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Swami Vivekanand College of Pharmacy, Udgir
Ascorbic acid (Vitamin C) is a strong topical antioxidant employed for its photoprotective and properties that stimulate collagen. Nevertheless, its elevated solubility in water, quick oxidation, and inadequate Permeation through the stratum corneum restricts its clinical effectiveness. The current research aimed to develop, refine, and assess Vitamin C-encapsulated liposomes through the homogenization technique to improve physical stability and transdermal absorption. Liposomes were created using the method of hydration for thin films utilizing Soya Lecithin and Cholesterol in a 2:1 proportion. The composition was improved by assessing various homogenization parameters. Original trials employing elevated shear homogenization led to aeration and phase separation; consequently, the process was optimized through ultrasonic homogenization to reduce foaming and attain a consistent nano dispersion. The optimized batch was assessed for visual characteristics, vesicle dimensions, zeta. potential, entrapment efficiency (%EE), drug content, and in-vitro release characteristics. Scanning Electron Microscopy (SEM) verified the creation of smooth, spherical nano-vesicles. Sure! Please provide the text you would like me to paraphrase. formulation demonstrated an ideal pH of 6.8, elevated entrapment efficiency, and a prolonged biphasic release profile of the drug over a 24-hour period. To sum up, improving the homogenization.
Vitamin C (L-ascorbic acid) is an essential water-soluble micronutrient in the fields of pharmaceutical and cosmetic science, prized for its antioxidant properties, involvement in collagen production, and promotion of wound healing. Although it is effective for addressing hyperpigmentation and photoaging, Vitamin C encounters notable formulation obstacles. It is very unstable, susceptible to quick oxidation when in contact with light or oxygen, and has low skin permeability because of its hydrophilic characteristics (1,2).
Ascorbic Acid
Traditional topical administration frequently struggles to penetrate the lipophilic stratum corneum, resulting in diminished clinical effectiveness. To address these obstacles, carriers utilizing nanotechnology—particularly liposomes—have developed as an enhanced delivery method. Liposomes are round phospholipid layers that can enclose both water-soluble and fat-soluble substances. Their biomimetic design improves skin absorption and safeguards the encapsulated Vitamin C from environmental deterioration (3).
Enclosing Vitamin C in liposomes protects it from oxidation while allowing for prolonged release and enhanced transdermal absorption relative to typical aqueous solutions. Although various preparation methods are available, the homogenization technique is typically favored for generating consistent, nanoscale vesicles with excellent stability. The effectiveness of these systems relies significantly on factors like lipid-to-cholesterol ratios and mechanical processing parameters.This research concentrates on the creation, refinement, and analysis of Vitamin C-encapsulated liposomes employing the homogenization technique.
Mechanism of liposomal drug delivery through skin
List of Materials Used in Formulation
|
Sr.No |
Material Name |
Category/Role |
Description |
|
1 |
Ascorbic Acid |
Active Pharmaceutical Ingredient |
Used as the active drug in the formulation due to its antioxidant and skin brightening properties. |
|
2 |
Soya Lecithin |
Phospholipid |
Used for formation of liposomal vesicles because of its amphiphilic nature. |
|
3 |
Cholesterol |
Stabilizer |
Added to improve membrane stability and rigidity of liposomes. |
|
4 |
Chloroform |
Organic Solvent |
Used for dissolving lipid components during preparation of lipid phase. |
|
5 |
Methanol |
Co-solvent |
Used along with chloroform to prepare uniform lipid solution. |
|
6 |
Sodium Phosphate Monobasic |
Buffer Reagent |
Used in preparation of phosphate buffer solution for pH adjustment. |
|
7 |
Sodium Phosphate Dibasic |
Buffer Reagent |
Used with monobasic phosphate to maintain buffer pH |
Formulation Design
|
Batch |
Lecithin (mg) |
Cholesterol (mg) |
Vitamin C (mg) |
|
F1 |
100 |
200 |
200 |
|
F2 |
150 |
300 |
200 |
|
F3 |
200 |
400 |
200 |
Optimization of the liposomal phrasings was carried out by varying expression and process parameters similar as phospholipid attention, cholesterol attention, homogenization speed, homogenization time, and medicine- to- lipid rate. Different batches were prepared and estimated to determine the optimized expression with desirable physicochemical characteristics.( 15)
The set liposomal phrasings were estimated for colorful physicochemical parameters including flyspeck size, zeta eventuality, ruse effectiveness, morphology, pH, density, and medicine content. In- vitro medicine release studies and stability studies were also performed to assess the performance and shelf- life of the optimized expression.( 16)
The optimized Vitamin C loaded liposomal expression was further characterized for its physicochemical and morphological parcels to confirm its felicity for topical delivery. Parameters similar as flyspeck size, zeta eventuality, ruse effectiveness, and face morphology were anatomized using standard logical ways. The attained results were compared to elect the stylish optimized expression with enhanced stability, zniformity, and medicine release profile.( 17)
The set liposomal phrasings were stored in watertight glass holders under cooled conditions until farther use to maintain stability and help declination of Vitamin C.( 12,13)
Methodology:
3. RESULT & DISCUSSION
The formulated Vitamin C loaded liposomes were estimated for their physical characteristics. The original batch prepared via high- speed shear homogenization displayed severe raging and phase separation. Upon optimizing the homogenisation system to ultrasonication, the optimized batch appeared as a livery, translucent to milky-white dissipation( 29). No visible summations or phase separation were observed, indicating a largely stable vesicular system.
