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Surface Deposition and Coalescence and Coacervation Phase Separation Methods: In Vitro Study and Compatibility Analysis of Eudragit RS30D, Eudragit RL30D, and Carbopol-PLA Loaded Metronidazole Microspheres.

Dewan I, Islam MM, Al-Hasan M, Nath J, Sultana S, Rana MS - J Pharm (Cairo) (2015)

Bottom Line: Metronidazole (MTZ) has extremely broad spectrum of protozoal and antimicrobial activity and is clinically effective in trichomoniasis, amoebic colitis, and giardiasis.The SEM and FTIR studies confirm good spheres and smooth surface as well as interaction between drug and polymers.Though release kinetic is uncertain, the best fit was obtained with the Korsmeyer kinetic model with release exponent (n) lying between 0.45 and 0.89.

View Article: PubMed Central - PubMed

Affiliation: Department of Pharmacy, University of Asia Pacific, Dhanmondi, Dhaka 1209, Bangladesh.

ABSTRACT
Metronidazole (MTZ) has extremely broad spectrum of protozoal and antimicrobial activity and is clinically effective in trichomoniasis, amoebic colitis, and giardiasis. This study was performed to formulate and evaluate the MTZ loaded microspheres by coacervation phase separation and surface deposition and coalescence methods using different polymers like Gelatin, Carbopol 934P, Polylactic Acid (PLA), Eudragit RS30D, and Eudragit RL30D to acquire sustained release of drug. In vitro dissolution studies were carried out in phosphate buffer (pH 7.4) for 8 hours according to USP paddle method. The maximum and minimum release of MTZ from microspheres observed were 84.81% and 76.6% for coacervation and 95.07% and 80.07% for surface deposition method, respectively, after 8 hours. Release kinetics was studied in different mathematical release models. The SEM and FTIR studies confirm good spheres and smooth surface as well as interaction between drug and polymers. Though release kinetic is uncertain, the best fit was obtained with the Korsmeyer kinetic model with release exponent (n) lying between 0.45 and 0.89. In vitro studies showed that MTZ microspheres with different polymers might be a good candidate as sustained drug delivery system to treat bacterial infections.

No MeSH data available.


Related in: MedlinePlus

Formulation of metronidazole microspheres based on surface deposition and coalescence method.
© Copyright Policy - open-access
Related In: Results  -  Collection


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fig2: Formulation of metronidazole microspheres based on surface deposition and coalescence method.

Mentions: Part A was taken in a beaker and an emulsion was made with 18 gm Eudragit RL/RS30D. Part B was taken in another beaker and placed onto a hot plate. The temperature was raised to 90°C. About 4 gm of 250–500-micron-sized metronidazole granules was added to this part of light liquid paraffin with continuous stirring. Part A containing Eudragit RL/RS30D emulsion was added in different installment. Few-minute time was allowed between each addition to settle down the Eudragit RL/RS30D over the granules. The temperature was maintained at 85 to 90°C for 90 minutes. After cooling to room temperature the microspheres were filtered and washed three times with petroleum ether and those were kept in dry air. Finally the microspheres were dried at 40°C for 12 hours shown in Figure 2.


Surface Deposition and Coalescence and Coacervation Phase Separation Methods: In Vitro Study and Compatibility Analysis of Eudragit RS30D, Eudragit RL30D, and Carbopol-PLA Loaded Metronidazole Microspheres.

Dewan I, Islam MM, Al-Hasan M, Nath J, Sultana S, Rana MS - J Pharm (Cairo) (2015)

Formulation of metronidazole microspheres based on surface deposition and coalescence method.
© Copyright Policy - open-access
Related In: Results  -  Collection

Show All Figures
getmorefigures.php?uid=PMC4663742&req=5

fig2: Formulation of metronidazole microspheres based on surface deposition and coalescence method.
Mentions: Part A was taken in a beaker and an emulsion was made with 18 gm Eudragit RL/RS30D. Part B was taken in another beaker and placed onto a hot plate. The temperature was raised to 90°C. About 4 gm of 250–500-micron-sized metronidazole granules was added to this part of light liquid paraffin with continuous stirring. Part A containing Eudragit RL/RS30D emulsion was added in different installment. Few-minute time was allowed between each addition to settle down the Eudragit RL/RS30D over the granules. The temperature was maintained at 85 to 90°C for 90 minutes. After cooling to room temperature the microspheres were filtered and washed three times with petroleum ether and those were kept in dry air. Finally the microspheres were dried at 40°C for 12 hours shown in Figure 2.

Bottom Line: Metronidazole (MTZ) has extremely broad spectrum of protozoal and antimicrobial activity and is clinically effective in trichomoniasis, amoebic colitis, and giardiasis.The SEM and FTIR studies confirm good spheres and smooth surface as well as interaction between drug and polymers.Though release kinetic is uncertain, the best fit was obtained with the Korsmeyer kinetic model with release exponent (n) lying between 0.45 and 0.89.

View Article: PubMed Central - PubMed

Affiliation: Department of Pharmacy, University of Asia Pacific, Dhanmondi, Dhaka 1209, Bangladesh.

ABSTRACT
Metronidazole (MTZ) has extremely broad spectrum of protozoal and antimicrobial activity and is clinically effective in trichomoniasis, amoebic colitis, and giardiasis. This study was performed to formulate and evaluate the MTZ loaded microspheres by coacervation phase separation and surface deposition and coalescence methods using different polymers like Gelatin, Carbopol 934P, Polylactic Acid (PLA), Eudragit RS30D, and Eudragit RL30D to acquire sustained release of drug. In vitro dissolution studies were carried out in phosphate buffer (pH 7.4) for 8 hours according to USP paddle method. The maximum and minimum release of MTZ from microspheres observed were 84.81% and 76.6% for coacervation and 95.07% and 80.07% for surface deposition method, respectively, after 8 hours. Release kinetics was studied in different mathematical release models. The SEM and FTIR studies confirm good spheres and smooth surface as well as interaction between drug and polymers. Though release kinetic is uncertain, the best fit was obtained with the Korsmeyer kinetic model with release exponent (n) lying between 0.45 and 0.89. In vitro studies showed that MTZ microspheres with different polymers might be a good candidate as sustained drug delivery system to treat bacterial infections.

No MeSH data available.


Related in: MedlinePlus