Pharmacoscintigraphic evaluation and antidiabetic efficacy of gliclazide-loaded 99mTc-labelled mucoadhesive microspheres

Abstract Background The current study was carried out to evaluate the possible application of Musa balbisiana starch in formulation of mucoadhesive microsphere for oral delivery of gliclazide (GLZ). The study objective was to improve the oral bioavailability along with prolongation of its duration o...

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Autores principales:	Ripunjoy Bordoloi, Abdul Baquee Ahmed, Kunal Bhattacharya
Formato:	article
Lenguaje:	EN
Publicado:	SpringerOpen 2021
Materias:	Gliclazide Mucoadhesive microspheres Gamma scintigraphy 99mTc-pertechnetate Ionic gelation Therapeutics. Pharmacology RM1-950 Pharmacy and materia medica RS1-441
Acceso en línea:	https://doaj.org/article/5394eaacc1d346fe8bbce6c347b3f5ad
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spelling	oai:doaj.org-article:5394eaacc1d346fe8bbce6c347b3f5ad2021-11-28T12:30:09ZPharmacoscintigraphic evaluation and antidiabetic efficacy of gliclazide-loaded 99mTc-labelled mucoadhesive microspheres10.1186/s43094-021-00376-32314-7253https://doaj.org/article/5394eaacc1d346fe8bbce6c347b3f5ad2021-11-01T00:00:00Zhttps://doi.org/10.1186/s43094-021-00376-3https://doaj.org/toc/2314-7253Abstract Background The current study was carried out to evaluate the possible application of Musa balbisiana starch in formulation of mucoadhesive microsphere for oral delivery of gliclazide (GLZ). The study objective was to improve the oral bioavailability along with prolongation of its duration of action for a better glycaemic control. Ionic gelation technique was employed in formulating the dosage form. Optimization of the batches was carried out by response surface methodology using 32 full factorial designs. The microsphere prepared was characterized for several parameters along with its in vitro release study. The gastrointestinal transit of the optimized batch of prepared microspheres after oral administration was studied in rabbits by using the gamma scintigraphy technique utilizing 99mTc as the labelling agent in the presence of stannous chloride. Also, the optimized batch was studied for its pharmacokinetic parameters. Moreover, the antidiabetic efficacy of the prepared microsphere was evaluated in rats by using the streptozotocin (STZ)-induced diabetic model. Results The factorial design experiment resulted in an optimum formulation coded as F8. The compatible nature of the drug and excipient was revealed from FTIR, DSC and IST studies. The scanning electron micrographs also showed the occurrence of spherical microspheres having a smooth surface. The in vitro release study provided an evidence of an initial burst effect that was followed by a prolong release phase. The pharmacokinetic parameters justified the ability of the prepared dosage form in sustaining the drug release with a 2.7-fold enhancement in drug bioavailability. The images obtained during the gamma scintigraphy study suggested the gastro-retentive nature of the dosage form with the gastro-retentive ability for more than 4 h. Also, the pharmacodynamics study carried out in diabetic rat model confirmed about the better efficacy of the dosage form in lowering the elevated blood glucose level. Conclusion The overall study data provide valuable information about the potential of this banana starch in formulation of a mucoadhesive dosage form that can be used for enhancement of bioavailability of drug-like gliclazide which in turn can provide a beneficial effect in the management of diabetes.Ripunjoy BordoloiAbdul Baquee AhmedKunal BhattacharyaSpringerOpenarticleGliclazideMucoadhesive microspheresGamma scintigraphy99mTc-pertechnetateIonic gelationTherapeutics. PharmacologyRM1-950Pharmacy and materia medicaRS1-441ENFuture Journal of Pharmaceutical Sciences, Vol 7, Iss 1, Pp 1-27 (2021)
institution	DOAJ
collection	DOAJ
language	EN
topic	Gliclazide Mucoadhesive microspheres Gamma scintigraphy 99mTc-pertechnetate Ionic gelation Therapeutics. Pharmacology RM1-950 Pharmacy and materia medica RS1-441
