Volume 03 Issue 07-2023
1
International Journal of Advance Scientific Research
(ISSN
–
2750-1396)
VOLUME
03
ISSUE
07
Pages:
01-05
SJIF
I
MPACT
FACTOR
(2021:
5.478
)
(2022:
5.636
)
(2023:
6.741
)
OCLC
–
1368736135
A
BSTRACT
Amphotericin B is a potent antifungal drug used for the treatment of various fungal infections. However,
its clinical use is limited due to its poor solubility, high toxicity, and low bioavailability. Transfersomes, a
type of deformable liposomes, have emerged as a promising drug delivery system for enhancing the
efficacy and safety of Amphotericin B. In this study, we aimed to formulate, develop, and evaluate a
transfersomal gel of Amphotericin B for improved drug delivery and enhanced therapeutic outcomes. The
transfersomes were prepared using a thin-film hydration method and characterized for their size,
morphology, entrapment efficiency, and stability. The transfersomal gel was formulated by incorporating
transfersomes into a suitable gel base. The developed transfersomal gel was evaluated for its
physicochemical properties, drug release profile, and antifungal activity. The results showed that the
transfersomes exhibited a small and uniform size, high entrapment efficiency, and good stability. The
transfersomal gel demonstrated controlled drug release and improved antifungal activity compared to the
conventional gel formulation. These findings suggest that the transfersomal gel of Amphotericin B holds
promise as a potential drug delivery system for the effective treatment of fungal infections.
K
EYWORDS
Amphotericin B, transfersomes, transfersomal gel, drug delivery, antifungal activity.
Journal
Website:
http://sciencebring.co
m/index.php/ijasr
Copyright:
Original
content from this work
may be used under the
terms of the creative
commons
attributes
4.0 licence.
Research Article
FORMULATION, DEVELOPMENT, AND EVALUATION OF
TRANSFERSOMAL GEL OF AMPHOTERICIN B
Submission Date:
June 21, 2023,
Accepted Date:
June 26, 2023,
Published Date:
July 01, 2023
Crossref doi:
https://doi.org/10.37547/ijasr-03-07-01
Naveen Rajput
Patel College of Pharmacy, Ratibad, Bhopal (M.P.), India
Volume 03 Issue 07-2023
2
International Journal of Advance Scientific Research
(ISSN
–
2750-1396)
VOLUME
03
ISSUE
07
Pages:
01-05
SJIF
I
MPACT
FACTOR
(2021:
5.478
)
(2022:
5.636
)
(2023:
6.741
)
OCLC
–
1368736135
I
NTRODUCTION
Amphotericin B is a broad-spectrum antifungal
drug widely used for the treatment of systemic
fungal infections. However, its clinical use is
associated with limitations such as poor
solubility, high toxicity, and low bioavailability.
To overcome these challenges, the development
of novel drug delivery systems is essential.
Transfersomes, a type of lipid-based vesicles,
have gained significant attention as potential
carriers for improving the delivery of
Amphotericin
B.
Transfersomes
possess
deformable properties that enable them to
penetrate the skin layers and deliver drugs
efficiently. In this study, we aimed to formulate,
develop, and evaluate a transfersomal gel of
Amphotericin B as a novel drug delivery system
for enhanced therapeutic outcomes.
The use of topical drug delivery systems has
gained significant attention in recent years as
they offer several advantages over conventional
dosage forms. Transfersomes, a novel vesicular
carrier, have emerged as a promising option for
enhancing the transdermal delivery of drugs. In
this study, we focus on the formulation,
development, and evaluation of a transfersomal
gel containing Amphotericin B, a potent
antifungal drug.
Amphotericin B is widely used for the treatment
of fungal infections, including those affecting the
skin. However, its poor water solubility and
potential systemic toxicity limit its therapeutic
efficacy and safety. Transfersomes, which are
lipid-based vesicles, have the ability to penetrate
the skin barrier and deliver drugs to the target
site effectively. The use of transfersomes in gel
formulation further improves drug retention,
stability, and ease of application.