Physical Appearance of final product
3.2 Percentage Yield
The practical yield of the set Vitamin C loaded liposomal phrasings was determined to estimate the effectiveness of the expression process and recovery of the final product. The chance yield of all set batches was set up to be satisfactory, indicating minimum loss of accoutrements during expression.
Observation Table:
|
Batch |
Theoretical Weight (mg) |
Practical Weight (mg) |
Percentage Yield (%) |
|
F1 |
170 |
150 |
88.23% |
|
F2 |
230 |
210 |
91.30% |
|
F3 |
290 |
260 |
89.65% |
The pH of the optimized expression was set up to be(7.44), which falls impeccably within the ideal physiologically compatible range for topical and dermal operation, icing no skin vexation occurs.
pH Dimension
The vesicle size and size distribution of the set Vitamin C- loaded liposomal phrasings were determined. The average vesicle size of the phrasings was set up to be in the nanometric range, attesting the successful conformation of nanosized liposomes.
This size range is suitable for enhanced topical medicine delivery.
Observation Table
|
Batch |
Vesicle Size (nm) |
Size Distribution |
|
F1 |
168.2nm |
Less uniform vesicles |
|
F2 |
143.1nm |
Better uniformity |
|
F3 |
181.5nm |
More aggregation |
Observation Table
|
Batch |
PolydispersityIndex (PDI) |
Interpretation |
|
F1 |
0.312 |
Moderate Uniformity |
|
F2 |
0.268 |
Good Uniformity |
|
F3 |
0.354 |
Acceptable Uniformity |
3.6 Zeta Potential
The zeta eventuality of the set Vitamin C loaded liposomal phrasings was measured to estimate the face charge and prognosticate the physical stability of vesicular dissipation. The attained zeta eventuality values indicated good electrostatic stabilization of the set liposomal phrasings.
Observation Table
|
Batch |
Zeta Potential (mV) |
Interpretation |
|
F1 |
-2.8mV |
Low Stable |
|
F2 |
-1.5mV |
Comparatively Stable |
|
F3 |
-2.1mV |
Moderate Stable |
3.7 Scanning Electron Microscopy(SEM)
Scanning Electron Microscopy(SEM) analysis was performed to examine the face morphology and structural characteristics of the set Vitamin C loaded liposomal vesicles. The
SEM images revealed that the vesicles were generally globular in shape with smooth face morphology and well- defined boundaries.
Observation
Scanning Electron Microscopy (SEM)
3.8 Entrapment Efficiency (%EE):
The ruse effectiveness of the set Vitamin C loaded liposomal phrasings was determined to estimate the quantum of medicine successfully reprised within the vesicles. The chance ruse effectiveness was measured using UV-Visible spectrophotometric analysis after separation of unentrapped medicine.
Observation Table
|
Batch |
Efficiency (%EE) |
Interpretation |
|
F1 |
72.45 |
Good Drug Entrapment |
|
F2 |
84.68 |
Highest Entrapment |
|
F3 |
78.92 |
Satisfactory Entrapment |
The total medicine content of the set Vitamin C loaded liposomal phrasings was determined using UV-Visible spectrophotometric analysis to insure invariant distribution of the medicine throughout the expression. The results indicated satisfactory objectification of Vitamin C in all set batches.
Observation Table
|
Batch |
Drug Content (%) |
Interpretation |
|
F1 |
89.24 |
Uniform Drug Distribution |
|
F2 |
95.67 |
Highest Drug Content |
|
F3 |
92.13 |
Satisfactory Drug Content |
The in- vitro medicine release study of the set Vitamin C loaded liposomal phrasings was performed using Franz prolixity cell outfit in phosphate buffer medium over a period of 24
hours. The accretive chance medicine release of each expression was determined at destined time intervals using UV-Visible spectrophotometric analysis.
|
Batch |
Drug Release after 24 hrs (%) |
Interpretation |
|
F1 |
78.42 |
Sustained Release |
|
F2 |
91.56 |
Maximum Drug Release |
|
F3 |
84.37 |
Controlled Release |
Stability studies of the set Vitamin C loaded liposomal phrasings were carried out at 4 °C and 25 °C for 30 days to estimate the effect of storehouse conditions on expression stability.
The phrasings were periodically observed for physical appearance, vesicle size, pH, and medicine retention.
Observation Table
CONCLUSION
The present study successfully formulated and estimated Vitamin C loaded liposomes using the homogenization system. Different expression batches were prepared by varying the attention of lecithin and cholesterol, and were estimated for colorful physicochemical parameters including vesicle size, polydispersity indicator, zeta eventuality, ruse effectiveness, medicine content, in- vitro medicine release, and stability. Among all set phrasings, the optimized batch displayed desirable vesicle size in nanometric range, invariant size distribution, satisfactory zeta eventuality, high ruse effectiveness, and excellent medicine content, indicating successful expression development. The invitro medicine release study demonstrated sustained and controlled release of Vitamin C from the liposomal vesicles over 24 hours. Stability studies revealed that the optimized liposomal expression remained more stable under refrigerated conditions as compared to room temperature, indicating the significance of proper storehouse due to the oxidation-sensitive nature of Vitamin C.
Overall, the study concludes that liposomal encapsulation is an effective approach for perfecting the stability, medicine retention, and controlled release of Vitamin C, thereby enhancing its eventuality for topical/ pharmaceutical operation.
REFERENCES:
Aman Mahagame *, Bajarang More, Bhakti More, Asmita More, Navnath Bendke, Formulation Optimization and Evaluation of Vit.C Loaded Liposomes by Homogenisation Method, Int. J. of Pharm. Sci., 2026, Vol 4, Issue 6, 7774-7782. https://doi.org/ 10.5281/zenodo.21071863
10.5281/zenodo.21071863