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Abstract: Mucoadhesive microcapsules of
rosiglitazone were prepared using sodium alginate as a
shell forming polymer and Carbapol 940, HPMC, Sodium CMC
as mucoadhesive polymer for the potential use of
treating acute and chronic diabetes mellitus (Type II
diabetes). Large spherical microcapsules with a coat
consisting of alginate and a mucoadhesive polymer could
be prepared by orifice-ionic gelation process. The
microcapsules exhibited good mucoadhesive properties in
an in-vitro test. Rosiglitazone release from these
mucoadhesive microcapsules was slow and extended over
longer periods of time and depending on the composition
of the coat. Drug release was diffusion controlled and
followed zero-order kinetic.
Introduction
Rosiglitazone, a member of the thiazolidinedione class
of antidiabetic agents, improves glycemic control by
improving insulin sensitivity while reducing circulating
insulin levels. Rosiglitazone is a highly selective and
potent agonist for the peroxisome proliferator-activated
receptor-gamma (PPARg). In humans, PPAR receptors are
found in key target tissues for insulin action such as
adipose tissue, skeletal muscle and liver. Activation of
PPARg nuclear receptors regulates the transcription of
insulin-responsive genes involved in the control of
glucose production, transport, and utilization. In
addition, PPARg-responsive genes also participate in the
regulation of fatty acid metabolism.
Microencapsulation has been accepted as a process to
achieve controlled release and drug targeting.
Mucoadhesion has been a topic of interest in the design
of drug delivery system to prolong the residence time of
the dosage form at the site of application or the
absorption and to facilitate intimate contact dosage
form with the underlying absorption surface to improve
and enhance the bioavailability of drugs. Therefore
control release (CR) products are needed for
Rosiglitazone, to improve duration of action and patient
compliance.
Material and methods
Materials
Rosiglitazone was supplied by Sun Pharma limited, India
as a gift sample, sodium carboxy methylcellulose (sodium
CMC) was kindly provided by Stadmed Private LTD.
(Kolkata, India), Hydroxypropylmethylcellulose (HPMC)
was a gift sample from Colorcon Asia PVT, LTD.(Verna,
India). All other ingredients used were of analytical
grade and used as provided. Spectrophotometeric studies
carried out by using double beam UV spectrophotometer,
Pharmaspac 1700, Shimadzu, Japan.
Methods
Preparation of mucoadhesive microcapsules
Microcapsules are prepared by orifice- ionic gelation
method. Sodium alginate and mucoadhesive polymer are
dissolved in purified water to form a homogenous polymer
solution. The active substance, Rosiglitazone is added
to polymer solution and mixed thoroughly with a stirrer
to form a viscous dispersion with different polymer and
different concentration (Table-1). The resulting
dispersion is then added manually drop wise into CaCl2
(10% w/v) solution through a syringe with a needle of
size no. 18. The added droplets are related in the CaCl2
solution for 15 min to complete the curing reactions and
to produce spherical rigid microcapsule. The
microcapsules are collected by decantation, and the
product thus separated, washed repeatedly with water and
dried at 45˚C for 12 hrs.
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