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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

It schematically presents the steps of microspheres prepared by coacervation phase separation method.
© Copyright Policy - open-access
Related In: Results  -  Collection


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fig1: It schematically presents the steps of microspheres prepared by coacervation phase separation method.

Mentions: According to Table 1 Gelatin-Carbopol/PLA mixture was dissolved in ten mL of water which was previously heated to 50°C. To this metronidazole was added and stirred approximately at 300 rpm with the help of magnetic stirrer for 15 minutes to get a stable dispersion. The dispersion was poured dropwise into the ten mL of sunflower oil which was also previously heated to 50°C on a water bath. The mixture was stirred with a help of magnetic stirrer for 2 hrs at 300 rpm at room temperature. At the end of two hrs, cross-linking agent formaldehyde 0.5 mL was added to the dispersion medium with continuous stirring for next 30 minutes. After that, the final dispersion was kept in refrigerator for 24 hrs to make sure of the rigidization of microspheres shown in Figure 1.


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)

It schematically presents the steps of microspheres prepared by coacervation phase separation method.
© Copyright Policy - open-access
Related In: Results  -  Collection

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

fig1: It schematically presents the steps of microspheres prepared by coacervation phase separation method.
Mentions: According to Table 1 Gelatin-Carbopol/PLA mixture was dissolved in ten mL of water which was previously heated to 50°C. To this metronidazole was added and stirred approximately at 300 rpm with the help of magnetic stirrer for 15 minutes to get a stable dispersion. The dispersion was poured dropwise into the ten mL of sunflower oil which was also previously heated to 50°C on a water bath. The mixture was stirred with a help of magnetic stirrer for 2 hrs at 300 rpm at room temperature. At the end of two hrs, cross-linking agent formaldehyde 0.5 mL was added to the dispersion medium with continuous stirring for next 30 minutes. After that, the final dispersion was kept in refrigerator for 24 hrs to make sure of the rigidization of microspheres shown in Figure 1.

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