Ondansetron Loaded pectin based microspheres for nasal administration: invitro and in vivo studies.
Hitenda S. Mahajan, Bhushankumar V. Tatiya, Pankaj P. Nerkar
Ondansteron is one of anti emetic drugs that is act selectively antagonist on 5-HT3 receptor in the central nervous system, it is used for preventing nausea and vomiting caused by chemotherapy. The main problem of this drug is under go first pass effect during first pass in liver about 40% of the drug metabolite, and after oral administration it will take time for the drug to reach therapeutic level and action, that is why preparation of ondansteron microspheres for nasal delivery solve this problems and give us the rapid onset of action, self administration and by pass first pass effect.
In this article, pectin use as natural substance for carrying ondansteron , and they were prepared as ondansteron loaded microspheres, moreover pectin enhance the residence time of the drug with in nasal cavity which may lead to enhance absorption, it has the ability to absorb water and swell, it make the viscous polymer with in nasal so lead to decrease mucociliary clearance which is the main problem in nasal drug delivery.
Ondansteron load microspheres were prepared by spray drying technique in three different drugs to polymer ratio. Their objective of this study was to examine the influence of formulation and variable process on the characteristic of the microspheres prepared. The effects of various experimental parameters were evaluated such as drug to polymer ratio, rate of feeding solution on the particle size and entrapment efficiency. The drug loading was between 23 and 29% and the drug loading is inversely related with polymer concentration and decrease with increasing drug to polymer ratio. The swelling properties of the microspheres showed increase with increasing the ration of polymer to the drug and vice versa, while the free and drug loaded microspheres had negative surface charge ( – 55 to 57), for confirming the adhesion of pectin to the mucous, mucoadhesion test carried out and the results showed that pectin can adhere to the mucous membrane and the percentage of mucoadhesion as the ratio of pectin was increased. The scanning electron microscopy used for morphological study and it showed the particles had smooth surface, while X-ray spectra confirmed that the drug molecularly dispersed in the polymer and conversion of the crystalline form of the drug into amorphous form after spray drying was determined by absence of crystalline peaks of ondansteron. Histo-pathological study showed no any histological change observed.
Over all the spray drying technique is the suitable technique for preparation of ondansteron loaded pectin microspheres, with desirable characterization and it can be used intranasally for preventing nausea and vomiting during anti cancer administration.