Objective: The aim of present investigation was to prepare liquisolid compacts of high dose water insoluble drug, carbamazepine (CBZ) using novel porous carriers such as Neusilin and Fujicalin in order to improve its dissolution rate and reduce the tablet weight. Materials and Methods: Solubility of CBZ was determined in different non volatile solvents to finalise vehicle having maximum solubility. The liquid retention potential (ф) of carriers and coating material was determined and 18 different liquisolid compacts of CBZ were formulated. The prepared liquisolid compacts were evaluated and compared for thickness, diameter, weight variation, uniformity of content, hardness, friability, disintegration and in vitro dissolution. Dissolution profile of liquisolid compacts was compared with marketed tablet formulation. Results and Discussion: The solubility of CBZ in polyethylene glycol 200 was found to be greater than the other solvents. Neusilin showed higher ф value than traditional carriers. Formulated liquisolid compacts showed all physical parameters within prescribed limit. Formulation containing Neusilin-Neusilin and Neusilin-Aerosil showed no disintegration while all other formulations showed disintegration up to 180 seconds. All the formulations showed drug release above 80% at the end of 15 minutes except marketed formulation. The weight of formulations containing Neusilin and Fujicalin ranged in between 0.383-0.947g. Formulation FA3 containing Fujicalin exhibited lower mean dissolution time and higher dissolution efficiency than all other formulations including marketed tablet. Conclusion: It can be concluded from this study that novel porous carriers are superior to traditional carriers in liquisolid systems and are suitable for loading high dose drugs like CBZ.
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.
The aim of present investigation was to characterize carboxymethyl tamarind gum (CMTG) based interpenetrating networks (IPNs) of aceclofenac for site specific sustained delivery. The drug loaded IPNs were prepared by using chitosan and CMTG as polymers and gluteraldehyde as crosslinking agent. The IPNs were characterized by Attenuated total reflectanceFourier transform infrared (ATR-FTIR) spectroscopy, thermal analysis, X-ray powder diffraction and solid state 13 C-nuclear magnetic resonance spectroscopy. The prepared IPNs were evaluated for the drug entrapment efficiency and equilibrium swelling. The drug release from IPNs was studied in 0.1NHCl for 2h followed by phosphate buffer pH 6.8 for further 10h and compared with commercial tablet. The results of ATR-FTIR and thermal analysis for blank IPNs indicated intercalation of polymeric chains of crosslinked CMTG and chitosan. The results of solid state characterization revealed that the aceclofenac is compatible with IPNs. Entrapment efficiency of IPNs was found to be increased with increase in crosslinker concentration as well as amount of CMTG. The equilibrium swelling study indicated pH dependent swelling of IPNs. The drug release by IPNs showed sustained release of aceclofenac upto 12h while commercial formulation showed fast release within 8h. From the results, it can be concluded that the IPNs of CMTG and chitosan has potential in development of site specific sustained drug delivery.
The present investigation aims at developing novel injectable in-situ gel containing ornidazole (ORDZ) loaded chitosan microspheres for treatment of periodontal disease. Microspheres were prepared by emulsificationionotropic gelation method. Prepared microspheres were evaluated extensively for particle size, equilibrium swelling studies, bioadhesion, percentage drug release and antimicrobial activity. The mean diameter of the microspheres was found in the range of 29.1-52.65 µm. The microspheres showed good swelling properties. Percentage equilibrium swelling was dependent upon the amount of chitosan. The in vitro drug release and bioadhesion studies were dependent on the extent of crosslinking and chitosan concentration. The ORDZloaded microspheres showed drug encapsulation in the range of 11.02±0.98 -32.45±0.62 % and sustained the release up to 5 days. The drug release from microspheres was diffusion controlled. The antimicrobial study indicated inhibition of growth of Staphylococcus aureus at all drug concentrations of in vitro release samples. In situ gel containing optimized microspheres extended the drug release up to 7 days. Results of the study demonstrated good bioadhesion of the in-situ gel containing microspheres as well as exhibited sustained release of drug. The in-situ gel containing ORDZ-loaded chitosan microspheres may be an efficient alternative to the other known delivery systems for treatment of Periodontitis.
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