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Name (Title):
Kohsaku Kawakami (MANA Researcher, Senior Researcher)
Affiliation:
International Center for Materials Nanoarchitectonics
(MANA) and Biomaterials Center, NIMS
Address:
1-1 Namiki, Tsukuba. Ibaraki 305-0044, Japan
Email: KAWAKAMI.Kohsaku@nims.go.jp
Home Page: http://www.nims.go.jp/bmc/group/ndg/kawakami/
Presentation Title:
Electrospray Deposition as a New Method for Preparing Fine Drug Particles
Poster Session PB-3
Abstract:
Although there has been much discussion on favorable physicochemical properties for drug
candidates over the last decade, formulators must still deal with many challenging compounds
including poorly soluble drugs. A novel formulation technology, electrospray deposition method,
is introduced in this presentation. This method enabled amorphization and micronization of the
formulation, both of which contribute to improvement of the solubility, in one-step preparation
procedure.
Electrospray Deposition (called as “Electrospinning” in polymer science field) has been
regarded as a promising method to prepare various fibrous materials such as filters, sensors, and
many types of biomedical materials. Various poorly soluble drugs including predonisolone
(PDN), phenylbutazone, phenytoin and carbamazepine were dissolved with polymeric carriers
including polyvinylpyrroridone (PVP), Eudragid E-100, and polyethylene glycol either in ethanol
or in its aqueous solution. The solutions were introduced to 8-pin manifold using a syringe pump,
followed by application of high voltage, typically in the range of 10-25 kV, to produce
electrospray to a stainless steel target. The setup was enclosed in an air- tight box to control
humidity of the environment. The dried particles were collected from the target surface.
Figure shows an example of the SEM picture of the particles prepared by this method.
Typically, the particle had very unique shape with its size of around a few micrometer. The unique
shape might be elucidated in terms of rapid formation of the polymer film on the droplet surface,
followed by removal of the solvent and the shrinkage of the droplet. The particle was in the
amorphous state in most cases except that crystal
structure was obtained when carbamazepine was
used as a model drug. In that case, the unique shape
was lost to form almost spherical shape, probably
because of the molecular rearrangement after the
deposition. The greatest advantage of this method
as a formulation technology is that it can be
operated at ambient temperature, because other
methods for preparing amorphous formulations
require very severe conditions such as high
temperature that may cause degradation of the
drug.
Figure: Particles of PVP/PDN=1/1(w/w)
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