Mucoadhesive

The aim of the proposed work was to develop stable mucoadhesive in situ (Phenylepherine HCL) thermo-reversible nasal gel by cold technique and evaluated its efficacy against congestion due to allergic rhinitis. By means of hit and trial methodology screened formulations were prepare via numerous thermo-sensitive hydro-Gel (Pluronic F-127, Poloxamer 407) and muco-adhesives (Carbopol 934-P, Polyvinylpyrrolidone K-30, Hydroxy propyl methyl cellulose (HPMC), Sodium alginate and methylcellulose) and characterized. Out of 15 formulations; T1, T5, T7, T12 & T14 formulation compositions were selected on the basis of drug released (in-vitro or ex-vivo release found approx. up-to 97.8%) behavior, gelation and mucoadhesive strength. Resulted, drug transformed (crystalline to amorphous) form in gel state was indicated better drug absorption due to its improved physicochemical parameters. Additionally, optimized formulation (T1) histopathology and stability studied has been demonstrated none nasal mucosa damage and stable at storage conditions according to the ICH guidelines respectively. Therefore, the developed optimized thermo-reversible in-situ nasal (T1) gel was showed tremendous local safety action which can be considered to use for allergic nasal congestion and explore, further.

The purpose of this study was selection of most influential variable for the preparation of prolonged release nanoparticulate formulation by desolvation method for diltiazem hydrochloride with bioadhesive polymer gelatin. Formulation and processing variables which effect various response variables were studied by a Taguchi design. Independent variables studied were the amount of polymer, amount of glutaraldehyde, amount of Poloxamer 237, acetone addition rate, pH, stirring time and stirring speed. The dependent variables considered were the particle size, polydispersity index, amount of drug released in 6 h, time required to release 60 % of drug, mucoadhesiveness, entrapment efficiency and loading efficiency. Pareto charts showed that the two significant factors affecting the response variables were amount of glutaraldehyde and amount of polymer.

The objectives of this study were to maximize; a) the in vitro transcorneal release, b) the IOP-lowering effect and, c) the duration of action, of Latanoprost acid (LAT) ophthalmic gels. The in vitro transcorneal release of LAT from a 1st set of gel formulations that containing different concentrations of Azone™ (as enhancer) with fixed concentration of C-974® (as mucoadhesive) were studied. Formulation that showed greatest permeability parameters at lowest Azone™ concentration was selected for preparation of a 2nd set of ocular gels containing various C-974® concentrations. The in vitro transcorneal release was assessed, and the best C-974® concentration required for preparation of formulations that can be conceded as ideal ophthalmic LAT gels hve been pinpointed and scaled up for in vivo IOP-lowering efficacy study using TONO-PEN™ AVIA tonometer in rabbits for 4-consecutive days.  Various test formulations have showed significant but varied augmentations in both, in vitro and in vivo results. Formulations (GAZ-4) & GC-4 have shown the highest therapeutic IOP lowering effects; i.e., (7.8±1.8), (6.5±2.1), respectively. Particularly noteworthy with both formulations the IOP base-line didn’t re-established after 24 hours, and their durations of action in the single-dose study were 47±2.25, and 48±1.5, respectively. The in vitro release, onset, magnitude & duration of action of action of LAT gels have been enhanced and extended for up to 2-day with two gel formulations.  Nonetheless, the success in developing a novel ophthalmic formulation depended for great extent upon the crucial net outcomes of a very sensitive interplay/balance between the drug and additives.

The Losartan Potassium buccal tablets have been developed as controlled drug delivery systems to improve the efficacy of Losartan Potassium through mucosal absorption, reduce dose frequency, toxicity, to improve bioavailability and patient compliance. Many processing variables can persuade the characteristics of the Losartan Potassium buccal tablets. The aim of the study was to study the effect of some selected process variables in the concentration of drug/locust bean gum, hydroxy propyl methyl cellulose K4M on the hardness, mucoadhesive strength and in-vitro release at different hours by applying central composite design, accounting the above independent variables. The central composite design with an R2 value of 0.9695, 0.9928, 0.5839, and 0.7556 has selected as a suitable model for further analysis. The model F value of 44.52, 277.61, 7.02, 15.46 with probability P>F

Mucoadhesive dosage forms may be designed to enable prolonged retention at the site of application, providing a controlled rate of drug release for better therapeutic results. Mucoadhesive drug delivery systems are used to prolong the residence time of the dosage form at the site of application or absorption and to facilitate intimate contact of the dosage form with the underlying absorption surface to improve and enhance the bioavailability of drug. Some of the promising plymers that have been commonly used in these systems include polycarbophil, carbopol, lectins, chitosan, carboxymethylcellulose, pectin, carragenan, alginic acid, polylysine, polybrene, polyethylene glycol, polyvinyl pyrrolidone , dextran etc. Now  scientists are developing mucoadhesive micro and nanoparticulate systems by using  novel mucoadhesive polymers for better therapeutic results and site specific targeting with lesser side effects. Improvements in mucoadhesive based oral delivery and, in particular, the development of novel, highly-effective and mucosa-compatible polymers, are creating new commercial and clinical opportunities for delivery of narrow absorption window drugs at the target site to maximize their efficacy. This review is an effort to provide information on such mucoadhesive drug delivery systems that are developed for oral, buccal, nasal, rectal and vaginal routes for both systemic and local effect.