Utjecaj kompleksacije piroksikama s ciklodekstrinima na oblikovanje gela

Scientific paper - Original scientific paper

• Title (english): Influence of cyclodextrin complexation on piroxicam gel formulations
• Author: Mario Jug
• Author: Mira Becirevic-Lacan
• Author: Aan Kwokal
• Author: Biserka Cetina-Cizmek
• Author's institution: University of Zagreb; Faculty of Pharmacy and Biochemistry; (Department of pharmaceutical technology)
• Scientific / art field, discipline and subdiscipline: BIOMEDICINE AND HEALTHCARE; Pharmacy; Pharmacy

Abstract (croatian)

Svrha rada bila je ispitati utjecaj kompleksacije piroksikama s ciklodekstrinima na oblikovanje pripravaka za topičku primjenu lijeka. Kompleksi piroksikama s β- i nasumično metiliranim β-ciklodekstrinom u krutom stanju pripremljeni su metodom sušenja
smrzavanjem i karakterizirani su diferencijalnom pretražnom kalorimetrijom, difrakcijom X-zraka na prahu, infracrvenom spektroskopijom s Fourierovim transformacijama, te spektroskopijom u niskom infracrvenom području. Fizička smjesa lijeka s ciklodekstrinima karakterizirana je poboljšanom topljivošću u usporedbi sa čistim lijekom zbog stvaranja kompleksa in situ. Kompleksacija piroksikama sa ciklodekstrinima dodatno je poboljšala topljivost lijeka u liofiliziranom kompleksu. Ispitan je utjecaj ciklodekstrina na permeaciju lijekova iz vodenih disperzija i pripremljenih gelova s hidroksipropil metilcelulozom. Permeacija lijekova uključuje više uzastopnih procesa: otapanje krute faze, difuziju lijeka kroz izbubreni polimerni matriks, te difuziju lijeka kroz polupropusnu membranu. Kompleksacija piroksikama s ciklodekstrinima povećala je difuzibilnost lijeka uslijed porasta količine lijeka raspoloživog za difuziju. Difuzija lijeka kroz izbubreni
polimerni matriks hidroksipropil metilceluloze pokazala se ključnim procesom koji određuje ukupnu difuziju lijeka. Interakcija hidrofilnog polimera s ciklodekstrinima utjecala je na fizikalno-kemijska svojstva gela, posebice na reološke parametere.

Abstract (english)

The aim of this work was to evaluate the role of cyclodextrins in topical drug formulations. Solid piroxicam (PX) complexes with beta-cyclodextrin (beta-CD) and randomly methylated beta-cyclodextrin (RAMEB) were prepared by freeze-drying and characterized using differential scanning calorimetry (DSC), X-ray powder diffractometry (XRPD), Fourier transform infrared spectroscopy (FTIR) and near infrared spectroscopy (NIR). A physical mixture of PX and cyclodextrins was characterized by enhanced dissolution properties compared to the dissolution profile of the pure drug due to in situ complex formation. Formation of the PX-cyclodextrin inclusion complex additionally improved the drug dissolution properties. Influence of CDs on drug permeation from the water dispersion and the prepared hydroxypropyl methylcellulose (HPMC) gels was investigated. Permeation of the drug involved three consecutive processes: dissolution of the solid phase, diffusion across the swollen polymer matrix and drug permeation through the membrane. Complexation increased PX diffusion by increasing the amount of diffusible species in the donor phase. Slower drug diffusion through the HPMC matrix was the rate limiting step in the overall diffusion process. Possible interaction between the hydrophilic polymer and cyclodextrin may result in physicochemical changes, especially in a change of rheological parameters.

• Keywords (croatian): piroksikam; hidroksipropil metilceluloza; ciklodekstrin; topička primjena
• Keywords (english): piroxicam; hydroxypropyl methylcellulose; cyclodextrin; topical delivery
• Language: croatian
• Language: english
• Publication type: Scientific paper - Original scientific paper
• Publication status: Published
• Peer review: Peer review - international
• Publication version: Published version
• Journal title: Acta Pharmaceutica
• Numbering: vol. 55, no. 3, pp. 223-236
• p-ISSN: 1330-0075
• e-ISSN: 1846-9558
• URN:NBN: urn:nbn:hr:163:266337
• Publication: 2005
• Document URL: https://hrcak.srce.hr/16760
• Type of resource: Text
• Access conditions: Open access
• Created on: 2020-04-08 15:27:35