Original Article

Preparation and in vitro and in vivo Evaluation of

Chitosan-Gliclazide Mucoadhesive Microparticles
by an Emulsification-Desolvation-Crosslinking
Technique
Pabbiniddi Veera Lakshmi1, Kora Pattabhi Rama Chowdary2,*, Avula Prameela Rani3, Sahini Venkata
Uma Maheswara Prasad1
1
School of Pharmacy, JNTUK College, Kakinada, Andhra Pradesh, INDIA.
2
Vikas Institute of Pharmaceutical Sciences, Rajahmundry, Andhra Pradesh, INDIA.
3
University College of Pharmaceutical Sciences, Acharya Nagarjuna University (ANU), Guntur, Andhra Pradesh, INDIA.

ABSTRACT
Introduction: Recently much emphasis is being laid on the development of microparticles
because of their potential benefits such as increased bioavailability, reduced risk
of systemic toxicity, reduced risk of local irritation and predictable gastric emptying.
Objective: The objective of the present study is to prepare and evaluate mucoadhesive
microparticles of chitosan-gliclazide for oral controlled release. Methods: A new method
namely emulsification-desolvation-crosslinking was used for the preparation of chitosan-
gliclazide microparticles and the microparticles were evaluated by in vitro and in vivo
methods. Results: Spherical chitosan-gliclazide microparticles could be prepared by
the emulsification-desolvation-crosslinking method. The method was reproducible
with regard to size and size distribution of the microparticles. The chitosan-gliclazide
microparticles exhibited good muoadhesive property. Gliclazide release from the chitosan
microparticles was slow and extended over longer periods of time and depended on
the proportion of core: coat. Gliclazide release from the chitosan microparticles was
by diffusion mechanism. Microparticles (F3) prepared using a core: coat ratio of 8:2
gave slow and controlled release of gliclazide over 12 hr similar to that of commercial
gliclazide SR tablets. In the in vivo evaluation, the gliclazide microparticles (F3) gave a
slower reduction in serum glucose levels and the reduced glucose levels were sustained
over longer periods of time. Conclusion: Microparticles (F3) are considered as a promising
Submission Date: 18-07-2018;
microparticulate drug delivery system for oral controlled release of gliclazide over 12 hr
Revision Date: 27-11-2018;
for b.i.d administration. Accepted Date: 26-07-2019
Key words: Mucoadhesive microparticles, Chitosan, Gliclazide, Emulsification- DOI: 10.5530/ijper.53.4.128
desolvation-crosslinking method, Oral controlled release. Correspondence:
Prof. Kora Pattabhi Rama-
Chowdary,
Chairman BOS in Pharmacy,
INTRODUCTION School of Pharmacy,
JNTUK, Kakinada-533003,
Microparticles and microparticulate drug resins, ethyl cellulose, polystyrene, polyvinyl Andhra Pradesh, INDIA.
Phone: +91-9866283578
delivery systems are topics of current interest acetate, Eudragits, starch acetate, chitosan E-mail: prof.kprchowdary@
in drug delivery. The design, characterization etc. In the present study chitosan, a muco- rediffmail.com

advantages and applications of microparticles adhesive polymer was tried for the prepara-
are reviewed in standard textbooks and tion of microparticles of gliclazide for oral
articles.1-4 Design of microparticles requires controlled release. We have earlier reported5
a suitable polymer to serve the intended the preparation and in vitro evaluation of
purpose. Examples of polymers used for chitosan-gliclazide microparticles.
the preparation of microparticles include Mucoadhesion is a topic of interest in the
cellulose nitrate, cellulose acetate, synthetic design of drug delivery systems and several www.ijper.org

