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. 2020 Jan 10;13(2):329.
doi: 10.3390/ma13020329.

Alginate-Based Aerogel Particles as Drug Delivery Systems: Investigation of the Supercritical Adsorption and In Vitro Evaluations

Daria Lovskaya  1 , Natalia Menshutina  1
Affiliations

Alginate-Based Aerogel Particles as Drug Delivery Systems: Investigation of the Supercritical Adsorption and In Vitro Evaluations

Daria Lovskaya et al. Materials (Basel). .

Abstract

The present work focuses on the preparation of alginate-based aerogels in the form of particles for their further study as potential drug delivery systems (solid dosage forms). The dripping method was used to prepare certain gel particles, and supercritical drying was used to obtain final alginate-based aerogel particles. Three model active substances (ketoprofen, nimesulide, loratadine) were impregnated into the obtained aerogels using the supercritical adsorption process. Using the method of X-ray analysis, it was shown that the in the obtained drug-loaded aerogels the corresponding active substances are in an amorphous state, and the stability of this state after six months of storage is confirmed. In vitro dissolution tests for obtained drug-loaded aerogels was performed. For each sample, an appropriate dissolution medium (with certain pH) was determined. In vitro investigations showed the increasing of the release rate for all model active substances. Time was required to release and dissolve 50% of the active drug from drug-loaded aerogels (T1/2), reduced in comparison with pure active drugs in crystalline form. Obtained results provide insight into the application of alginate-based aerogel particles as a drug delivery system to improve pharmacokinetic properties of certain active drugs.

Keywords: X-ray analysis; adsorption; aerogel; amorphization; drug delivery systems; in vitro tests; supercritical fluids.

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Conflict of interest statement

The authors declare no conflict of interest. The funders had no role in the design of the study; in the collection, analyses, or interpretation of data; in the writing of the manuscript; or in the decision to publish the results.

Figures

Figure 1
Figure 1
Scheme of the supercritical reactor. 1—CO2 tank, 2—condenser, 3—piston pump, 4—heater, 5—high pressure reactor, 6—thermal control system, 7—separator, 8—rotameter, PI—manometer, TC—temperature probe, TI—temperature probe.
Figure 2
Figure 2
Ketoprofen structure.
Figure 3
Figure 3
Nimesulide structure.
Figure 4
Figure 4
Loratadine structure.
Figure 5
Figure 5
Scheme of the installation for supercritical adsorption: 1—CO2 tank, 2—heat exchanger, 3—liquid diaphragm pump, 4—high pressure reactors with heating jacket, PI—manometers, TIC—temperature controller with operator panel.
Figure 6
Figure 6
SEM of alginate-based aerogel particles: Single particle (on the left) and outer surface of the particle (on the right).
Figure 7
Figure 7
X-ray diffraction patterns of pristine alginate-based aerogel.
Figure 8
Figure 8
X-ray diffraction patterns of ketoprofen loaded into the alginate-based aerogel: (a) 18.05, (b) 19.36, (c) 26.98 wt%.
Figure 9
Figure 9
X-ray diffraction patterns of nimesulide loaded into the alginate-based aerogel: (a) 5.50, (b) 5.56, (c) 14.96 wt%.
Figure 10
Figure 10
X-ray diffraction patterns of loratadine loaded into the alginate-based aerogel: (a) 24.32, (b) 26.92, (c) 30.55 wt %.
Figure 11
Figure 11
Results of in vitro dissolution test for ketoprofen loaded alginate-based aerogel.
Figure 12
Figure 12
Results of in vitro dissolution test for nimesulide loaded alginate-based aerogel.
Figure 13
Figure 13
Results of in vitro dissolution test for loratadine loaded alginate-based aerogel.
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