Design and Evaluate Terbinafine Hydrochloride Loaded gel by using
Modified Tamarind for Topical Drug Delivery
Deshmane Gorakh*, Dhawale Shashikant, Dhonde Satish
School of Pharmacy, S.R.T.M. University,
Nanded - 431606, MS, India.
*Corresponding Author E-mail:
gorakh.deshmane.gd@gmail.com
ABSTRACT:
The principal objective
of this study is to make and survey the properties of Gel containing
terbinafine hydrochloride (TH) stacked niosomal gel by functionalized tamarind
involving that might work as effective antifungal medication conveyance
frameworks (DDS) for the helpful treatment of contagious contaminations by
postponing the prescription delivery. Utilizing a characteristic direct
functionalized polymer and the ethanol infusion strategy, niosomal gel was made
(thionatinated and sulphonated tamarind). TH stacked niosomal scattering of
size going from 100 to 627nm and percent ensnarement effectiveness of 63 to 87%
were acquired. Both the factors for example length 60 and cholesterol impact
the molecule size and EE (%). In-vitro discharge concentrates on completed in
PBS (pH 5.5) for N4 and showcased cream displayed an arrival of 82.72% and
74.92% separately more than 24hr. The details of the Nanosponges were assessed
for their rates of creation yield (PY), entanglement effectiveness (EE), and
medication stacking (%DL). FTIR, DSC and PXRD studies uncovered that the
greater part of the medication was scattered all through the niosomes. DSC and
XRD concentrates on additionally shown that medication was in undefined state
in the N4 cluster while unadulterated TH was in translucent state. FESEM, TEM
and AFM pictures showed that niosomes had round shape with smooth surface. CLSM
picture demonstrated the smooth and bilayer design of niosomes. 1%w/v TH (0.1%)
stacked niosomal Sulphonated and thionated tamarindgel were ready and portrayed
for consistency studies. The consistency of fake treatment Sulphonated and
thionated tamarind and TH stacked niosomal gels with both were viewed as
20,500cps, 43,000cps, 10,300cps and 34,600cps respectively. It was apparent
from the pH and spreadability boundaries that the fake treatment and TH stacked
niosomal gels are viable for skin delivery.In-vitro discharge concentrates on
did in PBS (pH 5.5) for THNTT gel, THNST gel and showcased cream wereshowed
74.92±0.98 %,99.07±1.03% and 101.02±0.87% discharge toward the finish of 24 hr
respectively.Amount of medication held in skin after 24 hr was 47.68 for THNTT
gel while for promoted gel, it was viewed as 27.67 showing THNTT has great skin
maintenance properties than advertised cream (Texifen).CLSM investigation of
Wistar rodent skin uncovered that niosomes were circulated all through skin
with high fluorescence power which ready to help ex vivo skin penetration and
maintenance result.No indications of disturbance were seen upon the utilization
of fake treatment gel, N4 niosomal scattering, THNTT gel, and advertised cream
of TH to the Wistar rodents skin ,affirming that pre-arranged N4 niosomal
scattering as well as THNTT gel are liberated from irritation. In
vitro antifungal movement study for THNTT gel and showcased cream were
performed for both Aspergillusniger (ATCC 10578) and Candida albicans (CA14,
clinical confine) and results showed that N4 gel would be advised to antifungal
action in contrast with promoted cream.In vivo pharmacodynamic concentrates on
showed that THNTT gel lessens parasitic weight or count more actually than
advertised cream.
KEYWORDS: Thionated tamarind, sulphonated tamarind, Niosomal and
terbinafine hydrochloride.
INTRODUCTION:
How a medication is directed to the body could
influence its viability. A few prescriptions have an ideal fixation range where
the best advantage is gotten; focuses outside or within this variety cannister
be risky before have not in any way shape or form helpful benefit. The
objective of another medication movement conspire stays toward rapidly
accomplish and keep up with the right medication focus by conveying a valuable
portion of the medicine toward the proper spot popular the edge1.
