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Preparation and Characterization of Solid Dispersions of Artemether by Freeze-Dried Method.
Biomed Res Int. 2015; 2015:109563.BR

Abstract

Solid dispersions of artemether and polyethylene glycol 6000 (PEG6000) were prepared in ratio 12 : 88 (group-1). Self-emulsified solid dispersions of artemether were prepared by using polyethylene glycol 6000, Cremophor-A25, olive oil, Transcutol, and hydroxypropyl methylcellulose (HPMC) in ratio 12 : 75 : 5 : 4 : 2 : 2, respectively (group-2). In third group, only Cremophor-A25 was replaced with Poloxamer 188 compared to group-2. The solid dispersions and self-emulsified solid dispersions were prepared by physical and freeze dried methods, respectively. All samples were characterized by X-ray diffraction, attenuated total reflectance Fourier transform infrared spectroscopy, differential scanning calorimeter, scanning electron microscopy, and solubility, dissolution, and stability studies. X-ray diffraction pattern revealed artemether complete crystalline, whereas physical mixture and freeze-dried mixture of all three groups showed reduced peak intensities. In attenuated total reflectance Fourier transform infrared spectroscopy spectra, C-H stretching vibrations of artemether were masked in all prepared samples, while C-H stretching vibrations were representative of polyethylene glycol 6000, Cremophor-A25, and Poloxamer 188. Differential scanning calorimetry showed decreased melting endotherm and increased enthalpy change (ΔH) in both physical mixture and freeze-dried mixtures of all groups. Scanning electron microscopy of freeze-dried mixtures of all samples showed glassy appearance, size reduction, and embedment, while their physical mixture showed size reduction and embedment of artemether by excipients. In group-1, solubility was improved up to 15 times, whereas group-2 showed up to 121 times increase but, in group-3, when Poloxamer 188 was used instead of Cremophor-A25, solubility of freeze-dried mixtures was increased up to 135 times. In fasted state simulated gastric fluid at pH 1.6, the dissolution of physical mixture was increased up to 12 times and freeze-dried mixtures up to 15 times. The stability of artemether was substantially enhanced in freeze-dried mixtures by using polyethylene glycol 6000, Cremophor-A25, and Poloxamer 188 of self-emulsified solid dispersions of artemether in Hank's balanced salt solution at pH 7.4.

Authors+Show Affiliations

Faculty of Pharmacy, Bahauddin Zakariya University, Multan 6000, Pakistan.Faculty of Pharmacy, Bahauddin Zakariya University, Multan 6000, Pakistan.Faculty of Pharmacy, Bahauddin Zakariya University, Multan 6000, Pakistan.Faculty of Pharmacy, Bahauddin Zakariya University, Multan 6000, Pakistan.College of Pharmacy, University of the Punjab, Lahore 54000, Pakistan.College of Pharmacy, University of the Punjab, Lahore 54000, Pakistan.Department of Environmental Sciences, COMSATS Institute of Information Technology, Abbottabad 22060, Pakistan.Department of Chemistry, COMSATS Institute of Information Technology, Abbottabad 22060, Pakistan.Department of Pharmacy, COMSATS Institute of Information Technology, Abbottabad 22060, Pakistan.

Pub Type(s)

Journal Article
Research Support, Non-U.S. Gov't

Language

eng

PubMed ID

26097842

Citation

Ansari, Muhammad Tayyab, et al. "Preparation and Characterization of Solid Dispersions of Artemether By Freeze-Dried Method." BioMed Research International, vol. 2015, 2015, p. 109563.
Ansari MT, Hussain A, Nadeem S, et al. Preparation and Characterization of Solid Dispersions of Artemether by Freeze-Dried Method. Biomed Res Int. 2015;2015:109563.
Ansari, M. T., Hussain, A., Nadeem, S., Majeed, H., Saeed-Ul-Hassan, S., Tariq, I., Mahmood, Q., Khan, A. K., & Murtaza, G. (2015). Preparation and Characterization of Solid Dispersions of Artemether by Freeze-Dried Method. BioMed Research International, 2015, 109563. https://doi.org/10.1155/2015/109563
Ansari MT, et al. Preparation and Characterization of Solid Dispersions of Artemether By Freeze-Dried Method. Biomed Res Int. 2015;2015:109563. PubMed PMID: 26097842.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Preparation and Characterization of Solid Dispersions of Artemether by Freeze-Dried Method. AU - Ansari,Muhammad Tayyab, AU - Hussain,Altaf, AU - Nadeem,Sumaira, AU - Majeed,Humaira, AU - Saeed-Ul-Hassan,Syed, AU - Tariq,Imran, AU - Mahmood,Qaisar, AU - Khan,Abida Kalsoom, AU - Murtaza,Ghulam, Y1 - 2015/05/17/ PY - 2014/05/23/received PY - 2014/07/15/revised PY - 2014/08/10/accepted PY - 2015/6/23/entrez PY - 2015/6/23/pubmed PY - 2016/3/19/medline SP - 109563 EP - 109563 JF - BioMed research international JO - Biomed Res Int VL - 2015 N2 - Solid dispersions of artemether and polyethylene glycol 6000 (PEG6000) were prepared in ratio 12 : 88 (group-1). Self-emulsified solid dispersions of artemether were prepared by using polyethylene glycol 6000, Cremophor-A25, olive oil, Transcutol, and hydroxypropyl methylcellulose (HPMC) in ratio 12 : 75 : 5 : 4 : 2 : 2, respectively (group-2). In third group, only Cremophor-A25 was replaced with Poloxamer 188 compared to group-2. The solid dispersions and self-emulsified solid dispersions were prepared by physical and freeze dried methods, respectively. All samples were characterized by X-ray diffraction, attenuated total reflectance Fourier transform infrared spectroscopy, differential scanning calorimeter, scanning electron microscopy, and solubility, dissolution, and stability studies. X-ray diffraction pattern revealed artemether complete crystalline, whereas physical mixture and freeze-dried mixture of all three groups showed reduced peak intensities. In attenuated total reflectance Fourier transform infrared spectroscopy spectra, C-H stretching vibrations of artemether were masked in all prepared samples, while C-H stretching vibrations were representative of polyethylene glycol 6000, Cremophor-A25, and Poloxamer 188. Differential scanning calorimetry showed decreased melting endotherm and increased enthalpy change (ΔH) in both physical mixture and freeze-dried mixtures of all groups. Scanning electron microscopy of freeze-dried mixtures of all samples showed glassy appearance, size reduction, and embedment, while their physical mixture showed size reduction and embedment of artemether by excipients. In group-1, solubility was improved up to 15 times, whereas group-2 showed up to 121 times increase but, in group-3, when Poloxamer 188 was used instead of Cremophor-A25, solubility of freeze-dried mixtures was increased up to 135 times. In fasted state simulated gastric fluid at pH 1.6, the dissolution of physical mixture was increased up to 12 times and freeze-dried mixtures up to 15 times. The stability of artemether was substantially enhanced in freeze-dried mixtures by using polyethylene glycol 6000, Cremophor-A25, and Poloxamer 188 of self-emulsified solid dispersions of artemether in Hank's balanced salt solution at pH 7.4. SN - 2314-6141 UR - https://www.unboundmedicine.com/medline/citation/26097842/Preparation_and_Characterization_of_Solid_Dispersions_of_Artemether_by_Freeze_Dried_Method_ L2 - https://doi.org/10.1155/2015/109563 DB - PRIME DP - Unbound Medicine ER -