Volume 6, Issue 1, January – 2021 International Journal of Innovative Science and Research Technology

ISSN No:-2456-2165

Design Formulation and Evaluation of Transdermal

Patch of Aspirin Using Polymer Variation
Devina Chandra, Hakim Bangun, UripHarahap
Departement of Pharmacy, Universitas Sumatera Utara, Indonesia.

Abstract:- Oral aspirin treatment in the secondary bioavailability [5]. Giving aspirin orally can cause
prevention of heart and cerebral vascular disease is well gastrointestinal mucosal damage to bleeding, due to
known. However, oral administration can cause damage inhibition of cyclooxygenase which limits clinical use as a
to the gastrointestinal mucosa until bleeding occurs. primary and secondary prevention of cardiovascular disease
These problems can be overcome by development of and can lead to treatment discontinuation [6].
transdermal drug delivery system. The objective of this
study was to develop and evaluate the transdermal Transdermal delivery offers an alternative route for
patches of aspirin.Giving aspirin by transdermal patch administration of aspirin that is more convenient and safer
with matrix type to increase the antithrombotic for long-term use of low-dose aspirin as a primary and
efficiency of aspirin. The principle of making secondary prevention of cardiovascular disease; and inhibits
transdermal patches by solvent evaporation with aspirin platelet function by maintaining the inhibitory effect of
and polymer such as Eudragit RS 100, Eudragit RL 100, COX-2 and minimizing the vascular effect of COX-1, so
Ethyl Cellulose, Polyvinyl pyrrolidone, and that aspirin therapy can be used without risk to the
Polyvinylacetate. The prepared formulations were gastrointestinal tract.Aspirin is polar at physiological pH
uniform in their physical characteristics. The and rapidly hydrolyzes to salicylic acid in the skin, making
formulation F1-F4, combination of polymer (Eudragit it not a good candidate for transdermal delivery. However, a
RL 100 :EudragitRS 100) showed better performance. low dose of aspirin is needed per day to suppress platelet
The results specify that aspirin transdermal patch can be COX [6].
designed for obtaining better therapeutic benefits.
Therefore, efforts are needed to improve the
Keywords :- Aspirin; Polymers; Eudragit; Ethyl Cellulose; bioavailability of drugs administered transdermally by
Polyvinyl pyrrolidone; Polyvinylacetate. formulating aspirin into transdermal patch preparations with
the aim of increasing the therapeutic effect, safety and
I. INTRODUCTION stability, and to deliver controlled doses of drugs through
the skin within a certain period of time. Transdermal patch
In 2013, cardiovascular disease accounted for 800,937 is a drug delivery system that can distribute drugs to
of 2,596,993 deaths and is the number five death in the systemic circulation with controlled release rates using
United States [1]. Cardiovascular disease is one of the main polymers [7].
causes of morbidity and mortality worldwide, so the
development of effective drugs for the prevention and In general, the patch formulation method is divided
treatment of these diseases has increasingly attracted into 2 types of systems, namely the matrix system and the
worldwide attention [2]. membrane system [8]. This research will use a matrix
system type that can regulate the release of active medicinal
Platelet anti-agregration and anti-inflammatory have ingredients from patch preparations by considering the type
played an important role in the prevention and treatment of of polymer to be used [9]. In addition, the formed patch is
myocardial infarction and thrombosis since the 1970s [2]. thin and elegant so it is comfortable to use. [10].
Evidence-based has shown that anti-platelet therapy such as
aspirin is a common management in the management of II. MATERIALS AND METHODS
vaso-occlusive events such as stroke, myocardial infarction,
and coronary artery disease; can reduce the incidence rate of 2.1 Materials
25% in heart, brain and peripheral thromboembolic disease; Aspirin, Ethyl Cellulose, Polyvinyl pyrrolidone, and
and is a major contributor to primary and secondary Polyvinylacetate were purchasedfrom ASEAN Indonesia.
prevention of cardiovascular disease [3]. Eudragit RL 100 and RS 100 were kindly gifted by IMCD
Indonesia. All other chemical were of analytical or higher
Aspirin given orally requires high doses and is grade.
frequent because aspirin undergoes extensive pre-systemic
hydrolysis in the intestine and liver to salicylic acid and thus 2.2 Formulation of Transdermal Patch
has no antiplatelet activity [4]. Aspirin is rapidly absorbed in To determine the optimum combination of polymers,
the acidic environment of the stomach and alkaline in the plasticizer and solvents, placebo films were formulated.
small intestine, resulting in less than 50% of oral Matrix type transdermal patch of Aspirin were prepared by

