Gupta Ravikant1*, Bharadwaj Anjana1, Jain Alok Pal1, Yadav Akash2 and Gupta Shailesh3
1SRK University, Bhopal, MP, India
2COP, IPS Academy, Indore, MP, India
3Millennium college of Pharmacy, Bhopal, MP, India
*Corresponding Author: Gupta Ravikant, SRK University, Bhopal, MP, India.
Received: January 30, 2021; Published: March 30, 2021
In the current study ethosome transdermal patches were formulation and characterized for various parameters and evaluation were performed. On the basis of the study concluded that TF7 formulation was shows intended results and shows high entrapment efficiency and drug release kinetics shows higuchi model. Experimental work already published in the JETIR journal [7,8] here shows the extended study for drug excipient interaction study, permeation study, in-vivo and stability study, and optimization and skin irritation study. Results show there is no sign of the skin irritation and formulation is stable [1-4].
Keywords: Stability Study; Skin Irritation Study; In-vivo Study
In the current study Ethosomal based transdermal patches were formulated and characterized. Results show that formulation TF7 were produced intended results as compared to the other formulations. Study already published in JETIR journal here presenting extended study [7,8].
Methodology Physicochemical study Drug excipients interaction studyEthosome based transdermal patches were prepared by solvent evaporation technique and characterization and evaluation study was performed. Here presenting drug excipients interaction Parameter and results shows that there is no interaction as physical observation shows there were no change.
|
S. No. |
Additives (50 mg each) with drug |
Physical Observation |
Observation at 55°C after 15 days |
Remarks |
|
1. |
Drug |
White |
No change |
Accepted |
|
2. |
Drug + PVP |
White |
No change |
Accepted |
|
3. |
Drug + HPMC |
White |
No change |
Accepted |
|
4. |
Drug + Ethyl cellulose |
White |
No change |
Accepted |
|
5 |
Drug + all excipients |
White |
No change |
Accepted |
Table 1
The drug permeation from the Patches is depends on the polymer type as well used concentration. In-Vitro (permeation) studies were performed with Franz cell in Phosphate Buffer Saline pH 7.4. In drug Permeation study the formulation TF5 shows maximum drug permeation 95.24 % Lamivudine drug and 94.24 % Stavudine drug at 12 hrs. The drug permeation data of TF5 was plotted for Zero order, First order, Higuchi model and Korsmeyer-Peppas model to evaluate the permeation pattern of the dosage form. From these plots, kinetic values of the drug permeation were determined. Drug released from the matrix devices by diffusion studied with Higuchi's Model and result suggested that the drug permeation follow Higuchi model [7,8].
|
Formulation |
Flux (mg cm2 h-1) |
Permeability (cm2 h-1) |
|
F1 |
0.0255 ± 0.0011 |
0.010 ± 0.0006 |
|
F2 |
0.0317 ± 0.0018 |
0.015 ± 0.007 |
|
F3 |
0.0455 ± 0.0041 |
0.021 ± 0.0016 |
|
F4 |
0.0493 ± 0.028 |
0.028 ± 0.001 |
|
F5 |
0.0548 ± 0.032 |
0.032 ± 0.0023 |
|
F6 |
0.0623 ± 0.014 |
0.037 ± 0.028 |
|
F7 |
0.0626 ± 0.014 |
0.039 ± 0.028 |
Table 2
Stability studyThe TF5 was exposed for stability studies as per ICH guidelines and detected for all assessment parameters at a temperature of 250C and 60% RH, 400C and 75% RH, at an interval of 03 month. No physical changes in flexibility obtained, however physical and chemical evaluation parameter was slightly changed. Stability of the drug product is the crucial parameter to maintain the safety, quality and efficacy of the product. In case formulation is found to be unstable then influenced physical and chemical properties [7,8].
|
Day |
Appearance of different Formulation code |
|||||
|
F1 |
F2 |
F3 |
F4 |
F5 |
F6 |
|
|
After 7 days |
ü |
ü |
ü |
ü |
ü |
ü |
|
After 7 days |
ü |
ü |
ü |
ü |
ü |
ü |
|
After 7 days |
ü |
ü |
ü |
ü |
ü |
ü |
|
After 7 days |
ü |
ü |
ü |
ü |
ü |
ü |
|
After 3 days |
ü |
ü |
ü |
ü |
ü |
ü |
Table 3
Skin irritation testThe skin irritation test was examined on healthy albino rats for augmented formulation. As no sign of edema and erythema obtained this established the concept that formulation is suitable for topical applications [7,8].
