In Vitro and In Vivo testing of 3D-Printed Amorphous Lopinavir Printlets by Selective Laser Sinitering : Improved Bioavailability of a Poorly Soluble Drug
© 2024. The Author(s), under exclusive licence to American Association of Pharmaceutical Scientists..
The aim of this paper was to investigate the effects of formulation parameters on the physicochemical and pharmacokinetic (PK) behavior of amorphous printlets of lopinavir (LPV) manufactured by selective laser sintering 3D printing method (SLS). The formulation variables investigated were disintegrants (magnesium aluminum silicate at 5-10%, microcrystalline cellulose at 10-20%) and the polymer (Kollicoat® IR at 42-57%), while keeping printing parameters constant. Differential scanning calorimetry, X-ray powder diffraction, and Fourier-transform infrared analysis confirmed the transformation of the crystalline drug into an amorphous form. A direct correlation was found between the disintegrant concentration and dissolution. The dissolved drug ranged from 71.1 ± 5.7% to 99.3 ± 2.7% within 120 min. A comparative PK study in rabbits showed significant differences in the rate and extent of absorption between printlets and compressed tablets. The values for Tmax, Cmax, and AUC were 4 times faster, and 2.5 and 1.7 times higher in the printlets compared to the compressed tablets, respectively. In conclusion, the SLS printing method can be used to create an amorphous delivery system through a single continuous process.
Medienart: |
E-Artikel |
---|
Erscheinungsjahr: |
2024 |
---|---|
Erschienen: |
2024 |
Enthalten in: |
Zur Gesamtaufnahme - volume:25 |
---|---|
Enthalten in: |
AAPS PharmSciTech - 25(2024), 1 vom: 24. Jan., Seite 20 |
Sprache: |
Englisch |
---|
Beteiligte Personen: |
Kayalar, Canberk [VerfasserIn] |
---|
Links: |
---|
Themen: |
2494G1JF75 |
---|
Anmerkungen: |
Date Completed 26.01.2024 Date Revised 10.04.2024 published: Electronic Citation Status MEDLINE |
---|
doi: |
10.1208/s12249-023-02729-y |
---|
funding: |
|
---|---|
Förderinstitution / Projekttitel: |
|
PPN (Katalog-ID): |
NLM367580608 |
---|
LEADER | 01000caa a22002652 4500 | ||
---|---|---|---|
001 | NLM367580608 | ||
003 | DE-627 | ||
005 | 20240410232431.0 | ||
007 | cr uuu---uuuuu | ||
008 | 240125s2024 xx |||||o 00| ||eng c | ||
024 | 7 | |a 10.1208/s12249-023-02729-y |2 doi | |
028 | 5 | 2 | |a pubmed24n1371.xml |
035 | |a (DE-627)NLM367580608 | ||
035 | |a (NLM)38267637 | ||
040 | |a DE-627 |b ger |c DE-627 |e rakwb | ||
041 | |a eng | ||
100 | 1 | |a Kayalar, Canberk |e verfasserin |4 aut | |
245 | 1 | 0 | |a In Vitro and In Vivo testing of 3D-Printed Amorphous Lopinavir Printlets by Selective Laser Sinitering |b Improved Bioavailability of a Poorly Soluble Drug |
264 | 1 | |c 2024 | |
336 | |a Text |b txt |2 rdacontent | ||
337 | |a ƒaComputermedien |b c |2 rdamedia | ||
338 | |a ƒa Online-Ressource |b cr |2 rdacarrier | ||
500 | |a Date Completed 26.01.2024 | ||
500 | |a Date Revised 10.04.2024 | ||
500 | |a published: Electronic | ||
500 | |a Citation Status MEDLINE | ||
520 | |a © 2024. The Author(s), under exclusive licence to American Association of Pharmaceutical Scientists. | ||
520 | |a The aim of this paper was to investigate the effects of formulation parameters on the physicochemical and pharmacokinetic (PK) behavior of amorphous printlets of lopinavir (LPV) manufactured by selective laser sintering 3D printing method (SLS). The formulation variables investigated were disintegrants (magnesium aluminum silicate at 5-10%, microcrystalline cellulose at 10-20%) and the polymer (Kollicoat® IR at 42-57%), while keeping printing parameters constant. Differential scanning calorimetry, X-ray powder diffraction, and Fourier-transform infrared analysis confirmed the transformation of the crystalline drug into an amorphous form. A direct correlation was found between the disintegrant concentration and dissolution. The dissolved drug ranged from 71.1 ± 5.7% to 99.3 ± 2.7% within 120 min. A comparative PK study in rabbits showed significant differences in the rate and extent of absorption between printlets and compressed tablets. The values for Tmax, Cmax, and AUC were 4 times faster, and 2.5 and 1.7 times higher in the printlets compared to the compressed tablets, respectively. In conclusion, the SLS printing method can be used to create an amorphous delivery system through a single continuous process | ||
650 | 4 | |a Journal Article | |
650 | 4 | |a amorphous solid dispersion | |
650 | 4 | |a dissolution | |
650 | 4 | |a lopinavir | |
650 | 4 | |a pharmacokinetics | |
650 | 4 | |a printlets | |
650 | 4 | |a selective laser sintering | |
650 | 7 | |a Pharmaceutical Preparations |2 NLM | |
650 | 7 | |a Lopinavir |2 NLM | |
650 | 7 | |a 2494G1JF75 |2 NLM | |
650 | 7 | |a Excipients |2 NLM | |
700 | 1 | |a Helal, Nada |e verfasserin |4 aut | |
700 | 1 | |a Mohamed, Eman M |e verfasserin |4 aut | |
700 | 1 | |a Dharani, Sathish |e verfasserin |4 aut | |
700 | 1 | |a Khuroo, Tahir |e verfasserin |4 aut | |
700 | 1 | |a Kuttolamadom, Mathew A |e verfasserin |4 aut | |
700 | 1 | |a Rahman, Ziyaur |e verfasserin |4 aut | |
700 | 1 | |a Khan, Mansoor A |e verfasserin |4 aut | |
773 | 0 | 8 | |i Enthalten in |t AAPS PharmSciTech |d 2000 |g 25(2024), 1 vom: 24. Jan., Seite 20 |w (DE-627)NLM126699429 |x 1530-9932 |7 nnns |
773 | 1 | 8 | |g volume:25 |g year:2024 |g number:1 |g day:24 |g month:01 |g pages:20 |
856 | 4 | 0 | |u http://dx.doi.org/10.1208/s12249-023-02729-y |3 Volltext |
912 | |a GBV_USEFLAG_A | ||
912 | |a GBV_NLM | ||
951 | |a AR | ||
952 | |d 25 |j 2024 |e 1 |b 24 |c 01 |h 20 |