Since the medication enters fixated by the more deeply coatings of the film
before greased up coverings, intriguing plans stay utilized focused on
restricted possessions on the application area. The effective conveyance
framework's essential advantage is keeping away from essential grant retention.
Extra advantage of fascinating plans stays that they avoid the dangers then, at
that point, bothers of blood vessel treatment notwithstanding the different
states of distraction, for example pH varieties, the participation of catalysts,
then, at that point, gastrointestinal voidance while2.
Terbinafine hydrochloride (TH) has a place with BCS
class II medication and has extremely unfortunate water dissolvability. It is
exceptionally lipophilic with log P esteem 3.3 and goes through first pass
digestion. It is broadly utilized in the liver and hence, has low
bioavailability3. Oral organization has been demonstrated to be
related with drug communications, hepatotoxicity, gastrointestinal and
fundamental aftereffects, lactose bigotry and other antagonistic impacts.
Essentially, traditional skin definitions have restrictions like insufficient
maintenance of medication inside the skin and the less understanding
consistence. Thusly, a superior methodology is expected to convey the
medication in the ideal layer of skin without adjusting its physicochemical
properties, lessening secondary effects which can be accomplished by planning
is niosomalgel4,5.
MATERIALS AND METHODS:
Materials:
Terbinafine hydrochloride was a gift sample from Dr.
Reddys Lab, Hyderabad, Thionated tamarind & Sulphonated tamarind was
prepared in house. Other materials were purchase from AG chem. Ltd. Pune. All
other reagents and chemicals utilized were of analytical grades.
Methods:
Preparation
of terbinafine hydrochloride loaded niosomes:
To ensure there would be no interactions between the
drug and recipients during the preparation of the formulation dosage form,
reformulation tests were carried out. It offers guidance on choosing recipients
for the drug's formulation in a niosomes. The drug's compatibility with the
recipients physically was tested. Through FT-IR spectrum6,
differential scanning calorimetry (DSC)7 and powder X-ray diffraction analysis8
Preparation of terbinafine hydrochloride loaded
niosomes:
The clear and medication stacked niosomal scatterings
were ready by altered ethanol infusion (MEI) technique. Explicit measure of
Length 60, cholesterol and TH were broken down in 10ml of ethanol by shower
sonicator for 5min and followed bywarming to 60°C. This was quickly infused
through a needle in a characterized volume (10ml) of phosphate cushion (pH 7.4)
under blending at 500rpm (Remi attractive stirrer) utilizing Teflon covered
globule. The phosphate cushion (pH 7.4) quickly turned smooth in light of niosomes
arrangement and the blending was gone on for 2hr for the expulsion of the
ethanol. Phosphate support was added to change the volume of the last niosomal
scattering to 10ml. Besides it was refrigerated for 2-6 hrfor powerful vesicle
fixing. The arrangement of circular niosomes is affirmed by optical microscopy.
The niosomal scattering was additionally assessed on different boundaries.
Particle size and polydispersity index determination:
Molecule size
and polydispersity file of medication stacked niosomal not entirely settled by
powerful light dissipating utilizing 90 or more nanoparticle size analyzer
(Brookhaven Instruments Corp., NY, USA). Examination was conveyed out at room temperature
keep in gangle of detection 90°. The examples were weakened with refined water
to get a suitable laser obscuration. The width of size appropriation was shown
by polydispersity list (PDI). The examination was performed three fold and
results were communicated as mean±standard deviation (SD).
Field emission scanning electron microscope
(FESEM):
The FESEM of
the lyophilized upgraded cluster N4 test was performed to explore the surface
morphology. Enhanced niosomes were mounted on twofold confronted sticky tape
and covered with a slight gold-palladium layer with a falter covered unit and
dissected by FESEM (FEI Nova Nano SEM 450, Japan) worked at a 5kV speed
increase voltage.