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 Lakshmi, et al.: Design of Chitosan-Gliclazide Mucoadhesive Microparticles

studies reported6-12 mucoadhesive drug delivery systems gliclazide content. Encapsulation efficiency was estimated
in the form of tablets, microcapsules, films, patches and using the equation,
gels for various routes. In the present study mucoad- Estimated drug
hesive microparticles of gliclazide were prepared using content (%)
chitosan. The objective of the present study is to pre- Encapsulation efficiency (%) = × 100
Theoretical drug
pare and evaluate mucoadhesive chitosan-gliclazide mic-
roparticles by in vitro and in vivo methods. content (%)
Gliclazide, a potential second generation short-acting Size Analysis
sulfonylurea13 requires formulation of controlled release
systems for continuous therapeutic effect and better Size distribution analysis was done by sieving using a
range of standard sieves.
patient compliance by reducing the frequency of dosage
administrations. Morphological Characterization by SEM
The surface morphology of microparticles was observed
MATERIALS AND METHODS by scanning electron microscopy. The microparticles
Materials (F3) were vacuum dried. Before observation, samples
were mounted on metal grids using double-sided
Gliclazide was a gift sample from M/s Micro Labs, adhesive tape, coated with gold palladium and observed
Pondicherry. Chitosan, 75-85 percent deacetylated was microscopically using Joel, JSM-6360 LV scanning
obtained from Central Institute of Fisheries Technology, microscope. (Tokyo, Japan).
Cochin, India. Sodium tri polyphosphate (Sigma),
Acetic acid (Qualigens), Chloroform (Qualigens) and Drug Release Study
Soyabean oil were used. All other materials used were Release of gliclazide from the microparticles of size
of pharmacopoeial grade. 30/50 mesh was evaluated in phosphate buffer of pH
7.4 (900 ml) using an 8-station dissolution rate test
Methods
apparatus (model Disso-2000, M/s Lab. India) with a
Estimation of Gliclazide paddle stirrer (Apparatus 2) at 50 rpm and a temperature
of 37°C ± 1°C. A sample of microparticles equivalent
Gliclazide was estimated by measuring absorbance at
to 60 mg of gliclazide was used in each test. Each drug
227 nm in phosphate buffer of pH 7.4. Before using the
release experiment was replicated three times (n=3).
method was validated for linearity range, accuracy,
precision and interference by the excipients. The Analysis of Release Data
method exhibited linearity in the concentration range Drug release data were analyzed as per Zero order,
1 - 10 µg/ ml. The relative error and coefficient of variation First order, Higuchi14 equation and Korsmeyer-Peppas15
(RSD) in the estimation were found to be 0.80% and equation models.
1.2% respectively. No interference by the excipients was
Mucoadhesion Testing by in vitro Wash-Off Test
observed.
The mucoadhesive property of the microparticles (F3)
Preparation of Chitosan-Gliclazide Microparticles was evaluated by an in vitro adhesion testing method
An emulsification-desolvation-crosslinking method known as the wash-off method.16 The mucoadhesiveness
was used for the preparation of chitosan-gliclazide of the microparticles was compared with that of
microparticles, the details of which are as reported nonbioadhesive material, ethylene vinyl acetate micro­
earliar.5 Different proportions of core: coat namely 19:1 particles. Freshly excised pieces of intestinal mucosa
(F1), 9:1 (F2), 8:2 (F3) and 7:3 (F4) were used in the (2 × 2 cm) from sheep were mounted onto glass slides
preparation of chitosan-gliclazide microparticles. The (3 × 1 inch) with cyanoacrylate glue. Two glass slides
purpose of using different proportions of core: coat were connected with a suitable support. Fifty micropar-
was to prepare microparticles with varying amount of ticles were spread onto each wet rinsed tissue specimen
coat polymer and to achieve different release rates. and immediately thereafter the support was hung onto
the arm of a USP tablet disintegrating test machine.
Estimation of Drug Content and Encapsulation When the disintegrating test machine was operated,
Efficiency the tissue specimen was given a slow, regular up-and-
Four samples of 100mg each were taken from each down movement in the test fluid at 37°C contained in
batch of microparticles prepared and assayed for a 1 L vessel of the machine. At the end of 30 min, at
664 Indian Journal of Pharmaceutical Education and Research | Vol 53 | Issue 4 | Oct-Dec, 2019
 Lakshmi, et al.: Design of Chitosan-Gliclazide Mucoadhesive Microparticles

