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Gellan gum-based mucoadhesive microspheres of almotriptan for nasal administration: Formulation optimization using factorial design, characterization, and in vitro evaluation.

Abbas Z, Marihal S - J Pharm Bioallied Sci (2014)

Bottom Line: Regression analysis was performed to identify the best formulation conditions.In vitro drug diffusion was Higuchi matrix controlled and the release mechanism was found to be non-Fickian.Stability studies indicated that there were no significant deviations in the drug content, in vitro mucoadhesion and in vitro drug diffusion characteristics.

View Article: PubMed Central - PubMed

Affiliation: Research Scientist, Formulation Development Department, Apotex Research Private Limited, Bangalore - 560 099, India.

ABSTRACT

Background: Almotriptan malate (ALM), indicated for the treatment of migraine in adults is not a drug candidate feasible to be administered through the oral route during the attack due to its associated symptoms such as nausea and vomiting. This obviates an alternative dosage form and nasal drug delivery is a good substitute to oral and parenteral administration.

Materials and methods: Gellan gum (GG) microspheres of ALM, for intranasal administration were prepared by water-in-oil emulsification cross-linking technique employing a 2(3) factorial design. Drug to polymer ratio, calcium chloride concentration and cross-linking time were selected as independent variables, while particle size and in vitro mucoadhesion of the microspheres were investigated as dependent variables. Regression analysis was performed to identify the best formulation conditions. The microspheres were evaluated for characteristics such as practical percentage yield, particle size, percentage incorporation efficiency, swellability, zeta potential, in vitro mucoadhesion, thermal analysis, X-ray diffraction study, and in vitro drug diffusion studies.

Results: The shape and surface characteristics of the microspheres were determined by scanning electron microscopy, which revealed spherical nature and nearly smooth surface with drug incorporation efficiency in the range of 71.65 ± 1.09% - 91.65 ± 1.13%. In vitro mucoadhesion was observed the range of 79.45 ± 1.69% - 95.48 ± 1.27%. Differential scanning calorimetry and X-ray diffraction results indicated a molecular level dispersion of drug in the microspheres. In vitro drug diffusion was Higuchi matrix controlled and the release mechanism was found to be non-Fickian. Stability studies indicated that there were no significant deviations in the drug content, in vitro mucoadhesion and in vitro drug diffusion characteristics.

Conclusion: The investigation revealed promising potential of GG microspheres for delivering ALM intranasally for the treatment of migraine.

No MeSH data available.


Related in: MedlinePlus

Scanning electron microscope microphotograph of formulation AGM1 at low (a) and high (b) Magnification
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Figure 1: Scanning electron microscope microphotograph of formulation AGM1 at low (a) and high (b) Magnification

Mentions: The prepared microspheres were found to be discrete and spherical in shape and had nearly smooth surface morphology. These microspheres had no pores or rupture on the surface, such morphology would result in slow clearance and good deposition pattern in the nasal cavity.[44] The SEM photographs of the optimized formulation (AGM1) taken by SEM are depicted in Figure 1a and b.


Gellan gum-based mucoadhesive microspheres of almotriptan for nasal administration: Formulation optimization using factorial design, characterization, and in vitro evaluation.

Abbas Z, Marihal S - J Pharm Bioallied Sci (2014)

Scanning electron microscope microphotograph of formulation AGM1 at low (a) and high (b) Magnification
© Copyright Policy - open-access
Related In: Results  -  Collection

License
Show All Figures
getmorefigures.php?uid=PMC4231387&req=5

Figure 1: Scanning electron microscope microphotograph of formulation AGM1 at low (a) and high (b) Magnification
Mentions: The prepared microspheres were found to be discrete and spherical in shape and had nearly smooth surface morphology. These microspheres had no pores or rupture on the surface, such morphology would result in slow clearance and good deposition pattern in the nasal cavity.[44] The SEM photographs of the optimized formulation (AGM1) taken by SEM are depicted in Figure 1a and b.

Bottom Line: Regression analysis was performed to identify the best formulation conditions.In vitro drug diffusion was Higuchi matrix controlled and the release mechanism was found to be non-Fickian.Stability studies indicated that there were no significant deviations in the drug content, in vitro mucoadhesion and in vitro drug diffusion characteristics.

View Article: PubMed Central - PubMed

Affiliation: Research Scientist, Formulation Development Department, Apotex Research Private Limited, Bangalore - 560 099, India.

ABSTRACT

Background: Almotriptan malate (ALM), indicated for the treatment of migraine in adults is not a drug candidate feasible to be administered through the oral route during the attack due to its associated symptoms such as nausea and vomiting. This obviates an alternative dosage form and nasal drug delivery is a good substitute to oral and parenteral administration.

Materials and methods: Gellan gum (GG) microspheres of ALM, for intranasal administration were prepared by water-in-oil emulsification cross-linking technique employing a 2(3) factorial design. Drug to polymer ratio, calcium chloride concentration and cross-linking time were selected as independent variables, while particle size and in vitro mucoadhesion of the microspheres were investigated as dependent variables. Regression analysis was performed to identify the best formulation conditions. The microspheres were evaluated for characteristics such as practical percentage yield, particle size, percentage incorporation efficiency, swellability, zeta potential, in vitro mucoadhesion, thermal analysis, X-ray diffraction study, and in vitro drug diffusion studies.

Results: The shape and surface characteristics of the microspheres were determined by scanning electron microscopy, which revealed spherical nature and nearly smooth surface with drug incorporation efficiency in the range of 71.65 ± 1.09% - 91.65 ± 1.13%. In vitro mucoadhesion was observed the range of 79.45 ± 1.69% - 95.48 ± 1.27%. Differential scanning calorimetry and X-ray diffraction results indicated a molecular level dispersion of drug in the microspheres. In vitro drug diffusion was Higuchi matrix controlled and the release mechanism was found to be non-Fickian. Stability studies indicated that there were no significant deviations in the drug content, in vitro mucoadhesion and in vitro drug diffusion characteristics.

Conclusion: The investigation revealed promising potential of GG microspheres for delivering ALM intranasally for the treatment of migraine.

No MeSH data available.


Related in: MedlinePlus