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PLGA-based microspheres loaded with metformin hydrochloride: Modified double emulsion method preparation, optimization, characterization, and in vitro evaluation - 19/10/23

Microsphères à base de PLGA chargées de chlorhydrate de metformine : préparation, optimisation, caractérisation et évaluation in vitro de la méthode à double émulsion modifiée

Doi : 10.1016/j.pharma.2023.09.002 
Priyanka Chauhan a, Himanshu Paliwal b, Chetan Singh Chauhan a, , Ankit Paliwal c
a Faculty of Pharmacy, Bhupal Nobles’ University, Udaipur, Rajasthan, India 
b Department of Pharmaceutics and Pharmaceutical Technology, Faculty of Pharmacy, Shree S. K. Patel College of Pharmaceutical Education and Research, Ganpat University, Kherva, India 
c Pacific College of Pharmacy, Pacific University, Udaipur, Rajasthan, India 

*Corresponding author.

Highlights

PLGA-based microspheres were fabricated using double emulsion method to encapsulate metformin hydrochloride.
Effect of PLGA concentration on the % yield, particle size, and drug loading and encapsulation efficiency was studied.
Drug-loaded microspheres were also subjected DSC, FT-IR, and XRD to assess their characteristics and possible interactions.
One-year all-cause mortality was higher in patients with active cancer.
This was mainly driven by non-cardiovascular causes.
More data are warranted regarding specific outcomes after TAVR in these patients.
In vitro release study showed polymer concentration dependent-reduction in drug release rate from microspheress.

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Summary

The modified solvent removal method was used to encapsulate metformin hydrochloride (MH) within poly(lactic-co-glycolic acid) (PLGA) microspheres. The study investigated the effect of varying polymer concentrations on the loading and release of the drug from the microspheres. The encapsulation process involved using a double emulsion method, resulting in microspheres with particle diameters ranging from approximately 4.4μm to 2.7μm. The study achieved high encapsulation efficiencies, ranging from 81% to 90%, with drug loadings ranging from 18% to 11%. The release of the drug from the microspheres followed a biphasic pattern over 24 days, with nearly complete release by the end of the study period. Fourier transform infrared spectroscopy (FTIR) analysis indicated that there were no notable differences between PLGA and MH-loaded microspheres, suggesting minimal interactions between MH and PLGA. Differential scanning calorimetry (DSC) and X-ray diffraction (XRD) techniques were used to investigate the state of the MH within the microspheres. The results suggested that the MH was dispersed at a molecular level within the spheres and existed in an amorphous state. This amorphous state of the drug may explain the slow and prolonged release observed in the study.

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Résumé

La méthode modifiée d’élimination du solvant a été utilisée pour encapsuler le chlorhydrate de metformine (MH) dans des microsphères de poly(acide lactique-co-glycolique) (PLGA). L’étude a étudié l’effet de concentrations variables de polymère sur le chargement et la libération du médicament à partir des microsphères. Le processus d’encapsulation impliquait l’utilisation d’une méthode à double émulsion, résultant en des microsphères avec des diamètres de particules allant d’environ 4,4μm à 2,7μm. L’étude a atteint des efficacités d’encapsulation élevées, allant de 81 % à 90 %, avec des charges de médicament allant de 18 % à 11 %. La libération du médicament à partir des microsphères a suivi un schéma biphasique sur 24jours, avec une libération presque complète à la fin de la période d’étude. L’analyse par spectroscopie infrarouge à transformée de Fourier (FTIR) a indiqué qu’il n’y avait pas de différences notables entre les microsphères chargées de PLGA et de MH, ce qui suggère des interactions minimales entre MH et PLGA. Des techniques de calorimétrie à balayage différentiel (DSC) et de diffraction des rayons X (XRD) ont été utilisées pour étudier l’état du MH dans les microsphères. Les résultats suggèrent que le MH était dispersé au niveau moléculaire dans les sphères et existait à l’état amorphe. Cet état amorphe du médicament peut expliquer la libération lente et prolongée observée dans l’étude.

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Keywords : Microspheres, Metformin hydrochloride, Poly(lactic-co-glycolic acid), Sustained release

Mots clés : Microsphères, Chlorhydrate de metformine, Poly(acide lactique-co-glycolique), Libération prolongée


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Vol 81 - N° 6

P. 997-1006 - novembre 2023 Ritorno al numero
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