Transmission Electron Microscopy (TEM):9
Morphological evaluation of the niosomal
dispersion was performed using transmission electron microscopy (CM-200
Philips, Japan). A drop of niosomal dispersion was placed on carbon coated
copper grid and allowed to adhere with grid. The excess of the niosomes
suspension was then drawn off by a piece of filter paper (Whatman Inc., NJ,
USA). A drop of a negative stain solution, 1% (w/v) phosphotungstic acid
solution, was placed on the carbon grid thus staining the niosomes. After 3
min, the excess staining agent was removed by adsorbing the drop with the tip
of a filter paper and the sample was then air-dried. Imaging was performed on
TEM at a voltage of 80kV having magnification of 60000X using Digital
micrograph imaging viewer software.
Preparation of gels:10,11,12
Readiness of terbinafine hydrochloride
stacked niosomal in sulphonated tamarind gel:
The TH
stacked niosomal gel was ready by scattering 1000 mg of sulphonated tamarind
(at 1% w/v) in the advanced niosomes plan (N4) under steady mixing utilizing
attractive stirrer to deliver 0.1% TH stacked niosomal gel followed by
expansion of propylene glycol (at 2% w/w) and consequently killing the
scattering with tri-ethanolamine (TEA) to get satisfactory gooey gel.
Readiness
of terbinafine hydrochloride stacked niosomal in thionated tamarind gel:
The TH
stacked niosomal gel was ready by scattering 1000 mg of thionated tamarind (at
1% w/v) in the advanced niosomes detailing (N4) under consistent blending
utilizing attractive stirrer to deliver 0.1% TH stacked niosomal gel followed
by expansion of propylene glycol (at 2% w/w) and consequently killing the
scattering with tri-ethanolamine (TEA) to acquire satisfactory gooey gel.
Characterisation of gels:13,14
The
pre-arranged gel details were reviewed outwardly for their variety, lucidity,
homogeneity, pH and grittiness.To decide the medication content of gel, 1gm of
TH stacked niosomal gel was gauged and blended to 10ml of methanol and after
appropriate weakening with phosphate cushion pH 7.4, the centralization of
terbinafine hydrochloride (TH) was spectrophotometrically estimated at 282nm.66
Spreadability study of gel:15,16
Spreadability investigation of gel was
examined by wooden block and glass slide device. An overabundance of gel test
(1gm) was in the middle of between two glass slides and a 500gm weight was put
on upper slide for few moments to pack and consistently spread the gel between
the slides. A particular weight (10gm) was included the container and the time
was noted for the upper slide (versatile) to isolate totally from the decent
slides.
Viscosity:17
The
thickness of terbinafine hydrochloride stacked niosomal in thionated tamarind
gel and sulphonated tamarind gel were acquired by Brookfield viscometer
(Brookfield designing labs, Inc., Mama, USA) with axle no. 6 at 20rpm at room
temperature.
In-vitro drug release study:18,19
Drug discharge was concentrated by
utilizing Franz dissemination cells (utilizing counterfeit cellophane film)
(Membra - Cel MD 34-14, cut-off 14 kD). For this investigation an upward Franz
dispersion cell having a surface area of 3.14cm2 and a supply limit of 20ml was
utilized. The fake film was safely positioned between the two parts of the
dispersion cell. The receptor liquid comprised of phosphate cushion pH 5.5; its
temperature kept up with at 37±0.5°C and mixed persistently utilizing
attractive stirrer. A foreordained measure of TH stacked niosomal in thionated
tamarind gel, sulphonated tamarind gel and TH showcased cream containing 2mg of
TH was put in a benefactor compartment over the film. At various time spans
from 0 to 24hr, aliquot (2 ml) of delivery medium was removed through a
hypodermic needle and supplanted with a similar volume of new cradle
arrangement. The aliquots were reasonably weakened with the receptor medium and
medication content in the removed not entirely set in stone by an UV
spectroscopy at λmax 282nm utilizing a pre-built adjustment bend.
Estimations were acted in three-fold and their means were accounted for.