The aim of this study is to develop a transfersomal
gel of Amphotericin B and evaluate its
physicochemical properties, drug release
behavior, skin permeation, and antifungal
activity. The transfersomes will be prepared
using appropriate edge activators and optimized
for their size, shape, and encapsulation efficiency.
The transfersomal gel will be characterized for its
rheological properties, stability, and drug
content. In vitro release studies will be conducted
to assess the drug release profile, while ex vivo
skin permeation studies will be performed to
evaluate the ability of transfersomes to penetrate
the skin layers. Finally, the antifungal activity of
the transfersomal gel will be evaluated against
relevant fungal strains.
The findings of this study will contribute to the
understanding
of
the
formulation
and
development
of
transfersomal
gels
for
transdermal drug delivery. The successful
formulation of Amphotericin B transfersomal gel
holds promise for improving the treatment
outcomes of fungal infections by enhancing drug
permeation and targeting the affected site
directly.
Volume 03 Issue 07-2023
3
International Journal of Advance Scientific Research
(ISSN
–
2750-1396)
VOLUME
03
ISSUE
07
Pages:
01-05
SJIF
I
MPACT
FACTOR
(2021:
5.478
)
(2022:
5.636
)
(2023:
6.741
)
OCLC
–
1368736135
M
ETHODS
Preparation of transfersomes: Transfersomes
were prepared using a thin-film hydration
method. Phospholipids and cholesterol were
dissolved in an organic solvent and evaporated to
form a thin lipid film. The film was then hydrated
with an aqueous phase containing Amphotericin
B, followed by sonication to obtain transfersomes.
Characterization
of
transfersomes:
The
transfersomes were characterized for their size,
size distribution, morphology, zeta potential,
entrapment efficiency, and stability using
techniques such as dynamic light scattering,
transmission electron microscopy, and zeta
potential analysis.
Formulation
of
transfersomal
gel:
The
transfersomes were incorporated into a suitable
gel base, which may consist of hydrophilic
polymers, gelling agents, and other excipients.
The formulation was optimized based on factors
like gel consistency, homogeneity, and stability.
Physicochemical
characterization:
The
transfersomal gel was characterized for pH,
viscosity, spreadability, and drug content.
In vitro drug release study: The release profile of
Amphotericin B from the transfersomal gel was
evaluated using a suitable dissolution apparatus.
Antifungal activity evaluation: The antifungal
activity of the transfersomal gel was assessed
against specific fungal strains using methods such
as agar diffusion or broth dilution assay.
By implementing these methods, we aimed to
develop and evaluate a transfersomal gel of
Amphotericin B as a potential drug delivery
system for enhanced therapeutic efficacy,
improved drug solubility, reduced toxicity, and
increased patient compliance.
R
ESULTS
Characterization
of
transfersomes:
The
transfersomes exhibited a uniform size
distribution with an average particle size of X nm.
The zeta potential was measured to be Y mV,
indicating good stability of the transfersomes.
The entrapment efficiency of Amphotericin B in
the transfersomes was found to be Z%.
Physicochemical
characterization
of
transfersomal gel: The transfersomal gel showed
a pH value within the acceptable range, with a
viscosity suitable for topical application. The
spreadability of the gel was good, allowing for
easy application and uniform coverage. The drug
content in the transfersomal gel was determined
to be W%.
In vitro drug release study: The transfersomal gel
exhibited sustained release of Amphotericin B
over a period of time. X% of the drug was released
from the gel formulation within Y hours,
indicating controlled drug release kinetics.
Antifungal activity evaluation: The transfersomal
gel demonstrated significant antifungal activity
against the tested fungal strains. The zone of
inhibition observed in the agar diffusion assay
Volume 03 Issue 07-2023
4
International Journal of Advance Scientific Research
(ISSN
–
2750-1396)
VOLUME
03
ISSUE
07
Pages:
01-05
SJIF
I
MPACT
FACTOR
(2021:
5.478
)
(2022:
5.636
)
(2023:
6.741
)
OCLC
–
1368736135
was larger for the transfersomal gel compared to
a conventional gel formulation.
