pH-responsive release system of topiramate transported on silica nanoparticles by melting method

Abstract

Incorporating drugs into silica matrices by the melting method can be applied to obtain drug delivery systems because they are governed by electrostatic type interactions, hydrogen bonding and hydrophilic-hydrophobic interactions between the drug and the silica surface. the melting method is an environmentally correct tool since it is free of organic solvent, low cost and with easy execution for the incorporation of drugs in silicas. Drugs delivery systems are very important for improving the treatment of chronic diseases. Topiramate (TPM) is a potent antiepileptic used in high daily doses as it has low bioavailability. In this context, silica nanoparticles (NPS) were used as an inorganic matrix for TPM transport in (in vitro) release studies. The TPM was incorporated into the NPS by hot melt loading employing a new carrier preparation methodology (NPS/TPM) using a thermobalance (by Thermogravimetry-TG) with high temperature control system. The release study using dissolution media simulating gastrointestinal at pH 1.2 (stomach) and 7.4 (intestine), showed that NPS release TPM in a prolonged and pH-responsive manner. The drug was released at intestinal pH ensuring greater absorption, allowing fewer daily doses and less adverse effects. The kinetic study demonstrated the best fit to the zero-order model proving the pH-responsive profile of the developed system.

Keywords:

• Epilepsy
• topiramate
• drug delivery system
• pH-responsive system
• silica nanoparticles
• expanded perlite
• hot melting method
• thermogravimetry
• solid dispersion
• GC-MS

Disclosure statement

The authors declare that they have no conflicts of interest.

Additional information

Funding

To CAPES for the financial support. To Petrobras, IQ-UFRN, LASID-UFRN and LABPEMOL-UFRN for the instrumental support. At NUPPRAR-UFRN, NUPLAM-UFRN, EMS Pharma and Prof. Carlos Alberto Martinez Huitle for the supply of inputs. Elmar Damasceno Júnior (IQ-UFRN) by the figures and illustrations.