International Journal of PharmTech Research

CODEN (USA): IJPRIF ISSN : 0974-4304

Vol.3, No.4, pp 2215-2221, Oct-Dec 2011

Formulation and Evaluation of Fluconazole

Soap Strips for Dermal infections
Swati Jagdale*, Dhaval Bhavsar, Mahesh Gattani, Swapnil Borse, Aniruddha
Chabukswar

MAEER’s Maharashtra Institute of Pharmacy, S.No. 124,MIT Campus, Paud Road,

Kothrud, Pune-411038, MS, India

*Corres. Author: jagdaleswati@rediffmail.com

Tel. No. +91 9881478118.

Abstract: In present study, antifungal paper soap strips of fluconazole were prepared & evaluated for dermal
infections because the presence of thick foam on the infected part causes hydration of stratum corneum for better
penetration of drug. The formulation and evaluation of medicated soap strips were carried out in two phases.
Phase-I studies optimization, which was carried out to study water absorption capacity using different types of
papers (Whatman filter paper no. 1, 41 and 42, filter paper, bond paper and butter paper) by determining the
parameters weight gain, size, shape and foam test. From these parameters best soap, concentration of liquid soap
solution and papers were selected. Phase-II studies involve incorporation of drug in best soap solution and papers
chosen from phase-I studies. The medicated soap strips were prepared by dipping the selected paper in drug
containing soap solution. The prepared medicated paper soap strips were characterized for weight gain, foam test,
drug content uniformity, FTIR, in vitro drug release studies using diffusion cell with hydrated cellophane
membrane and primary skin irritation test. The microbial studies indicate drug activity by zone of inhibition against
microorganisms C.albicans, S.typhi, S.aureus, E.coli, klibsiella, B.subtilis, P.aeroginosa, A.niger and A.fumigatus
species. The obtained results for prepared medicated soap strip of fluconazole indicate that these strips are
economic, convenient, gives good foam on application, uniform in drug content and not showing any skin
irritation.
Keywords: - Dermal infections, fluconazole, thick foam, hydration of stratum corneum, medicated paper soap
strips.

