Formulation and Evaluation of Ethosomal Gel and Non-ethosomal Gel of S.grandiflora Leaves

 

Rohan Rajkumar Patekar1,3*, Heena Bholaram Choudhary2,3, Sachin Devidas Rede3

1Department of Pharmaceutical Sciences and Natural Products, Central University of Punjab, Bathinda,

Punjab, India-151401.

2Department of Pharmacology, Poona College of Pharmacy, Bharati Vidyapeeth Deemed University, Erandwane, Pune, Maharashtra, India- 411038.

3Department of Pharmaceutical Sciences, Rasiklal M. Dhariwal Institute of Pharmaceutical Education and Research, Chinchwad, Pune - 411019, MH- India.

*Corresponding Author E-mail: rohanpatekar181299@gmail.com

 

ABSTRACT:

The numbers of products based on new drug delivery systems have considerably increased in the past few years, and this growth is projected to carry on in the future. These bio-pharmaceuticals present challenges to drug delivery system because of their different nature and difficulty in delivery through conventional routes. Therefore, further research will focus on the delivery of these complex molecules through different routes, including nasal, pulmonary, vaginal, rectal, etc. The intend of the study was to formulate and evaluate ethosomes of Sesbania grandiflora leaves which may transport the drug to targeted site more efficiently than marketed gel preparation and also overcome the problems related with oral administration of drug. Trans-dermal drug delivery is a technique which can be exploited to overcome the variables, which could affect the oral absorption of drugs such as pH, food intake and gastrointestinal motility. As compared to liposome or hydro-alcoholic solution ethosomal systems were much more capable at delivering a fluorescent probe to the skin in terms of quantity and depth. The formulations were prepared with ethanol, lecithin, propylene glycol, and glycerol and were evaluated. The lecithin (phospholipids) used as a vesicles forming component, polyglycol and ethanol used as a skin penetration enhancer. The drug released of formulated ethosomal gel was 4-5 times improved as compared to non ethosomal gel which directly achieves unparalleled flexibility in formulation. Ethosomal gel successfully addresses the issues relating to the drug delivery of poorly water-soluble drugs, peptides, potent drugs and the release of multi-drugs.

 

KEYWORDS: Sesbania grandiflora, Ethosomes, Bioavailability, Transdermal, Ethosomal-gel, Nano-carrier, novel drug delivery, Diffusion.

 

 


INTRODUCTION:

Ethosomes are lipid vesicles containing phospholipids and high concentration of alcohol. Recurrently ethanol is used in the ethosomes as an alcoholic vehicle so it is named as ethosomes1,2. All components of the ethosomal systemsare well thought-out as safe for pharmaceutical use3. The typical size of ethosomes4 can be through the range from 30 nm to few microns5.

 

 

As compared to liposome6 and too many commercial transdermal and dermal delivery systems ethosomal systems were found to be extensively better at delivering drugs through the skin in terms of both quantity and intensity7,8,9.

 

Ethosomes are refined vesicular delivery carriers that are capable of delivering various chemical applications1. The penetration rate through the skin of ethosomes is higher as compared to liposome and hence ethosomes can replace liposome7,8. The main reason suggested to be responsible for deeper distribution and penetration in the skin was might be due to the combination of phospholipids and high concentration of ethanol in ethosomes3,10. S.grandiflora leaves are highly nutritive and have been shown to contain more amounts of proteins, fat, carbohydrates, fiber, and minerals such as iron, calcium, and phosphorus11. The young leaves are edible and are often used to supplement meals12. The plant has potency of antidote for tobacco and smoking related diseases13. Many reports mention the isolation of sterols, saponin, and tannins from the leaves of the plant11. It has property to treat the small pox and other eruptive fevers13. Leaves are chewed as it has disinfectant property11. These bioactive constituents have potential health benefits and possess important biological activities such as antibacterial14, antioxidant15, anticonvulsant and anxiolytic11,13. In the rural areas of Bangladesh, the villagers use a sweetened concentrated juice prepared from the leaves as a remedy for diarrhea12. Oral administration of crude ethanol extracts of Sesbania grandiflora reduces the duration of defecation. Since we found to publish scientific investigation on topical preparation of Sesbania grandiflora leaves through developing the ethosomes. Schematic representation of drug release through ethosomal system16 was given in (fig 1).