the end of 1 hr and at hourly intervals up to 12 hr, the

machine was stopped and the number of microparticles
still adhering to the tissue was counted. The test was
performed at both gastric pH (0.1N HCl, pH 1.2) and
intestinal pH (phosphate buffer, pH 6.8).
In vivo Evaluation
In vivo evaluation studies were conducted on (1) gliclazide
and (2) mucoadhesive microparticles F3, in normal,
healthy rabbits by measuring serum glucose levels
following their oral administration at a dose equivalent
to 3 mg/kg of gliclazide. The dose for experimental
rabbits was calculated as suggested by Bikash Medhi
and Ajay Prakash.17 The experiments were conducted
as per a crossover randomized block design (n=6).
In vivo study protocols were approved by Institutional
Animal Ethics Committee (No. CPCSEA/CH/
ORG/2015-051). The products were administered
orally the morning following overnight fasting. No Figure 1: SEM of Chitosan- Gliclazide Microparticles, d (F3).
food or liquid other than water was given during the
experimental period. After the zero-hour blood sample particles. The method consists of emulsification of the
(0.5 ml) was collected from the marginal ear vein, the chitosan solution in 1% v/v acetic acid containing the
product in the study was administered orally. Blood dispersed drug particles in an immiscible liquid medium
samples (0.5 mL) were collected from marginal ear vein (soya bean oil containing 10% chloroform) as micro-
at 0.5, 1, 2, 3, 4, 6, 8, 10, 12, 16, 20, 24 hrs after administra- droplets, followed by removal of the acetic acid from
tion. Serum glucose concentrations were determined by a the polymer solution into chloroform by desolvation
known oxidase-peroxidase method18 as described below and crosslinking with tripolyphosphate and glutaraldehyde
employing a glucose kit supplied by Dr. Reddy’s solution to form rigid microparticles. The microparticles
Laboratory, Diagnostic Division, Hyderabad, India.
were found to be discrete, spherical and free flowing.
The method was revalidated and the relative standard
SEM of microparticles F3 is shown in Figure 1.
deviation in the estimated values was found to be 1.2%.
The SEM photographs indicated that the microparticles
Blood samples collected were allowed to clot without
were spherical and completely covered with the coat
any anticoagulant and were centrifuged immediately
polymer. The sizes could be separated readily by sieving
at 5000 rpm for 20 min to separate the serum. To the
and a more uniform size range of microparticles could
serum (0.02 mL) and standard (0.02 mL) in separate
easily be obtained. The size analysis of different batches
clean, dry test tubes, enzyme reagent (2 mL) was added,
of microparticles showed that about 68-75% in each
mixed well and incubated at 37°C for 10 min. The solu-
batch were in the size range 35/50 mesh (398.5µm).
tions were diluted to 5 mL with distilled water and the
The size of the microparticles in the method employed
absorbance of the pink-colored solutions was measured
based on emulsification depends more on the speed of
in a spectrophotometer at 510 nm using a reagent blank.
the stirrer, which was kept constant at 1000 rpm in the
Serum glucose levels (mg/dL) and percentage reduction
preparation of all products. More over the polymer
in serum glucose levels were calculated.
chitosan is rapidly and completely dissolves in acetic
acid solutions forming thin polymer solutions. In such a
RESULTS AND DISCUSSION case the polymer concentration may not be influencing
Chitosan is sparingly soluble in water; practically insoluble the size of microparticles. Hence though the percent
in ethanol (95%) and other organic solvents. Chitosan coat polymer was increased the mean size of the
dissolves readily in dilute and concentrated solutions microparticles remained almost the same. Size analysis
acetic acid. In the present study chitosan was dissolved of three batches of microparticles prepared under iden-
in 1% v/v acetic acid solution. tical conditions indicated reproducibility of the method.
An emulsification-desolvation-crosslinking method5 was Microparticles of the size 35/50 mesh (398.5µm) were
used for the preparation of chitosan-gliclazide micro­ selected for further evaluation.
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 Lakshmi, et al.: Design of Chitosan-Gliclazide Mucoadhesive Microparticles

Table 1: Physical Characteristics of the Microparticles Prepared.