INTRODUCTION corneum for better penetration of drug5-9. Topical drug

Fluconazole is an antifungal azole. It is a broad
spectrum antifungal, first approved in Europe in 1988
and then in America in 1990. It was the first single
dose treatment approved for vaginal candidiasis.
Fluconazole is an effective agent in the treatment and
prophylaxis of Candidal infection1-4.Presence of thick
foam on the infected part causes hydration of stratum
delivery systems are available including medicated
soaps having disadvantages like their economy,
wastage, no accurate dosage, no proper foam
formation etc. Hence the aim for present work was to
prepare medicated soap strips which will be more
effective against dermal infections.
Swati Jagdale et al /Int.J. PharmTech Res.2011,3(4)
MATERIALS AND METHODS
Materials
Fluconazole was obtained from Nicholas Piramal as a
gift sample. Soap X & soap Y were purchased from
local market. Filter paper & Whatman filter paper no.
1, 41 & 42 were from New Neeta chemicals. Butter
paper & bond paper were purchased from local market.
Methods
1. PHASE-I
Selection of soap solution
Two non-medicated soaps of different brands were
selected and coded as X and Y. Soap solution of varied
concentration (5, 10, 15, 20% w/v) were prepared.
Formation of foam was avoided during solution
preparation. Foam test was the criteria for selection of
good soap. The soap capable of producing maximum
foam was selected.
Selection of paper
Six different branded papers (Whatman filter paper no.
1, 41 and 42, filter paper, bond paper and butter paper)
were selected and coded as A, B, C, D, E, and F. They
were evaluated for their absorption capacity and
weight gain. The paper showing maximum absorbing
capacity was considered as the best paper.
Formation of non medicated paper soap strips
The paper soap strips were prepared by Dipping
technique using modified disintegration apparatus and
air dried overnight at 37±2°C. For this purpose
different papers were dipped one after another into the
soap solution of varied concentration (5, 10, 15, 20%
w/v) and air dried overnight.
Evaluation of non-medicated paper soap strips
The prepared strips were subjected for determination
of size, shape, weight variation, pH and foam test by a
reported standard method and an average of 20 strips
was taken.
2. PHASE-II
Formulation of medicated paper soap strips
The drug was incorporated in the selected formulation
which showed good absorption capacity in phase-I
studies. Accurately weighed drug (2% fluconazole)
was mixed with 15% soap powder and distilled water
was added under constant and continuous stirring until
2216
a uniform soap-drug solution was formed. Then paper
soap strips were prepared.
Evaluation of paper soap strips
These prepared medicated soap strips were evaluated
for weight gain, foam test, pH, in vitro drug release
and primary skin irritation test. Microbial studies have
been done by using microorganisms like C.albicans,
S.typhi, S.aureus, E.coli, K.pneumoniae, P.aeroginosa,
B.subtilis and A.niger species. The % drug content is
measured by using UV spectroscopy at λmax 278 nm.
In vitro drug release9-12
In vitro drug release of fluconazole from prepared
soap strips was studied by using Keshary-Chien
diffusion cell. Prehydrated Cellophane paper was used
as a membrane in this study. The study was done by
using 0.1 N HCl media. The samples were collected at
the interval of 3 minutes for a period of 15 minutes.
The drug content was estimated by measuring the
absorbance at 278 nm.
% Drug content
The % drug content is measured by using UV
spectroscopy at λmax 278 nm.
Primary skin irritation test
For this, three human volunteers were selected and the
prepared soap strips were given to them and checked
for irritation.
Microbial study13
Microbial study has been done using microorganisms
such as C.albicans, S.typhi, S.aureus, E.coli, klibsiella,
B.subtilis, P.aeroginosa, A.niger and A.fumigatus
species. For measuring the effectiveness of an
antimicrobial agent against fungi/bacteria grown in
culture, the microorganism of interest was swabbed
uniformly across a culture plate. Then a soap strip of
5×5 mm was placed on the surface of the agar. Then
the plates were placed in incubator for 24 hrs at
30˚C.The drug diffuses out from the paper soap strip
into the agar. The concentration of the compound will
be higher next to the strip, and will decrease gradually
as distance from the strip increases.
IR spectral analysis for drug-excipient intraction14
The studies were carried out using IR method with the
help of IR (Varian) spectrophotometer.
Swati Jagdale et al /Int.J. PharmTech Res.2011,3(4) 2217

Table 1: Formulation of fluconazole soap strips Table 2: Evaluation parameters of miconazole soap
Sr. Ingredients Quantity taken No. strips
Sr. Parameters 2% Miconazole
1 Soap Y 15 gm each No. soap strips
1. Weight variation 0.1 ± 0.01 gm
2 Fluconazole 2 gm 2. Foam height 17 ± 0.02 ml
3 Distilled water 100 ml 3. % drug content 96 ± 5.0 %
4. pH 7.0

Table 3: Zone of inhibition obtained in microbial studies

Sr. Micro-organism Diameter of Zone of inhibition(cm)
No. Strip A Strip B Strip F
1 A.niger 2.9 ± 0.1 2.6 ± 0.2 0.0 ± 0.2
2 A.fumigatus 2.5 ± 0.2 3.3 ± .02 1.4 ± 0.1
3 C.albicans 3.3 ± 0.2 3.5 ± 0.3 1.1 ± 0.2
4 B.subtilus 3.8 ± 0.3 3.9 ± 0.3 0.4 ± 0.1
5 S.typhi 2.1 ± 0.3 1.9 ± 0.4 0.8 ± 0.1
6 E.coli 1.8 ± 0.1 2.4 ± 0.1 0.8 ± 0.1
7 S.aureus 4.0 ± 0.4 3.6 ± 0.4 0.0 ± 0.1
8 P.klebsiella 2.1 ± 0.2 2.6 ± 0.2 1.5 ± 0.1
9 B.aureginosa 2.3 ± 0.1 2.1 ± 0.2 0.6 ± 0.1