 

 

Fig. 1: Schematic representation of drug release of ethosomal system1, 3

 

MATERIAL AND METHOD:

Collection and Identification of Plant:

The raw material (leaves of S. grandiflora) was obtained from Empress Botanical Garden, Pune, Maharashtra, India. The authentication of collected sample was done by comparing our sample with authentic herbarium specimens at herbarium department of Empress Botanical Garden.

 

Preparation of Extract from Leaves of S. grandiflora11,15:

The leaves were air dried at room temperature, after drying it was blended using bender and was converted into fine powder. Measured 10gm of powder was subjected to the soxhlet apparatus for 4 hrs for extraction purpose with 500ml of ethyl acetate11. The solvent was evaporated using the tray dryer at (60°C) and the dried extract was stored for further study.

 

Preparation of Ethosomes2, 4,16:

a) Cold Method:1,16

This method was most commonly used as the lecithin (Vesicle forming component), extract, glycerol and other lipid materials are dissolved together in the ethanol (Penetration enhancer and smoothening to vesicle membrane) with the vigorous stirring at room temperature. During stirring the polyethylene glycol (Penetration enhancer) was added at 40°C. This mixture was heated up to 30°C in the water bath. The stirring is continued for 5 min in covered vessel and size reduction was done using the sonicator17.  Lemon oil was added for flavor. The ethosomes were stored in refrigerator.

 

b) Hot Method:1,2

The lecithin in this method was first dispersed in water at 40°C. In another vessel take polyethylene glycol with the ethanol and heat up to 40°C. Mix the ethanol phase to the aqueous phase and add the drug to the mixture18. The size reduction can be done by sonication. Lemon oil was added and the ethosomes are stored for further study.

 

c) Selection of Method:1,18

Overall four batches were prepared. The B1, B2 and B3 were prepared by using Cold method and B4 by hot method. Accordingly following batches are formulated. Formulation table of ethosomes17,19 given in Table 1

 

Preparation of Gel:20,21,22

The carbomer was soaked in dematerialized water overnight. The carbomer then was triturated in the mortar pestle. Triethanolamine was also triturated with the carbomer to form the homogenize mixture and the gel base was prepared. Then the ethosomes were added in the base. For non ethosomal gel the S.grandiflora extract was added in the gel base23. The gels were homogenized for 15min22. The composition of gels is given24 in Table.1.

 

Table 1: Composition of Various Batches of Ethosomes and Ethosomal Gel of S.Grandiflora.

Composition of ethosomes

Material

B1

B2

B3

B4

Extract

1 gm

1 gm

1 gm

1 gm

Lecithin

(2%)

5 ml

(10%)

10 ml

(10%)

5 ml

-----

Castor oil

5 ml

-----

5 ml

5 ml

Polyethylene glycol

(50%)

5 ml

(70%)

5 ml

(70%)

5 ml

(50%)

5 ml

Glycerol

2.5 ml

2.5 ml

2.5 ml

2.5 ml

Ethanol

30 ml

30 ml

30 ml

30 ml

Lemon oil

2 ml

2 ml

2 ml

2 ml

Composition of ethosomal gel

Material

EG1

EG2

EG3

EG4

Carbomer

0.5g

0.5g

0.5g

0.5g

Triethanolamine

0.08ml

0.08ml

0.08ml

0.08ml

Propylene glycol

8.5ml

8.5ml

8.5ml

8.5ml

Glycerine

------

-----

-----

-----

Ethosomes of extract

0.5mg

0.5mg

0.5mg

0.5mg

Leaves extract

------

-----

-----

------

Water

q.s.

q.s.

q.s.

q.s.

