eBook: How a CDMO Can Help Overcome LNP & Liposome Challenges - 6

Figure 3A. In-vitro dissolution of ASD-005 liposomal formulation.
Table 3. Short-term physical stability of F3 formulation
at different temperatures.
1 month at 40°C/75%RH, room temperature, and 5°C
(Table 3).
In-Vitro Dissolution & In-Vivo Study
In-vitro dissolution of liposomal
ASD-005 was
conducted in PBS buffer with 0.5%w/v Tween 80 under
a pH of 6.5 and a temperature of 37°C (Figure 3). An invitro
sustained-release profile of ASD-005 from those
formulations was demonstrated for up to 48 hours. The
PK data of those liposomal formulations after IV bolus
injection in rats confirmed the in-vivo sustained-release
properties of the ASD-005 liposomal formulations for
at least 24 hours, whereas the IV solution of the ASD005
compound is rapidly cleared from the rat body
within 4 hours (Figure 3A & 3B).
Summary
The study shows encapsulation of ASD-005 into a
liposomal formulation with a nano-size range of 100
nm to 150 nm and with good physical stability. DSC
thermogram indicated that ASD-005 is present inside
the liposomal formulation as an amorphous form.
Parenteral administration of liposomal ASD-005
Figure 3B. In-vivo sustained-release PK profile of ASD-005 liposomal
formulations versus IV solution.
has a rapid onset effect of lowering hypertension
followed by sustained release of the drug inside the
animal body for at least 24 hours. Thus, the ASD-005
liposomal formulation avoids the rapid clearance
that was experienced with the IV solution of the
ASD-005 compound. The results of the present
investigations suggest that the liposomal form
of ASD-005 present an attractive sustained drug
delivery for effective parenteral treatment of acute
hypertension and congestive heart failure.
Acknowledgement
The author would like to thank the following
scientists for their contributions of the scientific data
generated under Ascendia's labs: Drs. Vera Ivanova,
Kaoru Tominaga, and Zhao Liu.
6

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