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Volume 6, Issue 1, January – 2021 International Journal of Innovative Science and Research Technology
ISSN No:-2456-2165
solvent evaporation technique using different proportions of Folding endurance was determined by repeatedly
polymers like Eudragit RS 100, RL 100, Ethyl Cellulose, folding a small strip of patches at the same place till it
Polyvinyl pyrrolidone, and Polyvinylacetate in beaker glass, broke. The number of times patches could be folded at the
then add diethyl phthalate as plasticizer, while stirring using same place, without breaking gave the value of folding
a magnetic stirrer for 2 hours. The mixture was prepared in a endurance and it was recorded.
homogeneous dispersion, under slow stirring under
magnetic stirrer for 2 hours. After that, it was poured in e. Moisture content
aluminum foil and dried at room temperature for 24 hours. The patches were accurately weighed and kept in a
desiccator containing calcium chloride 24 hrs. Then
Table 1. Composition of Transdermal Patch theconcluding weight was noted. It can be calculated by
Formulati Dru Polyme Rati Plasticiz Solve following formula
on Code g r o er (w/w) nt
Initial Weight−Final Weight
(w/w % Moisture content = 𝑥 100%
𝐹𝑖𝑛𝑎𝑙 𝑊𝑒𝑖𝑔ℎ𝑡
)
F1 30 ERL 3 : 1 Propylen Ethan
f. Drug content
100 : e glycol ol
A specified area 2x2 of patch was dissolved in
ERS
mixtureof ethanol. It was closed and magnetic stirrer for 24
100
hours in a shaker. The resulting solutionwas filtered and the
F2 30 ERL 3:1 Diethyl Ethan
amount of drug present in the filtered was determined by
100 : Phthalate ol
using UV-VIS spectrophotometer at 528 nm.
ERS
100
Organoleptic properties of the drug were found within
F3 30 ERL 1: 0 Propylen Ethan
limits as shown in Table 2.
100 : e glycol ol
ERS
Table 2: Organoleptic Properties of Transdermal Patch
100
Formulation Color State Odor
F4 30 ERL 1:0 Diethyl Ethan
Code
100 : Phthalate ol
F1 Transparent Less Odorless
ERS
Crystalline
100
F2 Transparent Less Odorless
F5 30 EC : 3 : 1 Propylen Ethan
Crystalline
PVP e glycol ol
F3 Transparent Less Odorless
F6 30 EC : 3:1 Diethyl Ethan
Crystalline
PVP Phthalate ol
F4 Transparent Less Odorless
F7 30 PVA : 1 : 0 Propylen Ethan
Crystalline
PVP e glycol ol
F5 White to off More Odorless
F8 30 PVA : 1:0 Diethyl Ethan
white Crystalline
PVP Phthalate ol
F6 White to off More Odorless
white Crystalline
2.3 Evaluation of Transdermal Patch
F7 White to off More Odorless
All the prepared transdermal patches were evaluated
white Crystalline
by the following parameters:
F8 White to off More Odorless
a. Physical appearance white Crystalline
All the prepared patches were visually inspected for
color, clarity, entrapment of any air bubble, flexibility The formulated patch at F1 until F4 were found to be
andsmoothness. transparent, smooth, uniform, less crystalline and odorless,
while F5 until F8 were found to be white, uniform, more
b.Thickness crystalline and odorless. All formulated patches were found
Thickness of the patch was measured by using screw free from entrapment of air bubble.
micrometer at five different points and average thickness
was determined. The thickness of the transdermal patches for 8
different polymer ratio varied from 0.154±0.005 to
c. Weight variation 0.182±0.002 mm. Low standard deviation values indicates
5 patches from each formulation were weighed that all the prepared patches were are nearly uniform
individually and the average weight was calculated. The thickness. The results are given in table 3.
individualweight should not deviate significantly from the
average weight. The weight of the transdermal patches for 8 different
polymer ratio varied from 67.133±0.208 mg to
d.Folding endurance 68.633±0.208 mg. The variation in weight uniformity of the

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Volume 6, Issue 1, January – 2021 International Journal of Innovative Science and Research Technology
ISSN No:-2456-2165
prepared patches was within acceptable range. The results REFERENCES
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III. CONCLUSION

Preparation transdermal patches of aspirin have been

successfully by solvent evaporation technique. Evaluation of
the prepared patches in terms oforganoleptic, weight,
thickness, moisture content and drug content uniformity
recommend that the method employed for formulation of the
transdermal patches was reproducible and assured
outstanding quality and uniformity in patch characteristics
with least variability.

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