Design of amphotericin B oral formulation for antifungal therapy

Figures & data

Figure 1. Structure of amphotericin B.

Figure 2. The oral absorption mechanisms of nanoparticles in intestinal tract.

Table 1. In vivo release profiles of AmB from various oral formulation.

Formulation	Excipient	Animal	Dose	C max (ng/mL)	T max (h)	AUC
Nanosuspensions	Deoxycholate sodium	–	–	–	–	–
Nanosuspensions	Tween 80/Pluronic F68	–	–	–	–	–
Nanocrystals	Tween 80/poloxamer188	–	–	–	–	–
Nanoparticles	PLGA	Rat	10 mg/kg	176.0 ± 25.8	24	7938.8 ± 1450.7AUC0–inf (ng h/mL)
Nanoparticles	GCPQ	Beagle	4 mg/kg per 2 days	250	4	–
Nanoparticles	Hitosan	–	–	–	–	–
SLN	Emulsynt® GDL/ Epikuron™ 200	Rat	200 mg/kg	124.93 ± 13.61	9	6063.311AUC0–∞ (ng h/mL)
Liposomes	Yolk phosphatidylcholine	–	–	–	–	–
Cubosomes	Phytantriol	Rat	10 mg/kg	316.7 ± 32.6	26.0 ± 4.9	17 002.2 ± 3400.3AUC0 − 120 (ng h/mL)
Cubosomes	Glyceryl monoolein	Rat	10 mg/kg	286.4 ± 35.1	25.1 ± 3.7	11 749.1 ± 2231.2AUC0 − 120 (ng h/mL)
Emulsion	Mono/diglyceridephospholipid	Rat	50 mg/kg	96 ± 15	12.5 ± 2.7	1534 ± 229AUC0–24 (ng h/mL)
Cochleate	Phosphatidylserine	Rat	10 mg/kg × 15d	51.1 ± 5.8	–	–

Figure 3. Freeze–fracture electron micrographs of oral AmB nanocochleates (Thornton & Wasan, 2009).

Figure 4. Atomic force microscopy images of oral AmB emulsion (Thornton & Wasan, 2009).

Thornton SJ , Wasan KM. (2009). The reformulation of amphotericin B for oral administration to treat systemic fungal infections and visceral leishmaniasis. Expert Opin Drug Deliv 6:271–84

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