EVALUATION OF ETHOSOMES AND ETHOSOMAL GEL:

Evaluation of ethosomes4:

·       Vesicles size and shape23,25

·       UV Spectroscopy study11

·       Measurement of drug loading capacity13,26

·       Measurement of entrapment efficiency13,25,27,28,29

·       pH23, 26

·       Spreadability18, 31

·       Zeta potential8, 23, 28

·       In vitro drug release study13, 25, 26, 32

 

Vesicles Size:23,25

The vesicle size and size distribution of ethosomes were determined by nano-particle analyzer Horiba SZ-100 based on laser light scattering principle. The diluted samples were used for the particle size analysis at 90° angle and temperature at 25°C.

 

Vesicle Shape:23,25,31

The shapes of the ethosomes were examined under the Compound Microscope. The formulation was spread over the clean glass slide which was then covered with cover slip without a single bubble in it. Then the slide was kept under the eye piece of 100 X and the sample was examined under the compound microscope. The photographs were collected.

 

UV Spectroscopy Study:11

Cyclohexane was used as solvent for UV Spectroscopy study. The extract was dissolved in the cyclohexane to form a stock solution of 100 ppm. The dilutions of 2 ppm, 4 ppm, 6 ppm, 8ppm and 10 ppm were prepared by diluting the stock solution. The λmax was measured from the spectral analysis.

 

Measurement of Drug Loading Capacity:11,26

For measurement of drug loading capacity the ethosomes were subjected to centrifugation at maximum rpm for 30min.The supernant and the sediment was separated. The dilution of supernant and sediment was done by cyclohexane and diluted solutions were filtered. Both diluted supernant and sediment was subjected to the UV spectroscopy for assay.

 

D =   100

Where, D is drug loading capacity

U is the amount of drug in ethosomes

W is the total amount of drug taken

 

Measurement of Entrapment Efficiency:13,25,27,28,29

The procedure for entrapment efficiency was same as the drug loading capacity. The entrapment efficiency was calculated by using the below formula.28

 

EE =  100

Where, W is the total amount of drug taken

L is the unentrapped drug

pH:13,26

Skin compatibility was important parameter for a good topical formulation. The pH study was carried out by simply using a digital pH meter(Sigma-27 DP).The pH meter was first calibrated using the buffer solutions pH (9.2 and 7) and then the readings were taken in triplets.

 

Spreadability18,37,31

Spreadability is a term expressed to denote the capability of media being spread on application area. Spreadability was important parameter for better therapeutic efficacy. A special apparatus has been designed to study the spreadability of the formulations in which two glass slides of standard dimensions (6×2 cm) were selected. The formulation was placed over one of the slides and the second slide was placed over the slide in such a way that the formulation was sandwiched between them across a length of 6 cm along the slide. A 100 gram of weight was loaded over the slide so that the formulation spreads equally over the slide and it forms a thin layer. Then the load was removed and the extra formulation was scraped off. The lower slide was fixed on the board of the apparatus and one end of the upper slide was tied to a string to which 20 gram load could be applied. The time taken by slide to travel the space of 6 cm and disconnect away from lower slide under the weight was noted. Lesser the time taken for separation of slides better is the spreadability.

 

Zeta Potential:18,23,28

Zeta potential provides a measurement of the net charge on the ethosomal surface. It was determined using zeta potential analyzer (nanoparticle analyzer Horiba SZ-100) at 25.1°C. The measurement of Zeta potential gives electrophoretic mobility and means zeta potential values were obtained directly from the measurement.

 

In vitro Drug Release Study:13,25,26,32

The diffusion study of formulation was studied using cellophane membrane. The diffusion medium used was phosphate buffer (6.8).The receptor chamber was filled with the phosphate buffer (6.8). In the water jacket the hot water was circulated to maintain the temperature up to 37°C ± 0.5. The dilution medium was stirred continuously on the magnetic stirrer at the maximum r/min. The cellophane membrane was precisely kept on the top of the receptor chamber and above it the drug chamber was kept. The clamp was attached to avoid the shifting of the membrane and leakage of the formulation. The sample was withdrawn through the sample port using syringe in the time interval of 60 min.