Figure 1: Foam height produced by different non- Figure 2: Weight gain of different non-medicated
medicated paper soap strips. paper
FOAM TEST WEIGHT GAIN

16 0.12
(ml)

14 0.1
12
(g)

0.08
hight

gain

10 X
X
weig

8 Y 0.06 Y
ht

6
0.04
Foa

4
m

0.02
2
0 0
A B C D E FA B
A B C D E FA B
C DE F A B C D E F
C D E F A B C D E F
5% 10% 15%
5% 10% 15%

Figure 3: In vitro drug release study of fluconazole soap strips.

Swati Jagdale et al /Int.J. PharmTech Res.2011,3(4) 2218

Figure 4: Zone of inhibition against various micro-organisms

Swati Jagdale et al /Int.J. PharmTech Res.2011,3(4) 2219

Figure 5: IR spectral analysis of fluconazole

Figure 6: IR spectral analysis of soap

soap
100

2355.375 471.513
1040.990 10.016
95 490.224 0.00
1917.761 68.945
% T rans m itta nc e

3499.620 747.062
90

2114.819 -0.049 1190.906 660.797

85 610.454 0.000

2497.978 847.029 1678.997 353.533

80

75 2920.867 191.828 883.109 185.655

1460.319 1926.331

3800 3600 3400 3200 3000 2800 2600 2400 2200 2000 1800 1600 1400 1200 1000 800 600 400
Wavenumber
Swati Jagdale et al /Int.J. PharmTech Res.2011,3(4) 2220

Figure 7: IR spectral analysis of mixture of fluconazole and soap

100 fluco.+soap 2116.789 0.000

3463.244 0.000
95 2533.298 4.492 1925.869 89.493

90 1006.386 74.469

85
1244.528 0.000 570.295 13.532
% T ra ns m ittan c e

80
3381.928 0.000
75 2356.061 649.346
2717.585 130.139

70

3063.508 632.904 612.092 0.000

65
1699.028 650.741
2931.911 520.877 874.711 0.000
60 1606.910 398.080 1504.239 357.681
1140.924 58.428

3800 3600 3400 3200 3000 2800 2600 2400 2200 2000 1800 1600 1400 1200 81000 600 400
Wavenumber

RESULTS AND DISCUSSION Microbial study

Microbial study has been done using microorganisms
1. Non medicated soap strips
such as C.albicans, S.typhi, S.aureus, E.coli, klibsiella,
From the several papers studied the papers coded A, B B.subtilis, P.aeroginosa, A.niger and A.fumigatus
and F found to have optimum absorption capacity. The species. It gave zone of inhibition against all of the
solution of 15% Y soap was found good. All the strips microorganisms. The diameters of zone of inhibition
have pH near about 7.0. obtained in microbial testing by different strips against
2. Medicated soap strips various micro-organisms are given in table 3.
The medicated soap strips found uniform in drug IR spectral analysis for drug-excipient interaction
content, weight variation was found to be in the range
The unsubstituted peaks in IR spectra indicate that
and foam produced was ranging from 15 to 18 ml. The
15% soap solutions gave best results for foam, weight there is no interaction between drug and soap.
gain, pH and uniformity of soap distribution as shown CONCLUSION:
in figure 1 and 2.
From the prepared medicated soap strips, the strips of
In vitro drug release paper encoded B (Whatman filter paper no. 41) shows
In vitro drug release studies show the 100% drug the best results as compared to other selected papers.
released within 10 minutes as shown in figure 3. The medicated soap strips show excellent release
within 10 minutes indicating good efficiency and
Primary skin irritation test
penetration. The prepared medicated soap strips are
Primary skin irritation test showed none of the convenient to use and new type of dosage form for
medicated soap strip produces irritation. dermal infections such as candidiasis, aspergillus. It is
useful the patients of all ages and sex.
Swati Jagdale et al /Int.J. PharmTech Res.2011,3(4) 2221

