Gastroresistant microcapsules: new approaches for site-specific delivery of ketoprofen

Figures & data

Table 1.  Composition (w/w percentage) of the different microcapsule formulations containing ketoprofen.

	A	B	C	D	E	F	G	H
Ketoprofen	12.5	12.5	12.5	12.5	12.5	5.0	5.0	5.0
Castor oil	23.4	23.4	23.4	23.4	23.4	45.0	—	30.0
Mint essence	11.6	11.6	11.6	11.6	11.6	—	45.0	15.0
Arabic gum	50.0	40.0	40.0	40.0	35.0	35.0	35.0	35.0
Eudragit^® L100	—	10.0	—	5.0	7.5	7.5	7.5	7.5
Eudragit^® S100	—	—	10.0	—	—	—	—	—
Stearic acid	—	—	—	5.0	7.5	7.5	7.5	7.5

Table 2.  Ketoprofen (w/w percentage) solubilized in the different excipients.

Excipients	% Ketoprofen solubilized
Mineral oil	0.02
Olive oil	1.10
Wheat germ oil	1.40
Fish oil	4.70
Castor oil	10.00
Castor oil/Mint essence (2:1, w/w)	25.00
Mint essence	30.00

Figure 1.  Size distribution of the different spray-dried microcapsules.

Figure 2.  SEM image of microcapsules coated with Eudragit^® L100 (A: formulation B) and microcapsules coated with Eudragit^® L100 and stearic acid (B: formulation D).

Table 3.  Droplet mean diameter (± SD) after emulsion reconstitution by means of DLS analysis.

	A	B	C	D	E	F	G	H
Droplet mean diameter	850 ± 15	843 ± 11	854 ± 16	891 ± 11	882 ± 9	863 ± 5	872 ± 8	875 ± 8

Figure 3.  Release profile of ketoprofen from the different microcapsules at pH 1.2 (A) and pH 7.6 (B): A (×); B (□); C (Δ); D (⋄), and E (ℴ). The SD did not exceed the 5%.

Figure 4.  Effect of the different core material on apparent permeability (P_app) of ketoprofen across the rat ileum.