Micro particles Mesh Size Mean size Core: Coat Gliclazide content (%) Encapsu lation Percent Coat
(μm) ratio (x̅±sd) efficiency (%) Polymer
F1 20/35 670 19:1 94.2±1.2 99.0 5.8
35/50 398.5 19:1 94.6±1.8 99.5 5.4
F2 20/35 670 9:1 87.4±1.3 97.1 12.6
35/50 398.5 9:1 87.6±1.1 97.3 12.4
F3 20/35 670 8:2 79.2±1.9 99.0 20.8
35/50 398.5 8:2 79.4±1.6 99.2 20.6
F4 20/35 670 7:3 68.2±1.6 97.4 31.8
35/50 398.5 7:3 68.6±1.5 98.0 31.4

Table 2: Kinetic Parameters (R2 values, Rate constants

and n values) in the Analysis of Release Data as per
Various Kinetic Models.
DDS Zero order First order Higuchi Korsemeyer
Peppas
K0 R2 R2 K1 R2 n R2
F1 11.49 0.6464 0.9855 0.929 0.9003 0.24 0.9929
F2 6.94 0.8380 0.9308 0.506 0.9788 0.40 0.9792
F3 4.53 0.9703 0.9436 0.230 0.9890 0.64 0.9977
F4 3.25 0.9782 0.9793 0.120 0.9825 0.79 0.9881
CP 5.09 0.9602 0.9492 0.262 0.9691 1.00 0.9725

and n values) in the analysis of release data as per

various kinetic models are given in Table 2.
Gliclazide release from all the chitosan microparticles
Figure 2: Gliclazide Release Profiles of Various Microparticles was slow and extended longer periods of time and
Prepared and Commercial SR Tablets (CP).
depended on the proportion of coat in the microparticles.
As the coat proportion was increased the release rate
The physical characteristics of the microparticles prepared was decreased. A good linear relationship was observed
are given in Table 1. Low Coefficient of Variation (CV) between percent coat and release rate, ko (R² = 0.8448).
in percent drug content (< 2.0 %) indicated uniformity The linear relationship could be described by the equation,
y =11.849-0.3035x where x is percent coat and y is
of drug content in each batch of microparticles. The
release rate (ko).
encapsulation efficiency was in the range 97.1 -99.5 %.
The release data of all the formulations obeyed
Drug content of the microparticles was found to be
Korsmeyer Peppas equation model indicating that the
the same in the two sizes, 20/35, 35/50 mesh. A t-test
drug release from the microparticles was by diffusion
of significance indicated that the difference in the drug
mechanism. The release exponent (n) was 0.24 and 0.40
content of the two sizes in each case is not significant
in the case of formulation F1 and F2 respectively
(P>0.05). indicating Fickian diffusion was the release mechanism
Gliclazide release from various microparticles of size from these formulations. In the case of formulation
35/50 was studied in phosphate buffer pH 7.4. For F3 and F4 the release exponent (n) was 0.64 and 0.79
comparison gliclazide release from one commercial respectively indicating non-fickian (anomalous) diffusion
brand of gliclazide SR tablets was also studied. The was the release mechanism from these formulations.
drug release profiles are shown in Figure 2. The release The drug release was by zero order diffusion mechanism
data were analyzed as per Zero order, First order, (n=1.00) in the case of commercial product. Formulation
Higuchi14 equation and Korsmeyer-Peppas15 equation F3 prepared using a core: coat ratio of 8:2 gave slow and
models. The kinetic parameters (r2 values, rate constants controlled release of gliclazide over 12 h similar to that
666 Indian Journal of Pharmaceutical Education and Research | Vol 53 | Issue 4 | Oct-Dec, 2019
 Lakshmi, et al.: Design of Chitosan-Gliclazide Mucoadhesive Microparticles

