Polymers in Medicine

Polim. Med.
Index Copernicus (ICV 2021) – 120.65
MNiSW – 70
Average rejection rate – 27.13%
ISSN 0370-0747 (print)
ISSN 2451-2699 (online) 
Periodicity – biannual

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Polymers in Medicine

2019, vol. 49, nr 1, January-June, p. 35–43

doi: 10.17219/pim/111887

Publication type: original article

Language: English

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Creative Commons BY-NC-ND 3.0 Open Access

Influence of levodropropizine and hydroxypropyl-β-cyclodextrin association on the physicochemical characteristics of levodropropizine loaded in hydroxypropyl-β-cyclodextrin microcontainers: Formulation and in vitro characterization

Abid Mehmood Yousaf1,A,D, Alina Qadeer2,B, Syed Atif Raza3,E,F, Tahir Ali Chohan4,C,F, Yasser Shahzad1,E,F, Fakhar Ud Din5,E, Ikram Ullah Khan6,E,F, Talib Hussain1,E,F, Muhammad Nadeem Alvi2,E,F, Tariq Mahmood7,E,F

1 Drug Delivery Research Group, Department of Pharmacy, COMSATS University Islamabad, Lahore, Pakistan

2 Faculty of Pharmacy, University of Central Punjab, Lahore, Pakistan

3 Punjab University College of Pharmacy, University of the Punjab, Allama Iqbal Campus, Lahore, Pakistan

4 Institute of Pharmaceutical Sciences, University of Veterinary and Animal Sciences, Lahore, Pakistan

5 Department of Pharmacy, Quaid-i-Azam University, Islamabad, Pakistan

6 Department of Pharmaceutics, Faculty of Pharmaceutical Sciences, Government College University Faisalabad, Pakistan

7 Sahara College of Pharmacy, Narowal, Pakistan

Abstract

Background. Poorly water-soluble drugs do not dissolve well in aqueous-based gastrointestinal fluid; therefore, they are not well absorbed. Thus, employing a suitable solubility enhancing technique is necessary for such a drug. Drug/HP‑β‑CD complexation is a promising way to improve solubility and dissolution of a poorly water-soluble drug. Levodropropizine was used as a model drug in this study.
Objectives. The purpose of this research was to enhance the aqueous solubility and dissolution rate of levodropropizine by employing the inclusion complexation technique.
Material and Methods. A microparticle formulation was prepared from levodropropizine and hydroxypropyl-β-cyclodextrin (HP‑β‑CD) in a 1:1 molar ratio through the spray-drying technique. The host-guest relationship between levodropropizine and HP‑β‑CD was also investigated using the molecular docking computational methodology. The aqueous solubility and dissolution rate of levodropropizine in formulations were assessed and compared with those of the drug alone. X-ray diffraction (XRD), differential scanning calorimetry (DSC), scanning electron microscopy (SEM), and Fourier transform infrared spectroscopy (FTIR) were applied for the solid-state characterization of the prepared samples.
Results. According to the research outcomes, the levodropropizine/HP‑β‑CD formulation had enhanced the aqueous solubility (351.12 ±13.26 vs 92.76 ±5.00 mg/mL) and dissolution rate (97.83 ±3.36 vs 3.12 ±1.76% in 10 min) of levodropropizine, compared to the plain drug powder. The levodropropizine/ HP‑β‑CD formulation had converted the crystalline drug into its amorphous counterpart. Furthermore, no covalent interaction was found to exist between levodropropizine and HP‑β‑CD. The spray-dried particles were discrete. Each particle had a shriveled appearance.
Conclusion. The levodropropizine/HP‑β‑CD formulation is, therefore, recommended for the more effective administration of levodropropizine through the oral route.

Key words

dissolution rate, spray-drying, cyclodextrins, amorphous form, phase solubility

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