Ex-vivo skin permeation study:20
The
ex-vivo skin saturation study was performed on extracted Wister rodent skin as
indicated by the review convention was endorsed by IAEC (Institutional Creature
Morals Advisory group) comprised according to rules of the Council with the end
goal of Control and Oversight of Tests on Creatures (CPCSEA), Administration of
India. The stomach skin of the rodent was shaved and the full skin was
painstakingly extracted. Subcutaneous fat was taken out with a surgical tool;
skin was washed PBS pH 7.4 appropriately and utilized right away.
Saturation
investigations of arranged TH stacked niosomal in thionated tamarind gel,
sulphonated tamarind gel and showcased cream (Texifen) was performed utilizing
independently Franz-dispersion cells with a powerful dissemination area of
3.14cm2. The layer was mounted cautiously onto the dispersion cell with SC side
confronting the benefactor compartment. The receptor compartment was loaded up
with 20ml of dispersion medium (Phosphate cushion pH 5.5) and was kept up with
at 37º±0.50C. The arrangement in the receptor compartment was constantly mixed
utilizing Teflon covered attractive stirrer at 100rpm. At zero time, benefactor
compartments of Franz dispersion cells were loaded up with the test details (TH
stacked niosomal in thionated tamarind gel, sulphonated tamarind gel and
advertised plan for example 1% cream) comparable to 2 mg drug independently. At
chose stretches inside 24hr, 2ml of the example was removed from the receptor
compartment and supplanted with an equivalent volume of delivery medium to keep
up with sink conditions. The examples were then suitably weakened and
quantitatively broke down by UV Spectrophotometer at 282nm. Estimations were
acted in three-fold and their means were accounted for.
Skin retention of TH loaded niosomal gel:21,22
In the wake of performing skin penetration
studies, skin was painstakingly taken out from the Franz dissemination cell.
Remaining detailing was washed with q-tip absorbed phosphate cradle of pH 5.5.
The cleaned skin piece was crushed, and 10ml of methanol was added to the
coincided mass and precisely shaken in a water shaker shower at 37°C for 1 hr
and followed by centrifugation at 15,000rpm for 30 min (4±0.5°C) for the total
extraction of the medication. After extraction, the subsequent arrangement was
separated and how much medication content in filtrate was resolved utilizing UV
spectrophotometer at 282nm. Skin maintenance (%) was determined utilizing the
accompanying formula:
Skin retention (%) =Amount of drug in
skin/Total drug × 100
In-Vivo Pharmacodynamic studies:
All creature studies were performed by the rules
ordered by the Panel with the end goal of Control and Oversight of Trials on
Creature (CPCSEA, Administration of India). The convention of the investigation
was supported by the Institutional Creature Morals Board of Sudhakarrao Naik
Establishment of Drug store, Pusad, Dist-Yavatmal, Maharashtra (Endorsement
No.: CPCSEA/IAEC/CP-PL/21/2022). The rodents were housed in polypropylene
confines with free admittance to a standard lab diet and water. They were kept at
25± 2°C and 45-55% relative mugginess (RH) with a 12-hr light-dim cycle. The
microbe free Wistar rodents weighing 200-250gm were utilized for the
examination.
RESULT:
Drug Excipient Compatibility study:
Fourier Transform Infrared Spectroscopy (FTIR):
The FTIR spectroscopic examination was done to
research the collaborations between the parts of the niosomal detailing. The
FTIR spectra of the unadulterated medication, range 60, cholesterol and
lyophilized powder of un adulterated medication stacked niosomal scattering are
displayed in Fig. 1.
Differential Scanning calorimetry (DSC):
Warm examination of terbinafine hydrochloride (A),
length 60 (B), cholesterol (C), TH stacked niosome group N4 (D) were performed
and results are displayed in Fig 2. Endothermic tops at 208.2°C, 54.7°C and
148.5°C were distinguished, showing the dissolving points of translucent
unadulterated TH (A), range 60 (B) and cholesterol (C) separately. Lyophilized
plan of TH stacked bunch N4 (D) showed tops at 49.9°C, 138.2°C and 225.9 °C.