Table 3: Results of in vitro Wash-Off Test to Assess Table 4: Serum Glucose Levels (mg/dl) observed
Mucoadhesive Properties of the Microparticles Following the Oral Administration of Gliclazide Pure
Prepared. Drug and Its Mucoadhesive Microparticles.
Micro Percentage of Microparticles Adhering to Tissue at Time (h) Serum Glucose Levels (mg/dl) (Percentage
particles Times (h)† Glucose Reduction)
Fluid 0.1N HCL, pH 1.2 Gliclazide Chitosan Gliclazide
F3 1 2 4 6 8 12 (x̅±sd) Microparticles (x̅±sd)
69 (2.2) 62 (1.1) 32 (1.9) 19 (1.5) 15 (1.9) 6 (1.2) 0 99.5±4.2 (0)* 99.8±3.6 (0)*
EVA 52 (2.3) 40 (2.5) 08 (2.7) — — — 0.5 58.4±2.5 (41.3)* 84.8±3.2 (15.0)*
Fluid Phosphate Buffer, pH 6.8 1 44.4±3.2 (55.3) 79.2±2.9 (20.6)
F3 84 (1.0) 82 (0.5) 74 (0.8) 69 (0.5) 65 (0.4) 56 (0.8) 2 51.3±2.8 (48.4) 73.6±3.5(26.2)
EVA 55 (1.5) 41 (1.4) 11 (1.8) — — — 3 59.4±3.1 (40.3) 64.8±3.9 (35.0)
†Figures in parentheses are coefficient of variation values. 4 73.8±3.8 (25.8) 66.2±4.1 (33.6)
6 89.6±4.2 (9.9) 68.4±3.2 (31.4)
of commercial gliclazide SR tablets. The difference factor 8 92.6±4.6 (6.9) 69.6±3.8(30.2)
(f1=2.46) and similarity factor (f2=63.11) indicated that 10 94.2±3.7 (5.3) 71.1±2.9 (28.7)
the drug release profiles of formulation F3 and 12 95.4±4.1 (4.1) 72.8±4.2 (27.0)
commercial SR product are similar. 16 97.2±3.9 (2.3) 84.9±4.6 (14.9)
The results of in vitro wash-off test are given in Table 3. 20 98.1±3.6 (1.4) 87.8±3.9 (12.0)
Microparticles (F3) exhibited good mucoadhesive 24 98.4±4.2 (1.1) 91.5±4.6 (8.3)
properties in the in vitro wash-off test when compared Figures in parentheses are Percentage Glucose Reduction values.
to non-mucoadhesive material, ethylene vinyl acetate
microparticles. The wash-off was slow in the case of periods of time. A 25% reduction in glucose levels is
microparticles (F3) when compared to that of ethylene
considered a significant hypoglycemic effect.20 The
vinyl acetate microparticles (Table 3). The wash-off was
hypoglycemic effect was maintained during the period
faster in gastric pH 1.2 than in intestinal pH 6.8. Ch’ng
from 0.5 hr to 4 hr following the administration of
et al.19 observed that the pH of the medium was critical
gliclazide pure drug, but the hypoglycemic effect was
for the degree of hydration, solubility and mucoadhesion
maintained during the period from 2 hr to 12 hr in the
of the polymers. The relatively rapid wash-off of
microparticles F3 observed at gastric pH 1.2 is due to case of chitosan-gliclazide microparticles. The sustained
ionization and solubility of chitosan at acidic pH. The hypoglycemic effect observed over longer periods of
results of the wash-off test indicated that the micropar- time in the case of microparticles is due to the slow
ticles prepared had good mucoadhesive property. release and absorption of gliclazide over longer periods
of time. The hypoglycemic effect of gliclazide could be
In vivo evaluation sustained over 12 hr with microparticles.
In vivo evaluation of the chitosan-gliclazide mucoad-
hesive microparticles was carried out in healthy, normal CONCLUSION
rabbits by measuring the hypoglycemic effect produced
after their oral administration at a dose equivalent to Chitosan-gliclazide mucoadhesive microparticles could
3 mg/kg of gliclazide, in comparison to gliclazide be prepared by an emulsification–desolvation-cross-
(pure drug) at the same dose. The serum glucose levels linking method. These microparticles exhibited good
estimated and the percentage reduction in glucose levels mucoadhesive property. Gliclazide release from the
following the oral administration of gliclazide pure drug chitosan microparticles was slow and spread over longer
and chitosan–gliclazide microparticles are given in Table 4. periods of time. The drug release depended on the
When gliclazide was administered, a rapid reduction in proportion of core: coat in the microparticles. Gliclazide
serum glucose levels was observed; a maximum reduction release from the chitosan microparticles prepared was
of 55.3% was observed at 1.0 h after administration and by diffusion mechanism. Microparticles (F3) prepared
the glucose levels recovered rapidly to the normal level using a core: coat ratio of 8:2 gave slow and controlled
within 6-8 h. In the case of microparticles, the reduction release of gliclazide over 12 hr similar to that of
in glucose levels was slower; it reached maximum commercial gliclazide SR tablets. In the in vivo evalu-
reduction (35.0%) at 3 h after administration and the ation these microparticles (F3) gave a slower reduction
reductions in glucose levels were sustained over longer in serum glucose levels and the reduced glucose levels
Indian Journal of Pharmaceutical Education and Research | Vol 53 | Issue 4 | Oct-Dec, 2019 667
 Lakshmi, et al.: Design of Chitosan-Gliclazide Mucoadhesive Microparticles

