and assessed their quantitative behavior. Citronella oil, as a natural insect repellent, has been vehicularized with two different protective substances; cyclodextrine (CD), which forms complexes with it, and microcapsules of gelatin-arabic gum. The retention capability of the complexes and microcapsules has been assessed using an in vitro experiment. Structural characteristics have been evaluated using thermogravimetric methods and microscopy. The results show very interesting long-term capability of dosing and promising applications for home use and on clothes in environmental conditions with the need to fight against insects. Ethyl hexyl methoxycinnamate (EHMC) and gallic acid (GA) have both been vehicularized using two liposomic-based structures: Internal wool lipids (IWL) and phosphatidylcholine (PC). They were applied on polyamide and cotton substrates and the delivery assessed. The amount of active principle in the different layers of skin was determined in vitro using a Franz-cell diffusion chamber. The results show many new possibilities for application in skin therapeutics. Biofunctional devices with controlled functionality can be built using textile substrates and vehicles. As has been demonstrated, their behavior can be assessed using in vitro methods that make extrapolation to their final applications possible