Objective: The aim of this study was to develop a bioadhesive gel of gatifloxacin for the treatment of periodontal diseases.Methods: Periodontal gels of gatifloxacin were prepared using different hydrophilic polymers such as carbopol 940 (CP 940), carboxymethyl cellulose (CMC) and hydroxypropylmethyl cellulose (HPMC) in varied concentrations, either alone or as a combination. The prepared gels were evaluated for their physical appearance, pH, drug content, viscosity, bioadhesiveness and in vitro drug release profile. The influence of the type and the concentration of polymer on the drug release as well as on viscosity and mucoadhesiveness of prepared gels were investigated. Results:The prepared gels showed acceptable physical properties concerning color, homogeneity, consistency, spreadability, and pH value. Using different polymer types at different concentrations, as well as different polymer combinations, play a significant role in the variation of overall characteristics of formulations. Increasing the concentration of polymer increased the viscosity as well as mucoadhesion, and reduced drug release rate. Formulation F 11 (1 % CP 940 and 5 % CMC) was selected as the formula of choice based on the data of various evaluation parameters such as pH, drug content, viscosity, spreadability and bioadhesion as well as its ability to show a prolonged drug release pattern. Conclusion:The obtained results show that a bioadhesive periodontal gel of gatifloxacin can be prepared using hydrophilic polymers, and by using a combination of polymers the viscosity, mucoadhesiveness, spreadability and release behavior can be optimized.
Objective: The purpose of this study to develop and optimize nasal mucoadhesive in situ gel IG of sumatriptan ST (serotonin agonist) to enhance nasal residence time for migraine management. Method: Cold method was used to prepare ST nasal in-situ gel, using thermosensitive polymers (poloxamer 407 and/or poloxamer 188) with a mucoadhesive polymer (hyaluronic acid HA) which were examined for gelation temperature and gelation time, pH, drug content, gel strength, spreadability, mucoadhesive force determination, viscosity, in-vitro drug release, and the selected formula was subjected to ex-vivo permeation study and histological evaluation of the sheep mucosal tissue after application. Results: The results showed that the formula IG7 prepared from poloxamer 407(19%), poloxamer188 (4%) and HA (0.5%) had an optimum gelation temperature (32.66±1.52°C), gel strength (43.66± 1.52 sec), mucoadhesive force (8067.93± 746.45dyne\cm2), in-vitro drug release (95.98%) over 6hr, ex-vivo permeation study release (89.6%) during the 6 h. study with no histological or pathological change in the nasal sheep tissue. Conclusion: The ease of administration via a nasal drop of ST coupled with less frequent administration and prolong drug release, will enhance patient compliance.
Nefopam (N.F.) HCl is a non-narcotic centrally-acting, non-opioid benzoxazocine analgesic to relieve acute and chronic pain. It exhibits low bioavailability (about 36%) due to its first-pass degradation in the liver. Intranasal administration has been used as a new route for targeting active brain sites and enhancing the bioavailability of N.F. HCl bypassing hepatic metabolism. In situ gel of N.F. HCl was prepared by the cold method using different concentrations of Poloxamer 407, Poloxamer 188, HPMC K4M, Carbapol 934, and Hyaluronic acid polymers. The results show that identification tests are superimposed with references, solubility study shows that N.F. HCl is suitable to be administered intranasally; Compatibility studies reveal incompatibility of Nefopam HCl with HPMC K4M and Carbapol 934; meanwhile, no interaction with Methylcellulose and Hyaluronic acid. In conclusion, the obtained results revealed the incredible ability of the produced N.F. HCl intranasal in situ gel is intended to enhance drug bioavailability bypassing the metabolizing effect of the liver that N.F. HCl is facing when given orally.
The aim of the present investigation was to develop a microsponge delivery system of acyclovir to control its release when applied topically thereby reducing dosing frequency and enhancing patient compliance. The microsponge was produced by oil in oil emulsion solvent diffusion method. The effect of different formulation and process variables such as internal phase volume, polymer type, drug polymer ratio, stirring speed and stirring duration on microsponge production yield, loading efficiency, particle size, and in vitro drug release was evaluated. The results showed that the microsponge F2 prepared from Eudragit RS polymer had optimum physical properties regarding loading efficiency of 99.71±0.7 % and production yield which was 85%. Also, F2 showed 66% drug release through 8 hours. Accordingly, the oil in oil emulsion solvent diffusion method is an effective technique to formulate microsponge with maximum production yields and loading efficiency for acyclovir.
This study aims to develop a thermosensitive mucoadhesive periodontal in situ gel of secnidazole for local release of drug for treatment of periodontitis, in order to increase the drug residence time and to increase patient compliance while lowering the side effects of the drug. Cold method was used to prepare 30 formulas of secnidazole periodontal in situ gel, using different concentrations of thermosensitive polymers (poloxamer407 alone or in combination with poloxamer 188) and methyl cellulose (MC ) or hydroxypropyl methylcellulose (HPMC K4M )in different concentrations used as mucoadhesive polymer and the resultant formulations were subjected to several tests such as gelation temperature GT, appearance and pH value. The formulas with the most appropriate GT were subjected to in-vitro drug release. Three formulas were chosen with appropriate release, F6 (15% P407, 1% MC), F29 (18%P407,3% P188, 0.8% HPMC) and F30 (18%P407,3% P188, 1% HPMC). These formulas were subjected to mucoadhesive force, viscosity, drug content, spreadability, gelation time and Fourier Transform Infrared (FTIR) compatibility studies. The results indicates that formula F29 and F30 have best gelation temperatures (33°C, 32°C) gel strength (1.5h,2h) mucoadhesive force of (17.1, 23.4 dyne/cm2 ) and in-vitro drug release (98.2%, 100%) respectively during 3.5h and gelation, time about 10 seconds for both formulas and FTIR spectrum study show absence of important interaction between secnidazole and the polymers used.
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