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National Expressway, Banmore Near Gwalior M.P
Formulation Development and Evaluation of Clobetasol
Propionate Transferosomal Gel
ShriRam College of Pharmacy
Content…
Literature Review
Material and Methods
Drug and Excipient
Introduction
Experimental Work
Result
INTRODUCTION
• The development of topical medicine administration has received
a lot of attention over the past few decades since it offers a variety
of benefits. A typical adult's skin has a surface area of around 2
mm, weighs 3 kg, and gets roughly one-third of the blood that the
body circulates.
• Topical delivery of drug means the application of drug to skin for
the localized effect, and in transdermal drug delivery system
(TDDS) skin is used as a potential route for the delivery of the
systemic action of drugs.
• TDDS is One of the medication delivery method that has excellent patient
compliance. Some potential benefits of transdermal route over other
traditional routes, such as oral route and parenteral route, include avoiding
first-pass metabolism, predictable and extended duration of activity,
minimizing undesirable side effects, improving physiological and
pharmacological response, utility of short half-life drugs, avoiding the
fluctuation in drug levels, inter-patient variations, and most importantly, it
provides patients convenience.
• The major obstacle to dermal and transdermal drug delivery is the
permeation characteristics of the stratum corneum, which limits drug
transport, making this route of administration frequently insufficient
for the medical use.
• Stratum corneum is one of the top layer of the epidermis consists of
keratinized, flattened remnants of once actively dividing epidermal
cells, i.e. impermeable in water and behaves as tough flexible
membrane.
• Many technologies and systems have been investigated to evade this
barrier including the electrophoresis, iontophoresis, chemical
permeation enhancers, microemulsions, sonophoresis, and as well as
utilizing vesicular systems such as liposome, niosome, ethosome, and
transferosome, and the most promising technique to formulate novel
vesicular carrier for delivery through the skin as it delivered drug at
sustained or controlled manner.
Schematic representation of the two microroutes of penetration
Diagram of transferosome
• Transferosomes enjoy a benefit as phospholipids vesicles utilized
for transdermal medication conveyance. Due to their self optimized
and super adaptable film properties, they progressively convey drug
either into or through the skin, relies upon the decision of
organization or application, alongside high productivity.
Transferosomes are better than the standard liposomes in versatile
property and along these lines more appropriate for the skin
entrance. Transferosomes pressing themselves along the
intracellular fixing lipid of the layer corneum and defeat the skin
infiltration trouble.
• Transferosomes have high vesicle deformability, which allows the
section because of the mechanical pressure of encompassing, in a self-
collecting way. Adaptable nature of transferosomes layer is
accomplished by expansion of reasonable surface-dynamic segments in
phospholipids in legitimate proportion.
• Adaptability in transferosomes layer diminishes the danger of vesicle
burst in the skin and allows transferosomes to follow the normal water
slope across the epidermis when applied under nonocclusive condition.
• Transferosomes precipitously enter the flawless layer corneum
alongside two courses in the intracellular lipid that contrast in their
bilayers properties.
AIM & OBJECTIVES
Aim and Objectives
Aim: Formulation development and evaluation of clobetasol
Propionatetransferosomal gel
Objectives:
 Preformulation study
 Formulation of candy
 Evaluation of candy
 Stability study of candy.
PLAN OF WORK
Plan of Work
1. Literature review
2. Based on Drug
3. Based on Formulation
4. Selection of Drug and Polymer
5. Preformulation study of Drug
• Organoleptic characterization
• FT-IR spectroscopy
• UV-visible spectroscopy
• Melting point
• Partition coefficient
• Solubility
Plan of Work
5. Preformulation study of Drug
• Organoleptic characterization
• FT-IR spectroscopy
• UV-visible spectroscopy
• Melting point
• Partition coefficient
• Solubility
Plan of Work
6. Preparation of Transferosomal Gel
Characterization of
TransferosomalMorphology
• Vesicle size and size distribution
• Entrapment efficiency (%)
• In vitro release study
• Preparation of transferosomal gel
• Evaluation of transferosomal gel
• Percentage drug content
• Percentage drug release
• Drug release kinetic study
• Appearance: CP occurs as a white, almost white or
cream-coloured, crystalline powder and is odourless.