Figure 1: Transdermal patch applied to rabbit. Photographs of rabbit skin treated with transdermal patch.
Photographs of rabbit skin treated with transdermal patch
Figure 2: Intact after 24 hrs.
Figure 3: Abraded after 24 hrs.
Figure 4: Intact after 72 hrs.
Figure 5: Abraded after 72 hrs.
|
Day |
Control |
F1 |
F2 |
F3 |
F4 |
F5 |
F6 |
|
1 |
0 |
0 |
0 |
0 |
0 |
0 |
0 |
|
2 |
0 |
0 |
0 |
0 |
0 |
0 |
0 |
|
3 |
0 |
0 |
0 |
0 |
0 |
0 |
0 |
|
4 |
0 |
0 |
0 |
0 |
0 |
0 |
0 |
|
5 |
0 |
0 |
0 |
0 |
0 |
0 |
0 |
|
6 |
0 |
0 |
0 |
0 |
0 |
0 |
0 |
|
7 |
0 |
0 |
0 |
0 |
0 |
0 |
0 |
Table 4: Skin irritation study.
In-vivo studyIn-vivo study in male rats was performed and following results were obtained.
|
S. No. |
Parameter |
Mean ± S.D. |
|
1. |
Co (µg/ml) |
3.45 ± 1.04 |
|
2. |
AUCo (µg h/ml) |
5.54 ±1.28 |
|
3. |
CL (L/h) |
0.51 ± 0.13 |
|
4. |
T1/2 (h) |
0.22 ± 0.12 |
|
5. |
Vd (L/kg) |
3.57 ± 0.91 |
|
6. |
Vss (L/kg) |
10.93 ± 3.08 |
Table 5: Pharmacokinetic parameters of drug in rats.
|
S. No. |
Parameter |
Control cm2 |
|
1. |
Cmax (µg/ml) |
1.08 0.13 |
|
2. |
AUCo (µg h/ml) |
21.31 2.62 |
|
3. |
AUCo-∞ (µg h2/ml) |
28.35 4.16 |
|
4. |
Css (µg/ml) |
0.89 0.11 |
|
5. |
T max (h) |
13.5 8.43 |
|
6. |
MRT (h) |
14.83 1.18 |
Table 6: Pharmacokinetic parameter of drug after application of patches.
The observed data was r2 = 0.993. The steady state volume of distribution and clearance of drug were very low. The concentration of the drug was low to be detected in rat plasma up to 6 h of sampling. Transdermal patches were gave drug release for longer duration of time as compared to the intravenous route of administration [3].
OptimizationBased on the result of in-vitro permeation profiles of batches of transdermal patches the optimum composition of F7 batches of transdermal patch was obtained. The results showed that the physico-chemical characteristics of the optimized batches were satisfactory with respect to thickness, tensile strength, folding endurance, drug content uniformity, in-vitro permeation profile.
Various evaluation parameters were performed to confirm that formulated study produced patches which are stable and effective and solve the current study purpose. Drug interaction study shows there is no interaction between drug and the excipients and in vivo study, skin irritation study, stability study results that there is no skin irritation sign as no edema or erythema occur in the rat skin.
Citation: Gupta Ravikant., et al. “Formulation, Characterization and Evaluation of the Transdermal Drug Delivery System of the Antiretroviral Drugs for the Treatment of HIV/AIDS". Acta Scientific Pharmaceutical Sciences 5.5 (2021): 84-87.
Copyright: © 2021 Gupta Ravikant., et al. This is an open-access article distributed under the terms of the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original author and source are credited.
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