The DSC thermogram of improved cluster N4 showed vanishing of medication endothermic
pinnacle
Fig 1: FTIR Spectroscopy of: A) Terbinafine HCL B) Span
60 C) Cholesterol D) Lyophilized powder of drug loaded niosomal dispersion (N4
batch)
Fig 2: DSC thermograms of (A) Terbinafine hydrochloride
(Pure drug), (B) Span 60, (C) Cholesterol and (D) lyophilized powder of TH
loaded niosomal dispersion
Powder X-ray diffraction (PXRD):
TH powder was exceptionally translucent as obvious
from sharp pinnacles seen at the 2θ worth of TH in the X-beam check as
displayed in Fig 3 (a). Fig 3 (b) shows the PXRD examples of freeze dried TH
stacked niosomal powder 21,35
Figure 3: XRD patterns of a) pure terbinafine hydrochloride
b) Lyophilized TH loaded niosomal powder
Optimization of Formulation:
At the point
when measurable investigation of 32full factorial plan clusters was performed
utilizing Plan Master 8.0.7.1 (Detail Straightforwardness Inc., USA)
programming. A 32 full factorial plan was led to concentrate on the
impact of how much Range 60 (X1), how much cholesterol (X2). Information of
molecule size and capture effectiveness (%) for the all clusters showed a wide
variety which obviously demonstrate that the qualities were emphatically
subject to the free factors. The rundown of reactions of nine (9) clusters of
niosomal scattering is displayed in the Table 1
Flow properties:
The powder has shown better angle of response which
was 23±4.20°C (excellent), carr's index of 0.201±0.06 (g/cm3), and
tapped density was 20.38±3.15 (below 15 % is considered as a poor stream), bulk
density, and hausner's ratio of 0.204±0.05(g/cm3), and 1.13±3.15
(Below 1.25 Hausner's ratio shows the best flow characteristics than the
greater one) which proved its acceptability as a carrier.
Evaluation of Terbinafine Hcl Loaded Niosomes For
Optimised Batch:
Particle size and polydispersity index:
Molecule
size is one of the main boundary as it straightforwardly affects the pervasion,
steadiness, cell take-up and sedate delivery. The molecule size of the
streamlined medication stacked niosomal scattering was 105±1nm. The PDI of the
medication stacked niosomes was viewed as 0.339±0.013, uncovering that vesicles
populace was somewhat homogenous for example size circulation was somewhat
tight. 21, 37
Fig 4: Particle size distribution of
optimized batch of terbinafine hydrochloride loaded niosomal dispersion (N4)
Field emission scanning electron microscope (FESEM):
The FESEM microphotographs (Fig 7)
(a) (b)
Fig 5 (a): FESEM microphotographs of
drug (TH) loaded optimized batch N4 (b): FESEM microphotographs of drug
Preparation of Gel:
In the drug business, tamarind is much of the time
used as a mucoadhesive polymer, a normally happening polysaccharide that is
gotten from tamarind seed. In any case, tamarind's natural application in drug
conveyance is restricted at the same time, its functionalization has displayed
to upgrade its usefulness. The contemporary canvases were made fully intent on
assessing the tamarind's noticed oral harmfulness. IR and mass spectroscopy
have totally assessed the functionalized and unmodified tamarind.
The functionalized tamarind polymer was chosen to get
ready gel 1% w/v gel. Chosen measure of functionalized tamarind was gradually
added to refined water and saved for 2 hr. Then it was scattered at 500rpm with
an attractive stirrer to get a smooth scattering. TH broke down in fluid stage
containing functionalized tamarind to yield 1% w/v gel under predictable
blending to create unadulterated medication stacked gel. Functionalized
tamarind was gradually added to TH stacked niosomal scattering to get ready medication
stacked niosomal gel under attractive mixing. Functionalized tamarind was
chosen since it is protected and compelling because of its high sub-atomic
weight they can't enter the skin or influence the property of medication. It
has superb thickening, suspending and emulsification for effective details. It
has an extended buildup time at site of organization. Functionalized tamarind
adsorbs water then it hydrates which prompts expansion in consistency and swell
to shape adhesive scattering after it gets loosen up.