 

Evaluations of ethosomal gel:

·       Organoleptic characterization18,31

·       Viscosity23,25,30

·       pH23,26

·       Spreadability18,27

·       Tube extruability8

·       Drug contain18, 23, 26

·       Drug released18,20,30,33

·       Irritation study

·       Stability study31,33,34

 

Organoleptic Character:27,31

The organoleptic character of the ethosomal gel and non ethosomal gel was determined. The colour and odor and homogeneity were checked by visual inspection.

 

Viscosity:23,26,27,30

The viscosity was determined using the brook field viscometer. The r/min set at 25 unit and temperature was 25°C, at constant torque %. The readings were taken in triplicates using spindle no.63 (LV-1). The averages of three readings were recorded for more precise results.

 

pH:23,26

The pH of topical preparation should be evaluated for the compatibility of the gel. To test the pH of formulated gels, the gels were first diluted by using distilled water in dilution factor of 100 (gel: deionized water = 1:100). After that suspensions were formed, the pH of each suspensions tested by using pH meter (Sigma-27 DP).

 

Spreadability:18,27

The spreadability of both the types of gel was also measured in which the gel was sandwiched between the two slides across the length of 6 cm apart same as that of the ethosomes.

 

Tube Extruability:8

The gel was filled with the collapsible metal or aluminums tubes. The weight of tubes was taken. Then the load was given to the tube to extrude at least 0.5 cm ribbon of material in 10 sec. The test was performed in triplicates and the average was calculated. The extruability was calculated by using following formula.

 

                          Weight applied to extrude gel form tube (gram

Extruability = –––––––––––––––––––––––––––––––––––––––

                                                  Area (cm2)

 

Drug Content:18,23

The drug content was determined by UV spectroscopy. The standard solution, test solution was prepared and absorbance was measured at (λmax). The drug content was calculated by using standard plot.

 

Drug Release:18,20,30,33

The drug release was studied on the Franz diffusion cell using the cellophane membrane. The procedure used was same as that for the ethosomes. Diffusion apparatus: Fran’s diffusion cell; Volume of diffusion medium: 5.5 ml; Speed: max. Rpm; Temperature: 37 ± 0.5°C; Dissolution medium: Phosphate buffer (pH 6.8); Sampling interval: 60min; Quantity of sample withdrawn: 1ml; Samples analyzed: UV (λmax) at 416 nm and absorbance; Cumulative percent drug release was calculated.

 

Irritation Test:

The irritation test was done by simply spreading the gel on the skin and observing any changes on the skin22.

 

Stability Study:13, 31, 33, 34,36

The stability study was important parameter for the measurement of shelf life and storage temperature. It was mandatory to check the effect of environmental conditions on the product quality. The change in the quality of product can lead to the therapeutic efficacy of the dosage form.  The ethosomes were evaluated at initial day, 30 days, and 90 days according to its Entrapment efficiency, diffusion study, pH, and viscosity.

 

RESULT AND DISCUSSION:

Ethosomal Formulation:

The ethosomes were made by using the lecithin and castor oil as phospholipids which is responsible for formation of vesicles. Ethanol is used as penetration enhancer. In B2 and B3 the concentration of lecithin was kept same and in the B4 formulation the lecithin was not added. In B4 the vesicle former added was castor oil which was not be used in the B2 formulation. The concentration of ethanol was changed in all formulations. The lemon oil used as a flavoring agent.

 

Physicochemical Properties of Ethosomes:

The physical properties like vesicle shape, vesicle size, spreadability and the chemical properties like pH of ethosomes were performed and the results are presented in the Table 2. The vesicle size of all four batches was in the range and the shape was perfectly spherical as shown into microscopical image of ethosomes in fig 2. The spreadability found was good with pH ranging from 6.81 to 6.86 holding them most acceptable to avoid the risk of irritation after application on the skin.

 

Fig. 2: Microscopical study of formulated batches.


 

Table No.2: Characterization of Ethosomal Batches.