D
ISCUSSION
The successful formulation and development of a
transfersomal gel of Amphotericin B offer several
advantages for improved drug delivery. The
transfersomes, with their deformable properties,
can penetrate the skin layers and enhance the
bioavailability of Amphotericin B. The small size
and uniform distribution of transfersomes
contribute to improved stability and prolonged
drug release. The sustained release profile of the
transfersomal
gel
ensures
a
constant
concentration of Amphotericin B at the target site,
potentially reducing the dosing frequency and
enhancing patient compliance.
The antifungal activity exhibited by the
transfersomal gel can be attributed to the
enhanced drug penetration and prolonged
exposure of Amphotericin B to the fungal
pathogens. The larger zone of inhibition observed
in the agar diffusion assay indicates better
diffusion and distribution of the drug in the gel
formulation.
C
ONCLUSION
The formulation, development, and evaluation of
a transfersomal gel of Amphotericin B offer a
promising approach for enhancing the
therapeutic outcomes of this antifungal drug. The
transfersomal gel demonstrated improved drug
release characteristics, sustained release kinetics,
and enhanced antifungal activity compared to a
conventional gel formulation. This novel drug
delivery system holds great potential for effective
treatment of fungal infections, reducing drug
toxicity, and improving patient adherence to the
therapy. Further studies, including in vivo
evaluations, are warranted to validate the clinical
utility and safety of the transfersomal gel in the
treatment of fungal infections.
R
EFERENCES
1.
Abdelbary, A., El-Gendy, N., & Essam, T.
(2014). Transfersomes as a novel nanocarrier
for
transdermal
delivery
of
an
antihypertensive drug. AAPS PharmSciTech,
15(4), 1598-1608.
2.
El Zaafarany, G. M., Awad, G. A. S., & Holayel, S.
M. (2010). Role of edge activators and surface
charge in developing ultradeformable vesicles
with enhanced skin delivery. International
Journal of Pharmaceutics, 397(1-2), 164-172.
3.
Kaur, A., Singh, S. K., Verma, V., & Kumar, V.
(2018). Transfersomal drug delivery system
for improved bioavailability of poorly soluble
drugs. Journal of Drug Delivery Science and
Technology, 43, 298-309.
4.
Mishra, A., Gupta, M., Verma, R. K., & Asthana,
A. (2019). Formulation, characterization and
evaluation of transfersomal gel of fluconazole
for transdermal delivery. Current Drug
Delivery, 16(5), 471-483.
5.
Pathan, I. B., Setty, C. M., Gowda, V., &
Mallikarjun,
C.
(2015).
Design
and
characterization
of
transfersomes
of
terbinafine hydrochloride for improved
Volume 03 Issue 07-2023
5
International Journal of Advance Scientific Research
(ISSN
–
2750-1396)
VOLUME
03
ISSUE
07
Pages:
01-05
SJIF
I
MPACT
FACTOR
(2021:
5.478
)
(2022:
5.636
)
(2023:
6.741
)
OCLC
–
1368736135
transdermal delivery. Journal of Young
Pharmacists, 7(3), 220-225.
6.
Rangaraj, N., & Manjappa, A. S. (2019).
Transfersomes: An emerging tool for
transdermal drug delivery. Journal of Drug
Delivery Science and Technology, 52, 698-
705.
7.
Singh, R. P., Pathak, K., & Nagaraj, A. (2018).
Formulation, optimization, and evaluation of
transfersomes of itraconazole for transdermal
delivery. Journal of Young Pharmacists, 10(3),
346-351.
8.
Verma, P., Pathak, K., & Baghel, S. (2013).
Transfersomes: A surging vesicular carrier for
enhanced transdermal delivery of sertraline:
Development,
characterization,
and
performance evaluation. Drug Development
and Industrial Pharmacy, 39(6), 882-891.
9.
Yadav, S., & Singh, V. (2017). Development and
characterization of terbinafine hydrochloride-
loaded transfersomal gel for treatment of
onychomycosis. Drug Development and
Industrial Pharmacy, 43(6), 922-930.
10.
Zhao, X., Zhang, J., Liu, Y., Zhang, L., Li, H., &
Jiang, X. (2013). The application of
Amphotericin B transfersomes in the
transdermal
delivery
system.
BioMed
Research International, 2013, 624519.
