Russian Journal of Applied Chemistry, 2013, Vol. 86, No. 5, pp. 782−786.
Pleiades Publishing, Ltd., 2013.
Original Russian Text © M.V. Sardushkin, K.I. Kienskaya, E.V. Il’yushenko, G.V. Avramenko, 2013, published in Zhurnal Prikladnoi Khimii, 2013, Vol. 86,
No. 5, pp. 835−839.
AND POLYMERIC MATERIALS
Fabrication of Rifampicin Microcapsules
with a Polylactide Shell
M. V. Sardushkin, K. I. Kienskaya, E. V. Il’yushenko, and G. V. Avramenko
Mendeleev University of Chemical Technology of Russia, Moscow, Russia
Received March 27, 2013
Abstract—Procedure for encapsulation of rifampicin by evaporation of a volatile solvent was developed. An ef-
fective stabilizer making it possible to reach a 23% incorporation of the main substance into capsules was selected.
The basic microcapsule parameters (particle size distribution, degree of polydispersity, and electrokinetic potential)
were determined. The kinetics of rifampicin release from microcapsules was examined.
The fabrication of microencapsulated medicinal
preparations has been described in sufﬁ cient detail [1,
2]. Preparations of this kind have speciﬁ c properties
predetermining their application ﬁ eld. Among their
main properties should be named the prolonged action
and possible protection of a medicinal substance
from the external medium, which is topical, e.g., for
protein and peptide preparations [3, 4]. The possible
microencapsulation of a number of biologically active
substances has been demonstrated previously [5, 6].
However a large interest of numerous researchers
has been attracted recently by the problem of
microencapsulation of a number of antibiotics, especially
those of antituberculous type. The development of new
preparation of preparations for curing of tuberculosis
is necessitated by the rise in the drug resistance of
micobacteria causing the disease. The semisynthetic
broad-spectrum antibiotic rifampicin (RFP) is a
comparatively new preparation that belongs to the
ﬁ rst line in chemotherapy of tuberculosis, but causes
a number of toxicoallergic reactions. One of possible
ways to diminish the constitutional toxic reactions and
reduce the chemotherapy duration is by inhalational
administration of microencapsulated forms of the
The goal of the study was to develop a procedure for
RFP encapsulation for inhalational administration.
Microcapsules of rifampicin were fabricated by
evaporation of a volatile solvent, chloroform. The choice
of chloroform as the solvent is due to the possibility of
its application in pharmaceutical industry at satisﬁ ed
requirements to its residual content in the ﬁ nal product
. In the ﬁ rst stage of microencapsulation, an oil-
in-water emulsion was produced with a Nissei AM-
11 homogenizer. In this emulsion, the role of the oil
phase was played by a solution of the active substance,
rifampicin, and a ﬁ lm-forming agent, polylactide
(PLA), in chloroform, and the aqueous phase contained
preliminarily dissolved stabilizers: OT aerosol (AOT),
which is sodium bis(2-ethylhexyl) sulfosuccinate
(anionic surfactant) and polyvinyl alcohol (PVA). In the
second stage, chloroform was evaporated in a vacuum
from the emulsion stable during several hours, with a
polymeric shell thus formed on the surface of drops.
The choice of PLA as the ﬁ lm-forming agent is due to
its nontoxic nature and biodegradability. The resulting
suspension of microcapsules was separated by ﬁ ltration.
The process scheme is shown in Fig. 1.
The particle size distribution was determined by