Spreadability study of gel:
Spreadability of blank TT gel, blank ST gel, TH loaded
niosomal TT gel and TH loaded niosomal ST gel are shown in Table 2. Spreadability
was an important property of the topical formulation from the point of view of
the patient compliance. In fact, gel application on the inflamed or diseased
skin would be more comfortable if it can be spread easily. Result concluded
that both blank and N4 gel have good spreadability.23
Table 2: Spreadability values of different gel
|
Formulation
|
Spreadability (gm.cm/sec)
|
|
Blank TT gel
|
15 ± 1.8
|
|
Blank ST gel
|
13 ± 0.98
|
|
TH loaded niosomal TT gel
|
18.75±1.15
|
|
TH loaded niosomal ST gel
|
16.59±0.9
|
Viscosity:
The viscosity of the placebo (or blank) TT gel, blank
ST gel, TH loaded niosomal TT gel and TH loaded niosomal ST gel was determined
using Brookfield viscometer at room temperature. The results of viscosity are
given in Table 3, within acceptable limits.26,27
Table 3: Viscosity values of different gel
|
Formulation
|
Viscosity (cps)
|
|
Blank TT gel
|
43,000
|
|
Blank ST gel
|
20,500
|
|
TH loaded niosomal TT gel
|
34,600
|
|
TH loaded niosomal ST gel
|
10,300
|
In vitro drug release study:
To elucidate the drug release from drug loaded
niosomal gel and marketed gel, vertical Franz diffusion cell was used. The
temperature was maintained at 37 ± 0.5 °C. Phosphate buffer pH 5.5 was used as
release media and result depected in Fig. 6.
Figure 6: In vitro drug release study of
optimized batch (N4) loaded TT gel, (N4) loaded ST gel and marketed cream using
phosphate buffer pH 5.5
In vivo pharmacodynamics studies.26,27
Fungal burden was quantitatively analyzed
in terms of colony forming units (CFUs) after initiation of the treatment. CFUs
were counted using a colony counter. Table 4 and Fig 7 give the quantitative
analysis of fungal burden. Control group did not show any growth, as infection
was not induced to this group. Group treated with TH loaded niosomal TT gel (N4
gel) showed a significant decrease in fungal burden after 5 days (893 ± 51.71
CFUs) as compared to CFUs before initiation of treatment (221,595±3,205.55 CFUs).
Group treated with marketed cream also showed a significant decrease in fungal
burden after 5 days (8678±240.54 CFUs) as compared to CFUs before initiation of
treatment (233,498±3,349.55 CFUs), but it was higher as compared to the group
treated with developed formulation. These results showed that the niosomal TT
gel reduced the fungal burden in a shorter duration of time as compared to
marketed formulation. Thus, TH was found to be more effective when formulated
as niosomal based TT gel because of improved contact, adhesion, occlusion and
sustained release.
In vivo pharmacodynamics studies:
Fungal burden was quantitatively analyzed
in terms of colony forming units (CFUs) after initiation of the treatment. CFUs
were counted using a colony counter. Table 4 and Fig 7 give the quantitative
analysis of fungal burden.