REFERENCES 9) Rao KP, Patil AB, Reddy H, Sagre P. “Design of

ketoconazole soap strips for dermal infections”,
1) Beale JM, Block JH. “Wilson and Gisvold’s The Pharma Review, 2008; 133-136.
Textbook of organic, medicinal and 10) Carr MM, Pryce DM, Ive FA. “Treatment of
pharmaceutical chemistry”, Wolters Kluwer seborrhoeic dermatitis with ketoconazole:
(India) Pvt. Ltd: New Delhi, 12th ed., 2011; Response of seborrhoeic dermatitis of scalp to
pp:203. topical ketoconazole”, Br J Dermatol., 1987;
2) Tripathi KD. “Essentials of medical 116; 2: 213-16.
pharmacology”, Jaypee Brothers Medical 11) Farr PM, Shuster S. “Treatment of seborrhoeic
Publishers: New Delhi, 6th ed., 2008; pp:763. dermatitis with topical ketoconazole”, Lancet.,
3) Barar FSK. “Essentials of 1984; 2: 1271-72.
Pharmacotherapeutics”, S. Chand and company 12) Green CA, Farr PM, Shuster S. “Treatment of
Ltd: New Delhi, 5th ed., 2009; pp:505. seborrhoeic dermatitis of the face, scalp and
4) http://en.wikipedia.org/wiki/fluconazole. trunk to topical ketoconazole Response of
5) Banker GS, Rhodes CT. “Modern seborrhoeic dermatitis of the face, scalp and
Pharmaceutics”, Marcel Dekker Inc: New York, trunk to topical ketoconazole”, Br J Dermatol.,
4th ed., 2002; pp:190. 1987; 116: 217-21.
6) Montagna W. “The structure and function of 13) Kokare CR. “Pharmaceutical microbiology
skin”, Academic Press: New York, 3rd ed., principles and applications”, Nirali Prakashan;
1974; pp:10. Pune, 2008; pp:19.4-19.5.
7) Misra AN. Transdermal Drug Delivery In: Jain 14) Indian Pharmacopoeia, Controller Publications:
NK editors. “Controlled and novel drug Delhi, vol. І, 2010; pp:333.
delivery”, CBS publishers and Distributors: New
Delhi, 1st ed., 1997; pp:100-127.
8) Indian Standard “Shampoo, Soap based-
specification” (first revision). IS7669-1990:
Bureau of Indian standards.1996; NO-AnnexaB-
2; pp:2-4.

*****
Formulasi dan Evaluasi Strip Sabun Flukonazol untuk infeksi Dermal

1. Abstrak: Dalam penelitian ini, strip sabun antijamur flukonazol disiapkan & dievaluasi untuk
dermal infeksi karena keberadaan busa tebal pada bagian yang terinfeksi menyebabkan hidrasi
stratum korneum menjadi lebih baik penetrasi obat. Formulasi dan evaluasi sabun strip obat
dilakukan dalam dua fase.Tahap-I studi optimasi, yang dilakukan untuk mempelajari kapasitas
penyerapan air menggunakan berbagai jenis kertas (kertas saring Whatman no. 1, 41 dan 42,
kertas saring, kertas bond dan kertas mentega) dengan menentukan parameter penambahan berat
badan, ukuran, bentuk dan uji busa. Dari parameter tersebut sabun terbaik, konsentrasi sabun cair
solusi dan makalah dipilih. Studi fase-II melibatkan penggabungan obat dalam larutan sabun dan
kertas terbaik dipilih dari studi fase-I. Strip sabun obat disiapkan dengan mencelupkan kertas
yang dipilih dalam obat mengandung larutan sabun. Strip sabun kertas obat yang disiapkan
dicirikan untuk penambahan berat badan, tes busa, keseragaman kandungan obat, FTIR, penelitian
pelepasan obat in vitro menggunakan sel difusi dengan plastik terhidrasi membran dan uji iritasi
kulit primer. Studi mikroba menunjukkan aktivitas obat berdasarkan zona inhibisi terhadap
mikroorganisme C.albicans, S.typhi, S.aureus, E.coli, klibsiella, B.subtilis, P.aeroginosa, A.niger
dan A.fumigatusspecies. Hasil yang diperoleh untuk strip sabun obat flukonazol yang disiapkan
menunjukkan bahwa strip ini ekonomis, nyaman, memberikan busa yang baik pada aplikasi,
seragam dalam kandungan obat dan tidak menampilkan kulit apa pun gangguan.

