Nasal Mucoadhesive In Situ Gel of Granisetron Hydrochloride using Natural Polymers

Abstract

The prolonged residence of drug formulation in the nasal cavity is of utmost importance for intranasal delivery of drug. Present investigation was aimed to develop a mucoadhesive in situ gel of Granisetron hydrochloride (GH) with reduced nasal mucocilliary clearance in order to improve the bioavailability of the antiemetic drug, granisetron hydrochloride. The in situ gelation upon contact with nasal mucosa was conferred via the use of the thermogelling Pluronic flake 127 (PF 127). Moringa gum (MG), carboxymethyl tamarind gum (CMTG) and sodium alginate (SA) was used to modulate mucoadhesion whereas drug release of optimized formulation was modified by 0.3% polyethylene glycol 6000 (PEG 6000). Results revealed that as the concentration of mucoadhesive polymer increased the mucoadhesive strength increased and gelation temperature decreased significantly. Preformulation studies showed that addition of GH in 18% PF 127 gels modulated gelation temperature significantly while mucoadhesive polymers alters mucoadhesion. Formulation F6, F11 and F15 showed more than 80% of drug diffusion at 240 min. Gelation temperature and mucoadhesive strength of all three formulations were found in the range of 30-31 C and 963.66±9.60 to 991.33±10.26 dyne/cm 2 respectively. Formulation F11 showed optimum results and further histopathological evaluation reveled formulation is safe for use. Addition of PEG 6000 increased drug diffusion in formulation F11 with flux 0.034 mg.cm 2 /min. This study concluded the potential use of CMTG as mucoadhesive in situ nasal gel in terms of ease of administration, accuracy of dosing, prolonged nasal residence and improved nasal bioavailability.

Citric Acid Crosslinked Carboxymethyl Cellulose-based Composite Hydrogel Films for Drug Delivery

“…TG is composed of (1→4)-β-D-glucan back-bone substituted with side chains of α-D-xylopyranose and β-D-galactopyranosyl(1→2)-α-D-xylopyranose linked (1→6) to glucose residues [20] . It has been used in the development of various drug delivery systems due to its hydrophilic and bioadhesive properties [21][22][23][24][25][26][27] . Although TG shows presence of non-sterically hindered hydroxyl groups, very few reports mentioned the use of pure TG in chemically crosslinked hydrogels [28] .…”

Formulation and Evaluation of Mucoadhesive Microbeads of Domperidone.

“…The results also showed that increase in concentration of crosslinking agent decreases the percentage mucoadhesion; the reason may be attributed to less availability of polymer chains for entanglement with the mucus. In vitro drug release study It was observed that formulation C1 shows only 37.18 % at the end of 8 hrs which contains pure drug which indicates drug molecules presenting difficulties in their solubility in dissolution medium [17].It was observed that formulation C5 showed more drug release than formulation C4 and C3, thus it was found from result that with the increasing concentration of DOM solid dispersion in formulation, % drug release also get increased.…”

“…The microbeads are more spherical in shape before solid dispersion loading. The drug loading and solid dispersion loading lead to formation of irregular microbeads with rough surface which may provide higher specific surface area [17]. SEM of the surface of sectioned solid dispersion loaded microbeads shows that many large pores are present in the gel matrix may be due to contraction of gel matrix caused by water evaporation is depressed by the presence of carbopol [4].…”

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“…The formulation has the advantage to prevent the anterior leakage of the dosage form and enhance the nasal bioavailability due to longer residence time in the nasal cavity. For better patient compliance, it is desirable to deliver the drug quickly through the nasal mucosa because it is difficult to hold the gel in the nasal cavity for more than 7-8 h. So, we have used the permeation enhancer 4,5,6 .…”