Mucoadhesive

Chitosan based microspheres containing were prepared by the emulsion cross linking method for nasal delivery of zolmitriptan. Nasal microspheres offer significant advantages over other type of drug delivery system. It modulates absorption characteristics of the drug by enhancing drug residence time in the nasal cavity and subsequently may increase bioavailability profile of administered drug. For the present study, Chitosan was selected as a mucoadhesive polymer. The microspheres were evaluated with respect to the particle size, production yield, encapsulation efficiency, shape and surface properties, drug and polymer interaction, mucoadhesive property, in vitro drug release. To optimize the microsphere formulation, 23factorial design was employed for investigating the effect of three factors, polymer concentration (chitosan), emulsifier concentration (Span 80) and cross-linking agent (gluteraldehyde) on response variable, which are encapsulation efficiency, in vitro drug release.

The present study involves the formulation and evaluation of buccal tablets of Pravastatin, an antihyperlipidemic drug which has high first pass metabolism, So buccal drug delivery has been considered an alternative to the oral dosing for compound subjected to degradation in the gastrointestinal tract or to first pass metabolism. An attempt has been made to developed mucoadhesive buccal tablets comprising of drug containing mucoadhesive layers and drug free backing layer ethyl cellulose of to release the drug for extended period of time with reduction in dosing frequency, dose related side effects and improve bioavailability of drug. Tablets of Pravastatin were prepared by direct compression using mucoadhesive polymers Carbopol 943-P HPMC K4M and Sodium CMC. Buccal tablets were evaluated by different parameters such as thickness, hardness, weight uniformity, content uniformity, swelling index, surface pH,  bioadhesive strength, in vitro drug release, ex vivo drug permeation and FTIR studies. The modified in vitro assembly was used to measure the bioadhesive strength of tablets with fresh goat buccal mucosa as model tissue. In order to determine the mode of release, the data was subjected to Krosmeyer and Peppas diffusion model. All the formulations followed Fickian release mechanism. Tablet containing Carbopol 934P & Na CMC in the ratio of 1:1 had maximum in vitro drug release for 6 hrs.

The nasal route has gained importance in recent decades as a non-invasive drug application route that offers many advantages for the introduction of drugs into systemic circulation. Its major advantage is the rapid absorption of drugs and therefore quick onset of their effect. In addition, it has the advantage of avoiding the hepatic first-pass effect. Thus, nasal drug delivery may be used for either local or systemic effects. Cancer induced nausea and vomiting is one of the major side effects of the cancer chemotherapy. For the treatment of the CINV the use 5HT3 recepter antagonist is the most effective. Ondansetron has a oral bioavailability of 60% due to the first pass metabolism. So our objective was to prepare an in situ nasal gel of the Ondansetron using PF-127 as the thermo reversible polymer. There are many approaches for increasing the residence time of drug formulations in the nasal cavity resulting in enhanced drug absorption. We used HPMC E15 and Chitosan as the mucoadhesive polymer to increase the nasal residence time of the formulation. To increase the permeation we used Polyethylene Glycol 400 and Propylene glycol as the permeation enhancer. Further,  a 3-factor, 2-level full factorial design (23) study was carried out to optimize the Ondansetron gel with PF 127 amount (%, X1), permeation enhancers (PEG 400 1%/PPG 1%, X2) and polymers (HPMC E15 1 %/Chitosan 0.5 %, X3) as the prime selected independent variables, which were varied at 2 different levels (low and high). The effect of formulation variables on the response variables were statistically evaluated by using a commercially available software package Design-Expert® version 8.0 (Stat-Ease, Inc.).The formulation Om2 was found to be the best composition formula based on statistical finding, while conformation experiment also proves this result.