Batches

Vesicle Size(nm)

Vesicle Shape

Spreadability*(gm.cm/sec)

pH*

Viscosity (cp)

B1

240 - 760

Spherical

39.1 ± 0.28

6.86 ± 0.02

193.56

B2

140 - 517

Spherical

57.3 ± 0.36

6.81 ± 0.01

112.83

B3

160 - 620

Spherical

44.9 ± 0.31

6.83 ± 0.04

96.23

B4

310 - 840

Oval

36.8 ± 0.26

6.84 ± 0.02

268.29

* SD: Standard deviation, (n=3).

 


Drug Loading Capacity:

The drug loading capacity was same as the entrapment efficiency which gives the idea of amount of drug loaded per unit weight of the vesicle. It was an important parameter for the nano medicines. B2 had maximum loading capacity as the concentration of ethanol used was more. Loading capacity of B4 was minimum. The other two batches had almost same drug loading capacity.

 

Entrapment efficiency:

The entrapment efficiency (EE) ranges from 42.2  ±  1% to 88.5 ± 2%. B2 batch had the maximum whereas B4 batch had the lowest %EE. The maximum %EE of B2 batch was due to the average more amounts of the phospholipids, polyglycol and ethanol. B4 had lowest %EE due to the absence of the lecithin as a phospholipids. If all batches are compared then the entrapment efficiency increased with increase in the concentration of ethanol as ethanol is responsible for the penetration of the drug in the vesicles.  However it was also observed that the 70% of polyglycol also increased the %EE as it is also a penetration enhancer. Data of %DLC and %EE is given in Fig. 3

 

Zeta Potential:

The Zeta potential observed in fig.no.4 of B2 was found to be -28.5mV .The values indicates that batches had good physical stability due to electrostatic repulsion of individual particle. The solution resists aggregation.

 

 

Fig. 3: Comparative study of %DLC and %EE of ethosomal formulation.

 

In-vitro drug release:

The diffusion study of ethosomes gave promising results. The results were in between 60 to 80 %. The B2 gave maximum release so we considered B2 as the optimized batch. B1 and B3 gave almost same drug release. The B4 gave minimum drug release as compared to the other batches as the %EE, %CDR and other parameters of B4 were also not satisfying. It concludes that the presence of lecithin helps to prepare better ethosomes with promising results. Data mentioned in (fig 5) and comparison of %CDR given in Table 3.


 

 

Fig. 4: Zeta potential of optimized B2 ethosomes.

 

   

a) S.grandiflora ethosomes                                                               b) Ethosomal gel and non ethosomal gel

Fig. 5: a) Comparison of in-vitro drug diffusion studies among the four batches of S.grandiflora ethosomes. b) Comparison of in-vitro drug diffusion studies of ethosomal gel and non ethosomal gel.

 

  

a) Zero Order Model                                                                 b) First Order Model

   

c) Higuchi's Model                                                            d) Peppa's Model

Fig. 6 (a, b, c, d): In vitro diffusion kinetics of ethosomal gel and non ethosomal gel.

 


Table 3: In-Vitro Drug Diffusion Studies of Formulations.

TIME (min)

%CDR(Cumulative drug release)

B1

B2

B3

B4

0

0.00

0.00

0.00

0.00

60

8.80

9.28

8.25

7.21

120

16.48

18.64

15.71

13.33

180

27.08

32.01

28.73

23.56

240

40.10

45.52

40.02

36.18

300

54.04

62.52

53.48

48.31

360

66.40

75.64

70.02

57.94

420

72.02

85.38

77.91

63.12

 

Gel Formulation:

Organoleptic Characterization:

The color of ethosomal gel (EG) observed was Chartreuse yellow while of non ethosomal gel (NEG) was yellow green. The EG had smooth texture while NEG was uneven. The homogeneity and consistency of EG was excellent whereas NEG was satisfactory. The picture of the gels is given below to know the physical appearance. It was given in Table 4.