Table 4: Quantitative analysis of fungal
burden
|
Group
|
Formulation
|
CFU on different days (CFUs)
|
|
|
|
0
|
1
|
3
|
5
|
|
Group-I
|
Control
|
-
|
-
|
-
|
-
|
|
Group-2
|
N4 TT gel
|
221,595± 3,205.55
|
126,357 ± 2,134.64
|
9,543 ±
245.22
|
893 ± 51.71
|
|
Group-3
|
Marketed
|
233,458± 3,349.55
|
120478± 2,136.43
|
82,456± 2,434.34
|
8,678 ± 240.54
|
Fig 7: In vivo antifungal activity of
formulations (drug TH loaded niosomal TT gel and marketed cream)
DISCUSSION:
The upgraded lyophilized niosomal powder showed
vanishing and shift of the places of the assimilation groups in contrast with
FTIR of terbinafine hydrochloride, length 60 and cholesterol demonstrating that
the majority of the medication was scattered in the niosomes. Pinnacles of
various utilitarian gathering present in terbinafine hydrochloride and
lyophilized powder of terbinafine hydrochloride stacked niosomal scattering are
displayed in fig no.1,
Lyophilized plan of TH stacked bunch N4 (D) showed tops at 49.9°C, 138.2°C and
225.9°C. The DSC thermogram of improved cluster N4 showed vanishing of
medication endothermic pinnacle in fig 2. in Fig 3 (a). Fig 9.12 (b) shows the
PXRD examples of freeze dried TH stacked niosomal powder, proposed that the
singular parts have somewhat lost their glasslike nature when integrated into
niosome vesicles. The decline in vesicle size of TH niosomes may be ascribed to
the diminishing in the bilayer thickness. From the factorial plan it was
presumed that Clump N4 was viewed as have more modest size and greatest
embodiment proficiency among each of the 9 clusters. So Clump N4 was taken as
advanced cluster and further portrayal of Bunch N4 was evaluated further. The
FESEM microphotographs (Fig 5) uncovered that the niosomes were round with
pretty much smooth surface. Infrequent clusters were likewise seen which could
emerge from issue related with the shrinkage of niosomes during lyophilization
of scattering medium. 24 In Fig. 6. The noticed niosomes N4
uncovered circular formed particles with smooth surface. The TEM pictures show
the medication encased in the niosomes vesicles. in Fig 6. The noticed niosomes
uncovered a circular shape with smooth surface and furthermore showed molecule
size in the scope of 100-300 nm. 25 The functionalized tamarind
polymer was chosen to get ready gel 1% w/v gel. In
Table 2.Spreadability was an important property of the topical formulation from
the point of view of the patient compliance. In fact, gel application on the
inflamed or diseased skin would be more comfortable if it can be spread easily.
Result concluded that both blank and N4 gel have good spreadability and results
of viscosity are given in Table 3, within acceptable limits.28,29
Control group did not show any growth, as
infection was not induced to this group. Group treated with TH loaded niosomal
TT gel (N4 gel) showed a significant decrease in fungal burden after 5 days
(893±51.71 CFUs) as compared to CFUs before initiation of treatment
(221,595±3,205.55 CFUs). Group treated with marketed cream also showed a
significant decrease in fungal burden after 5 days (8678±240.54 CFUs) as
compared to CFUs before initiation of treatment (233,498±3,349.55 CFUs), but it
was higher as compared to the group treated with developed formulation. These
results showed that the niosomal TT gel reduced the fungal burden in a shorter
duration of time as compared to marketed formulation. Thus, TH was found to be
more effective when formulated as niosomal based TT gel because of improved
contact, adhesion, occlusion and sustained release.30,31
CONCLUSION:
From the present study, the TH loaded niosomal TT gel
successfully achieved stable, nanosizedniosomes with suitable % entrapment
efficiency. This thionatinated tamarind offers the advantages of being
sustained, one-step-based process and reproducible. It is clear that niosomes
can be used as an effective carrier for the delivery of antifungal agent TH for
the treatment of localized fungal infections. The topical delivery of TH to the
skin by means of niosomes could possibly minimize its systemic access and side
effects. These delivery systems also showed good sustained release behaviour of
drug and good skin retention properties which proved their effectiveness for a
long-term drug therapy. TH loaded niosomal vesicles can easily distributed in
skin and may form depots in the skin. All these studies proved the
effectiveness of TH loaded niosomal gel for treating skin fungal infections,
and thus, it can be taken as a preferred choice of carrier system for topical
drug delivery. However, this formulation can find a place in clinical use after
clinical evaluation.
CONFLICT OF INTEREST:
The
authors have no conflicts of interest regarding this investigation.
ACKNOWLEDGMENTS:
Sudhakarrav Naik College of Pharmacy, Pusad Dist-
Yavatmal for pharmacodynamics studies.
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