Utilization of a sol-gel method for encapsulation of doxorubicin.
The sol-gel pre-doping method was used to encapsulate doxorubicin in silica gels and optimum conditions of preparation of drug-loaded gel were established, ensuring both reproducible and effective results of quantitative encapsulation of doxorubicin and its gradual but complete release. Doxorubicin was encapsulated in polysiloxane polymers using the method based on sol-gel encapsulation without a catalyst, with an acid catalyst (HCl) and a base catalyst (NH3). The time of gelation of the gel loaded with doxorubicin, encapsulation efficiency of the drug and the degree of release of the drug from the gel are all affected by the kind of catalyst (acidic or basic) or its absence at the gel preparation stage, and the temperature of the gelation process. The time of sol gelation when using the NH3 or HCl catalyst was 9 days at 21 degrees C, 2 days at 30 degrees C and 1.5 days at 37 degrees C, while for the gel prepared without a catalyst it was 90 days at 21 degrees C, 75 days at 30 degrees C and 70 days at 37 degrees C. The efficiency of doxorubicin encapsulation was 99.5 +/- 0.5% (w/w) for acid-catalyzed gel, 98.9 +/- 1.01% (w/w) for base-catalyzed gel and 86.4 +/- 11.6% (w/w) for non-catalyzed gel. A 100% (w/w) release of doxorubicin by diffusion through pores was found only in the case of base-catalyzed gel after a 140-h incubation time. For acid-catalyzed gel and non-catalyzed gel, the total amounts of released doxorubicin after 140 h of incubation were 3-5% (w/w) and 9-11% (w/w), respectively. The stability of doxorubicin encapsulated in the three kinds of gel matrices was found to be improved compared to the stability of a free form of the drug in solution.
Prokopowicz
Magdalena
M
Division of Physical Chemistry with Instrumental Analysis Laboratory, Medical Academy of Gdańsk, Hallera 107, 80-416 Gdańsk, Poland. mprokop@biology.pl
Lukasiak
Jerzy
J
Przyjazny
Andrzej
A
D002021:Buffers; D002214:Capsules; D004317:Doxorubicin / Q000737:chemistry* / Q000493:pharmacokinetics; D004339:Drug Compounding / Q000379:methods*; D004355:Drug Stability; D005782:Gels; D015203:Reproducibility of Results
D002021:Buffers; D002214:Capsules; D005782:Gels; D004317:Doxorubicin