Monika Bansal1, Neelam Mittal1, Sarita Kumari Yadav2, Gayasuddin Khan2, Pooja Gupta3, Brahmeshwar Mishra2, Gopal Nath3. 1. Faculty of Dental Sciences, Institute of Medical Sciences, Banaras Hindu University, Varanasi, 221005, India. 2. Department of Pharmaceutics, Indian institute of Technology, Banaras Hindu University, Varanasi, 221005, India. 3. Department of Microbiology, Faculty of Medicine, Institute of Medical Sciences Banaras Hindu University, Varanasi, 221005, India.
Abstract
BACKGROUND: This study aimed to formulate and characterize in-situ gel containing levofloxacin and metronidazole to release drugs in controlled manner for treatment of periodontitis. MATERIAL AND METHODS: Medicated in-situ gel with levofloxacin (10% w/v), metronidazole (25% w/v) and vehicle in-situ gel without drugs having poloxamer 407 (20% w/v) and chitosan (0.5%, 1%, 1.5%, 2.0% 2.5% w/v) were prepared and characterized for physicochemical, mechanical properties, stability and in-vitro drug release. Fourier transform infrared spectroscopy and differential scanning calorimetery studies were done. Optimized formulation was evaluated by scanning electron microscope (SEM) and in-vitro antimicrobial activity against 5 bacterial strains. RESULTS: The results revealed that drugs and polymers were compatible to formulate. All formulations were light yellow, clear and syringeable except formulation having 2.5% w/v chitosan. pH was in the range of 6.20 to 6.74. 1.0% w/v and 1.5% w/v chitosan formulations showed gelation temperature 37 ± 0.32 °C and 34 ± 0.21 °C. Further, mucoadhesive strength indicated mucoadhesivity of gel. In-vitro release study of 1.5% w/v chitosan formulation showed initial burst where about 55-60% MZ and 60-70% LVF got released within 6-7 hrs followed by sustained release upto 48 hrs. SEM images of 1.5% w/v chitosan optimized medicated in-situ and vehicle in-situ gel appeared similar indicating homogeneous mixing of polymers with drugs. In-vitro antimicrobial study showed that medicated in-situ gel was more effective than vehicle. CONCLUSIONS: In conclusion, optimized 1.5% w/v chitosan in-situ gel was thermoresponsive, mucoadhesive, syringeable, and released drugs in slow and controlled manner with effectiveness against broad range of microbes.
BACKGROUND: This study aimed to formulate and characterize in-situ gel containing levofloxacin and metronidazole to release drugs in controlled manner for treatment of periodontitis. MATERIAL AND METHODS: Medicated in-situ gel with levofloxacin (10% w/v), metronidazole (25% w/v) and vehicle in-situ gel without drugs having poloxamer 407 (20% w/v) and chitosan (0.5%, 1%, 1.5%, 2.0% 2.5% w/v) were prepared and characterized for physicochemical, mechanical properties, stability and in-vitro drug release. Fourier transform infrared spectroscopy and differential scanning calorimetery studies were done. Optimized formulation was evaluated by scanning electron microscope (SEM) and in-vitro antimicrobial activity against 5 bacterial strains. RESULTS: The results revealed that drugs and polymers were compatible to formulate. All formulations were light yellow, clear and syringeable except formulation having 2.5% w/v chitosan. pH was in the range of 6.20 to 6.74. 1.0% w/v and 1.5% w/v chitosan formulations showed gelation temperature 37 ± 0.32 °C and 34 ± 0.21 °C. Further, mucoadhesive strength indicated mucoadhesivity of gel. In-vitro release study of 1.5% w/v chitosan formulation showed initial burst where about 55-60% MZ and 60-70% LVF got released within 6-7 hrs followed by sustained release upto 48 hrs. SEM images of 1.5% w/v chitosan optimized medicated in-situ and vehicle in-situ gel appeared similar indicating homogeneous mixing of polymers with drugs. In-vitro antimicrobial study showed that medicated in-situ gel was more effective than vehicle. CONCLUSIONS: In conclusion, optimized 1.5% w/v chitosan in-situ gel was thermoresponsive, mucoadhesive, syringeable, and released drugs in slow and controlled manner with effectiveness against broad range of microbes.
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