2. Alat dan bahan :

Alat :
a. Spektroskopi UV
b. Kertas saring
c. kertas saring Whatman no. 1, 41 & 42
d. Kertas mentega
e. kertas bond
Bahan :
a. Flukonazol
b. Sabun X
c. Sabun Y
3. Metode
1. fase-I
a. Pemilihan larutan sabun
Dua sabun non-medicated dari berbagai merek dipilih dan dikodekan sebagai X dan
Y. Solusi Sabun konsentrasi bervariasi (5, 10, 15, 20% b / v) disiapkan. Pembentukan
busa dihindari selama persiapan solusi. Tes busa adalah kriteria untuk pemilihan sabun
yang baik. Sabun yang mampu menghasilkan busa maksimal dipilih.
b. Pemilihan kertas
 Enam kertas bermerek yang berbeda (kertas saring Whatman no. 1, 41 dan 42, kertas
saring, kertas bond dan kertas mentega) dipilih dan dikodekan sebagai A, B, C, D, E,
dan F. Mereka dievaluasi untuk kapasitas penyerapan mereka dan penambahan berat
badan. Kertas yang menunjukkan daya serap maksimum dianggap sebagai kertas
terbaik.
c. Pembentukan strip sabun kertas non obat
Strip sabun kertas disiapkan dengan teknik Pencelupan menggunakan alat disintegrasi
yang dimodifikasi dan udara kering semalam pada 37 ± 2 ° C. Untuk tujuan ini kertas
yang berbeda dicelupkan satu demi satu ke dalam larutan sabun dengan konsentrasi
bervariasi (5, 10, 15, 20% b / v) dan udara kering semalam.
d. Evaluasi strip sabun kertas non-obat
Strip yang disiapkan menjadi sasaran untuk penentuan ukuran, bentuk, variasi berat,
pH dan uji busa dengan metode standar yang dilaporkan dan rata-rata 20 strip diambil.
2. fase-II
Formulasi strip sabun kertas obat. Obat itu dimasukkan dalam formulasi yang dipilih
yang menunjukkan kapasitas penyerapan yang baik dalam studi fase-I. Obat yang ditimbang
secara akurat (2% flukonazol) dicampur dengan 15% bubuk sabun dan air suling
ditambahkan di bawah pengadukan konstan dan kontinu sampai larutan sabun-obat yang
seragam dibentuk. Kemudian strip sabun kertas disiapkan.
a. Evaluasi strip sabun kertas
Ini strip sabun obat disiapkan dievaluasi untuk kenaikan berat badan, tes busa, pH,
pelepasan obat in vitro dan uji iritasi kulit primer. Studi mikroba telah dilakukan dengan
menggunakan mikroorganisme seperti C.albicans, S.typhi, S.aureus, E.coli,
K.pneumoniae, P.aeroginosa, B.subtilis dan A.niger spesies. Isi obat% diukur dengan
menggunakan spektroskopi UV pada λmax 278 nm.
b. Rilis obat in vitro9-12
Pelepasan obat flukonazol secara in vitro dari strip sabun yang disiapkan dipelajari
dengan menggunakan sel difusi Keshary-Chien. Kertas Cellophane prahidrasi digunakan
sebagai membran dalam penelitian ini. Penelitian dilakukan dengan menggunakan 0,1 N
HCl media. Sampel dikumpulkan pada interval 3 menit untuk jangka waktu 15 menit.
Kandungan obat diperkirakan dengan mengukur absorbansi pada 278 nm.
c. % Konten obat
Isi obat% diukur dengan menggunakan spektroskopi UV pada λmax 278 nm.
d. Tes iritasi kulit primer
Untuk ini, tiga sukarelawan manusia dipilih dan strip sabun disiapkan diberikan
kepada mereka dan diperiksa untuk iritasi.
e. Studi mikro13
Studi mikroba telah dilakukan menggunakan mikroorganisme seperti C.albicans,
S.typhi, S.aureus, E.coli, klibsiella, B.subtilis, P.aeroginosa, A.niger dan A.fumigatus
 spesies. Untuk mengukur efektivitas agen antimikroba terhadap jamur / bakteri yang
ditanam dalam kultur, mikroorganisme yang tertarik diseka secara seragam di seluruh
lempeng budaya. Kemudian strip sabun 5 × 5 mm ditempatkan pada permukaan agar-
agar. Kemudian piring ditempatkan dalam inkubator selama 24 jam pada 30˚C. Obat
berdifusi keluar dari strip sabun kertas ke dalam agar. Konsentrasi senyawa akan lebih
tinggi di sebelah strip, dan akan berkurang secara bertahap saat jarak dari strip
meningkat.
f. IR spektral analisis untuk obat-excipient intraction14
Studi dilakukan menggunakan metode IR dengan bantuan spektrofotometer IR
(Varian).
4. Evaluasi
a. Kenaikan berat badan
b. Uji ph
c. Tes busa
d. Pelepasan obat in vitro dan
e. Uji iritasi kulit primer

