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23 Full factorial design for optimization of stable amorphous host–guest-based mirabegron complex for extended-release action

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Journal of Inclusion Phenomena and Macrocyclic Chemistry Aims and scope Submit manuscript

Abstract

The current study was to develop a stable amorphous mirabegron complex with improved solubility, stability, and extended-release of action. HPβCD was screened as a suitable complexing agent, which exhibited an entrapment efficiency of 91.2 ± 3.4% and facilitated transformation of drug into the amorphous state. The addition of ethylcellulose extended the release of the complex by 81.4 ± 2.8% for 12 h. The influence of HPβCD and ethyl cellulose on the crystal habit of mirabegron was analyzed by XRPD, DSC, ATR FTIR and morphological behavior were analyzed by SEM. 23 Full factorial design was used to optimize the mirabegron complex. The outcomes of stability studies illustrated amorphous complex was stable for 6 months at long-term and accelerated storage conditions, where content uniformity came under the accepted range of 98–102%. Thus, HPβCD-based inclusion complex represents a futuristic approach to design mirabegron formulation with improved solubility and extended-release of action in over active bladder syndrome.

Graphic abstract

Host-guest complex of HPβCD and mirabegron.

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Abbreviations

β-CD:

β-Cyclodextrin

HPβCD:

2-Hydroxypropyl-β-cyclodextrin

BHT:

Butylated hydroxytoluene

PVPK-30:

Polyvinyl pyrrolidone K-30

EC:

Ethyl cellulose

DoE:

Design of experiments

PTFE:

Polytetrafluoroethylene

PVDF:

Polyvinylidene fluoride

SEM:

Scanning electron microscopy

HPLC:

High-performance liquid chromatography

ATR FTIR:

Attenuated total reflectance Fourier transform infrared spectroscopy

DSC:

Differential scanning calorimetry

RH:

Relative humidity

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  1. Shobhaben Pratapbhai Patel School of Pharmacy and Technology Management, SVKM’S NMIMS, V.L. Mehta Road, Vile Parle (W), Mumbai, India

    Pankaj Mandpe, Bala Prabhakar & Pravin Shende

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  1. Pankaj Mandpe
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  2. Bala Prabhakar
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  3. Pravin Shende
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Correspondence to Pravin Shende.

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Mandpe, P., Prabhakar, B. & Shende, P. 23 Full factorial design for optimization of stable amorphous host–guest-based mirabegron complex for extended-release action. J Incl Phenom Macrocycl Chem 96, 111–123 (2020). https://doi.org/10.1007/s10847-019-00955-1

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