 

Physicochemical properties:

The viscosity of the EG was in the range of 43 163.6 cps – 56 289.4cps and of NEG was 46 521.6cps. The viscosity depends on the type and concentration of polymer used in the formulation. Higher the concentration of the polymer more is the viscosity and lesser is the drug release. So, viscosity of all the batches was in the limit. The pH of the gel observed was in the range of   6.43 - 6.76. It is compatible with pH of the skin so irritation problem will not occur. The spreadability was also good i.e. 16.49 gm.cm/sec - 32.34 gm.cm/sec and tube extruability measured was in the range of 21.91 g/cm2 - 39.14 g/cm2.30


Table 4: Organoleptic Characterization and Physicochemical Evaluation of Ethosomal Gel and Non Ethosomal Gel

Batches

Texture

Homogeneity

Odour

Consistency

Viscosity(cps)

(mean ± SD*)

pH

(mean ± SD*)

Spreability

(gm.cm/sec)

Tube extrudability

(g/cm2) (mean ± SD*)

EG1

Smooth

Excellent

Sweet

Excellent

48 251.3 ± 5.12

6.73 ± 0.05

22.68 ± 0.91

27.21 ± 0.89

EG2

Smooth

Excellent

Sweet

Excellent

38 085.1 ± 4.34

6.66 ± 0.01

32.34 ± 1.66

39.14 ± 1.53

EG3

Smooth

Excellent

Sweet

Excellent

43 163.6 ± 5.41

6.53 ± 0.04

27.10 ± 1.34

33.16 ± 1.41

EG4

Smooth

Good

Sweet

Fair

56 289.4 ± 7.64

6.76 ± 0.02

16.49 ± 0.72

21.91 ± 0.85

NEG

Uneven

Fair

Nil

Satisfactory

46 521.6 ± 5.37

6.43 ± 0.09

25.05 ± 1.28

29.95 ± 1.32

 


Drug Content:

The drug content of EG was in the range of 98.93 % to 99.71 % and of NEG was 98.41 %. Thus, EG had high drug content than NEG. EG2 had maximum drug content so the release will also be maximum and this batch can be considered as optimized.

 

In-vitro Drug Release and Kinetic Study:

The table no.5 shows that the EG2 had maximum drug release than all the other batches. NEG had minimum drug release it means that the ethosomal gel is novel and had many advantages over the non ethosomal gel. The drug release of EG ranges from 59.85 % - 81.06 % and of NEG was 25.86 %. The drug kinetic given in table no.5 and fig. 6 (a, b, c, d)

 

Table 5: In Vitro Drug Release Profile of Ethosomal Gel and Non Ethosomal Gel and Data of Drug Kinetics of Ethosomal Gel.

TIME(min)

%CDR

EG1

EG2

EG3

EG4

NEG

0

0.00

0.00

0.00

0.00

0.00

15

8.62

8.95

7.86

6.45

2.81

30

14.06

14.09

14.26

11.91

5.33

60

18.35

24.15

26.61

21.62

9.43

120

26.92

37.65

38.13

33.16

14.72

210

38.56

59.83

50.37

44.17

19.68

330

51.38

73.39

66.51

52.44

23.32

480

64.22

81.06

73.15

59.86

25.86

Kinetic Model

R2

EG1

EG2

EG3

EG4

NEG

Zero Order Kinetic

0.96

0.97

0.98

0.99

0.98

First Order Kinetic

0.87

0.90

0.94

0.97

0.98

Higuchi’s Model

0.82

0.82

0.85

0.86

0.87

Peppa’s Model

0.96

0.96

0.98

0.98

0.98

Best Fitted Model

Zero Order

Zero Order

Zero Order

Zero Order

Zero Order

%CDR: % Cumulative drug release; EG: Ethosomal gel; NEG: Non ethosomal gel.

 

Stability Study:

The change in the results of stability study was negligible. The fractional change in the viscosity indicated that the gel formulation was physically stable till 90 days. The pH remained unchanged which indicated it is chemically stable and non irritants to the skin. The drug content remained same and also the drug release didn’t change. All the formulation gave good results so the gels prepared were stable till the end of 90 days. It was given in Table 6.

 

Table 6: Stability Study of Ethosomal Gel and Non Ethosomal Gel.