5. Formulasi
Sabun Y 15 gram
Sabun X 15 gram
Fluconazole 2 gm
Air suling 100 ml

6. Hasil dan pembahasan

1. strip sabun Non obat
Dari beberapa makalah yang dikaji makalah yang diberi kode A, B dan F ditemukan
memiliki kapasitas penyerapan yang optimal. Solusi dari 15% sabun Y ditemukan
baik. Semua strip memiliki pH sekitar 7,0.
2. Strip sabun obat
Strip sabun obat ditemukan seragam dalam kandungan obat, variasi berat ditemukan
berada di kisaran dan busa yang dihasilkan berkisar 15-18 ml. Larutan sabun 15%
memberikan hasil terbaik untuk busa, berat badan, pH dan keseragaman distribusi
sabun seperti yang ditunjukkan pada gambar 1 dan 2.

a. Pelepasan obat in vitro

Studi rilis obat in vitro menunjukkan obat 100% dilepaskan dalam 10 menit
seperti yang ditunjukkan pada gambar 3.
b. Tes iritasi kulit primer
 Uji iritasi kulit primer menunjukkan tidak ada sabun yang menghasilkan
iritasi.
c. Studi mikroba
Studi mikroba telah dilakukan menggunakan mikroorganisme seperti
C.albicans, S.typhi, S.aureus, E.coli, klibsiella, B.subtilis, P.aeroginosa,
A.niger dan A.fumigatus spesies. Ini memberi zona penghambatan terhadap
semua mikroorganisme. Diameter zona inhibisi yang diperoleh dalam
pengujian mikroba oleh strip yang berbeda terhadap berbagai mikro-organisme
diberikan dalam tabel 3.
d. Analisis spektral IR untuk interaksi eksipien.
Puncak yang tidak disubstitusi dalam spektrum IR menunjukkan bahwa
tidak ada interaksi antara obat dan sabun.

7. Kesimpulan
Dari strip sabun obat yang disiapkan, potongan kertas yang disandikan B (kertas saring
Whatman no. 41) menunjukkan hasil terbaik dibandingkan dengan kertas terpilih lainnya. Strip
sabun obat menunjukkan pelepasan yang sangat baik dalam 10 menit menunjukkan efisiensi dan
penetrasi yang baik. Strip sabun medicated yang disiapkan mudah digunakan dan jenis sediaan
baru untuk infeksi kulit seperti kandidiasis, aspergillus. Ini berguna bagi pasien segala usia dan
jenis kelamin.