were sustained over longer periods of time. A significant 5. Lakshmi PV, Chowdary KPR, Prameela RA, Ravi SK. Preparation
and Evaluation of Chitosan-Gliclazide Microparticulate Drug Delivery
hypoglycemic effect was maintained during 2-12 hr with Systems by Emulsification- Desolvation-Crosslinking Technique. IAJPS.
these microparticles after their oral administration. As 2018;05(04):2713-20.
such microparticles (F3) are considered as a promising 6. Alejandro S, José DNBS. Mucoadhesive polymers in the design of nanodrug
microparticulate DDS for oral controlled release of delivery systems for administration by nonparenteral routes: A review.
Progress in Polymer Science. 2014;39(12):2030-75.
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ACKNOWLEDGEMENT 2016;98:76-89.
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Cochin for providing the gift samples of gliclazide and
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SUMMARY

The objective of the present study is to prepare and evaluate microparticles of gliclazide using chitosan,
a mucoadhesive polymer for oral controlled release. A new technique namely emulsification-desolvation-
crosslinking method was tried for the preparation of chitosan microparticles and the microparticles were
evaluated by in vitro and in vivo methods. Spherical chitosan- gliclazide microparticles could be prepared by the
emulsification-desolvation-crosslinking method. The method was reproducible with regard to size and size
distribution of the microparticles. The chitosan-gliclazide microparticles prepared exhibited good muoadhe-
sive property. They also exhibited good controlled release characteristics in the in vitro and in vivo evaluation.
Microparticles (F3) are considered as a promising microparticulate drug delivery system for oral controlled
release of gliclazide over 12 hr for b.i.d administration.

668 Indian Journal of Pharmaceutical Education and Research | Vol 53 | Issue 4 | Oct-Dec, 2019
 Lakshmi, et al.: Design of Chitosan-Gliclazide Mucoadhesive Microparticles

PICTORIAL ABSTRACT ABOUT AUTHORS

P. Veera Lakshmi, PhD Scholar in
Jawaharlal Nehru Technological
University, Kakinada, carrying out the
research work under the guidance of Prof.
K P R Chowdary, AU. She has published
7 research articles in reputed national
Journals.

Chowdary, KPR, Retired Principal and

Professor from University College
of Pharmaceutical Sciences, Andhra
University. He is having 43 yrs of
teaching experience. Presently he is a
Research Director in Vikas College of
Pharmaceutical Sciences, Rajahmundry.
Dr. Prameela Rani Avula, Principal
and Professor University College of
Pharmaceutical Sciences Acharya
Nagarjuna University, Nagarjuna Nagar,
Guntur. She is having 26 yrs of teaching
experience.

Cite this article: Lakshmi PV, Chowdary KPR, Rani AP, Prasad SVUM. Preparation and in vitro and in vivo Evaluation
of Chitosan- Gliclazide Mucoadhesive Microparticles by an Emulsification-Desolvation-Crosslinking Technique.
Indian J of Pharmaceutical Education and Research. 2019;53(4):663-9.

Indian Journal of Pharmaceutical Education and Research | Vol 53 | Issue 4 | Oct-Dec, 2019 669