spellingShingle	Gliclazide Mucoadhesive microspheres Gamma scintigraphy 99mTc-pertechnetate Ionic gelation Therapeutics. Pharmacology RM1-950 Pharmacy and materia medica RS1-441 Ripunjoy Bordoloi Abdul Baquee Ahmed Kunal Bhattacharya Pharmacoscintigraphic evaluation and antidiabetic efficacy of gliclazide-loaded 99mTc-labelled mucoadhesive microspheres
description	Abstract Background The current study was carried out to evaluate the possible application of Musa balbisiana starch in formulation of mucoadhesive microsphere for oral delivery of gliclazide (GLZ). The study objective was to improve the oral bioavailability along with prolongation of its duration of action for a better glycaemic control. Ionic gelation technique was employed in formulating the dosage form. Optimization of the batches was carried out by response surface methodology using 32 full factorial designs. The microsphere prepared was characterized for several parameters along with its in vitro release study. The gastrointestinal transit of the optimized batch of prepared microspheres after oral administration was studied in rabbits by using the gamma scintigraphy technique utilizing 99mTc as the labelling agent in the presence of stannous chloride. Also, the optimized batch was studied for its pharmacokinetic parameters. Moreover, the antidiabetic efficacy of the prepared microsphere was evaluated in rats by using the streptozotocin (STZ)-induced diabetic model. Results The factorial design experiment resulted in an optimum formulation coded as F8. The compatible nature of the drug and excipient was revealed from FTIR, DSC and IST studies. The scanning electron micrographs also showed the occurrence of spherical microspheres having a smooth surface. The in vitro release study provided an evidence of an initial burst effect that was followed by a prolong release phase. The pharmacokinetic parameters justified the ability of the prepared dosage form in sustaining the drug release with a 2.7-fold enhancement in drug bioavailability. The images obtained during the gamma scintigraphy study suggested the gastro-retentive nature of the dosage form with the gastro-retentive ability for more than 4 h. Also, the pharmacodynamics study carried out in diabetic rat model confirmed about the better efficacy of the dosage form in lowering the elevated blood glucose level. Conclusion The overall study data provide valuable information about the potential of this banana starch in formulation of a mucoadhesive dosage form that can be used for enhancement of bioavailability of drug-like gliclazide which in turn can provide a beneficial effect in the management of diabetes.
format	article
author	Ripunjoy Bordoloi Abdul Baquee Ahmed Kunal Bhattacharya
author_facet	Ripunjoy Bordoloi Abdul Baquee Ahmed Kunal Bhattacharya
author_sort	Ripunjoy Bordoloi
title	Pharmacoscintigraphic evaluation and antidiabetic efficacy of gliclazide-loaded 99mTc-labelled mucoadhesive microspheres
title_short	Pharmacoscintigraphic evaluation and antidiabetic efficacy of gliclazide-loaded 99mTc-labelled mucoadhesive microspheres
title_full	Pharmacoscintigraphic evaluation and antidiabetic efficacy of gliclazide-loaded 99mTc-labelled mucoadhesive microspheres
title_fullStr	Pharmacoscintigraphic evaluation and antidiabetic efficacy of gliclazide-loaded 99mTc-labelled mucoadhesive microspheres
title_full_unstemmed	Pharmacoscintigraphic evaluation and antidiabetic efficacy of gliclazide-loaded 99mTc-labelled mucoadhesive microspheres
title_sort	pharmacoscintigraphic evaluation and antidiabetic efficacy of gliclazide-loaded 99mtc-labelled mucoadhesive microspheres
publisher	SpringerOpen
publishDate	2021
url	https://doaj.org/article/5394eaacc1d346fe8bbce6c347b3f5ad
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Pharmacoscintigraphic evaluation and antidiabetic efficacy of gliclazide-loaded 99mTc-labelled mucoadhesive microspheres

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