Parameters

Batches

Initial Day

After 30 Days

After 90 Days

 

 

Viscosity

(cps)

EG1

48 251.3 ± 5.12

48 404.1 ± 6.23

48 889.5 ±

5.46

EG2

38 085.1 ± 4.34

38 245.3 ±

5.38

38 605.9 ±

4.35

EG3

43 163.6 ± 5.41

43 354.1 ±

5.69

43 736.6 ±

6.98

EG4

56 289.4 ± 7.64

56 499.4 ±

8.03

56 846.1 ±

8.45

NEG

46 521.6 ± 5.37

46 852.5 ±

6.82

47 012.5 ±

6.54

 

pH

 

 

EG1

6.73 ± 0.05

6.70 ± 0.05

6.64 ± 0.06

EG2

6.66 ± 0.01

6.61 ± 0.06

6.57 ± 0.02

EG3

6.53 ± 0.04

6.49 ± 0.03

6.42 ± 0.03

EG4

6.76 ± 0.02

6.71 ± 0.01

6.62 ± 0.02

NEG

6.43 ± 0.09

6.39 ± 0.06

6.32 ± 0.04

 

% Entrapment Efficacy

 

EG1

57.9 ± 1.05

55.1 ± 1.56

51.3 ± 1.68

EG2

88.5 ± 2.14

86.6 ± 7.14

84.9 ± 6.03

EG3

72.6 ± 2.04

70.7 ± 1.86

64.6 ± 7.42

EG4

42.2  ± 1.85

39.5  ± 7.04

33.4  ± 8.06

NEG

0.00  ± 1.47

00.0  ± 1.42

00.0  ± 1.87

 

% Drug Content

EG1

55.1 ± 1.08

98.19 ± 3.48

97.85 ± 3.79

EG2

51.3 ± 1.02

98.89 ± 1.97

98.01 ± 2.16

EG3

98.93 ± 2.04

98.13 ± 3.78

97.23 ± 3.98

EG4

99.39 ± 3.16

98.66 ± 3.37

97.49 ± 4.79

NEG

98.41 ± 2.84

97.86 ± 3.46

96.91 ± 4.69

% Drug released

(At 420 min)

EG1

64.22

63.65

60.59

EG2

81.06

79.39

77.95

EG3

73.15

69.97

66.87

EG4

59.85

56.89

53.63

NEG

25.83

23.35

21.27

EG: Ethosomal Gel; NEG: Non Ethosomal Gel

 

CONCLUSION:

The study revealed that ethosomes can be considered as a possible vesicular carrier for transdermal delivery of S.grandiflora leaves extract. The formulation was successfully prepared by loading leaves extract, phospholipids; ethanol and ethosomal gel-based formulations were prepared with hydrophilic polymer carbomer. The ethosomes were spherical and discrete in shape. The size of vesicle was found to be in the range and sensible for skin penetration. The ethosomes showed highest entrapment efficiency and rapidly penetrate through the skin because of tiny vesicular size. The kinetic study of ethosomal gel shows that the formulations were follow zero order models means the drug is released at constant rate. The viscosity of the gel was four times greater than the ethosomes. So, it can prevent the aggregation of ethosomes, stabilize the formulation and avoid increasing size of vesicles which was analyzed by zeta potential result. As viscosity increases the spreadability decreases and the results obtained follow the same. The carbomer used for gel is acidic in nature and it can be quite irritating to the skin so we used triethanolamine to balance pH. The stability study carried out for the period of 90 days showed negligible changes at room temperature. Ethosomal gel gave high in-vitro drug release than the non-ethosomal gel. The highest drug release leads to the increase in the bioavailability which indicates that the ethosomes are advanced nanoparticles. Hence it is concluded that S.grandiflora leaves extract loaded ethosomal is advance over the non ethosomal gel.

 

ACKNOWLEDGMENT:

We are thankful to our guide Sachin Devidas Rede, providing us innovative and thoughtful domain so that we could complete our research work successfully.

 

REFERENCE:

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Received on 26.12.2020            Modified on 26.03.2021

Accepted on 11.05.2021           © RJPT All right reserved

Research J. Pharm.and Tech 2022; 15(3):1029-1036.

DOI: 10.52711/0974-360X.2022.00172