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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

Release of metronidazole from formulations F25 to F27 and formulations F28 to F29 by coacervation phase separation and surface deposition and coalescence method, respectively. (a) Zero order, (b) first order, and (c) Higuchi and (d) Korsmeyer models.
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fig4: Release of metronidazole from formulations F25 to F27 and formulations F28 to F29 by coacervation phase separation and surface deposition and coalescence method, respectively. (a) Zero order, (b) first order, and (c) Higuchi and (d) Korsmeyer models.

Mentions: Polymers such as Gelatin, Carbopol, and Polylactic Acid (PLA) in different concentrations were used in formulations F25 to F27. The initial burst release of formulations F25, F26, and F27 was about 13.68%, 12.73%, and 12.26%, respectively, after 1 hour (Figure 4). After the end of 8 hours of dissolution, the release of microspheres from F25, F26, and F27 was 84.81%, 78.49%, and 76.60%, respectively. The addition of Carbopol along with Gelatin in formulation F26 retards the rate of drug release. The addition of PLA along with the same concentration of Gelatin in formulation F27 retards the rate of drug release significantly. Besides formulations F28 and F29 were prepared using the polymers of Eudragit RL30D and Eudragit RS30D in different concentrations. The initial burst release of formulations F28 and F29 was about 20.94% and 17.31%, respectively, after 1 hour (Figure 4). After the end of 8 hours of dissolution, the release of microspheres from F28 and F29 was 95.07% and 80.07%, respectively. The release of drug is significantly higher for formulation F28 than formulation F29. Eudragit RS30D retards the release of drug more than Eudragit RL30D.


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)

Release of metronidazole from formulations F25 to F27 and formulations F28 to F29 by coacervation phase separation and surface deposition and coalescence method, respectively. (a) Zero order, (b) first order, and (c) Higuchi and (d) Korsmeyer models.
© Copyright Policy - open-access
Related In: Results  -  Collection

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

fig4: Release of metronidazole from formulations F25 to F27 and formulations F28 to F29 by coacervation phase separation and surface deposition and coalescence method, respectively. (a) Zero order, (b) first order, and (c) Higuchi and (d) Korsmeyer models.
Mentions: Polymers such as Gelatin, Carbopol, and Polylactic Acid (PLA) in different concentrations were used in formulations F25 to F27. The initial burst release of formulations F25, F26, and F27 was about 13.68%, 12.73%, and 12.26%, respectively, after 1 hour (Figure 4). After the end of 8 hours of dissolution, the release of microspheres from F25, F26, and F27 was 84.81%, 78.49%, and 76.60%, respectively. The addition of Carbopol along with Gelatin in formulation F26 retards the rate of drug release. The addition of PLA along with the same concentration of Gelatin in formulation F27 retards the rate of drug release significantly. Besides formulations F28 and F29 were prepared using the polymers of Eudragit RL30D and Eudragit RS30D in different concentrations. The initial burst release of formulations F28 and F29 was about 20.94% and 17.31%, respectively, after 1 hour (Figure 4). After the end of 8 hours of dissolution, the release of microspheres from F28 and F29 was 95.07% and 80.07%, respectively. The release of drug is significantly higher for formulation F28 than formulation F29. Eudragit RS30D retards the release of drug more than Eudragit RL30D.

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