• Melting Range: CP has a melting range of
approximately 195.5-197.0°C.
• Solubility: Clobetasol propionate Drug is soluble in
organic solvents such as), ethanol
• (C2H5OH), Dimethyl Sulfoxide (DMSO) and Dimethyl
Formamide (DMF), which should be purged with as an inert
gas. The solubility of clobetasol propionate in ethanol is
approximately
1 mg/ml and approximately 25 mg/ml in DMSO and DMF38.
• LogP: 2.48 (LogP)
S. No. MATERIALS MANUFACTURER
1. Phospholipids Lipoid, Germany.
2. Clobetasol propionate Leisha pharam Pvt. Ltd. Bhiwadi
3. Cholesterol Thomas baker (chemical), Mumbai.
4. Ethanol Changshu yangquan chemical, China.
5. Methanol Finar Pvt.Lltd. Ahmedabad
6. Span 80 Avarice Laboratories Pvt. Ltd, G.B nagar, India.
7. Tween 20 Molychem, Mumbai.
8. Tween 80 Thomas baker (chemical), Mumbai.
9. Sodium chloride Thomas baker (chemical), Mumbai.
10. Disodium hydrogen
phosphate Thomas baker (chemical), Mumbai.
11. Potassium dihydrogen
phosphate Molychem, Mumbai.
Material and Methods
S. No. INSTRUMENTS MANUFACTURER
1. UV/VIS Spectrophotometer UV-1700 Shimadzu
2. Weighing balance Shimadzu
3. Microscope Kyowa Getnar
4. pH meter Lab india pH/con meter
5. Centrifuge machine Remi
6. Sonicator Digital ultrasonic cleaner
7. FTIR FTIR-8400S Shimadzu, japan
8. Rota evaporator Super scientific pvt. ltd, vadodara
9. Particle size and zeta potential Malvern
Material and Methods
Experimental Work
• Preformulation studies
• Organoleptic properties
• Melting point
• Solubility
• Drug- excipients compatibility study
• Partition coefficient studies
• Physical appearance
• Vesicles size, polydispersity index, and zeta
potential
• Entrapment efficiency determination
Formulation Clobetasol
Propionate
(w/w)
Soya
Lecithin
(%w/w)
Surfactant (%w/w)
Tween 80 Span 80 Tween 20
CT1 0.05% 80 20 - -
CT2 0.05% 80 - 20
CT3 0.05% 80 - - 20
CT4 0.05% 90 10 - -
CT5 0.05% 70 30 - -
CT6 0.05% 60 40 - -
CT7 0.05% 50 50 - -
Formulation code Clobetasol propionate
containing transferosome
Carbapol
concentration
%w/w)
CT1G1 Equivalent to 0.05% 0.5
CT1G2 Equivalent to 0.05% 1
CT1G3 Equivalent to 0.05% 1.5
CT1G4 Equivalent to 0.05% 2
Result
8.1 Preformulation studies
8.1.1 Preparation of standard curve of clobetasol propionate in methanol
Table 6: Absorbance of different dilutions of drug at 238 nm in
methanol
Con.(µg/ml)Absorbance
1 0.036±0.031
2 0.147±0.009
3 0.251±0.083
4 0.360±0.0047
5 0.457±0.0018
6 0.545±0.056
7 0.638±0.037
8 0.744±0.006
9 0.852±0.0918
10 0.948±0.052
y = 0.1002x
- 0.0532
R² = 0.9994
0
0.1
0.2
0.3
0.4
0.5
0.6
0.7
0.8
0.9
1
0 5 10 15
Absorbance
Con.(
µg/ml)
Absorbance
Linear (Absorbance)
kri.pptx

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kri.pptx

  • 1. National Expressway, Banmore Near Gwalior M.P Formulation Development and Evaluation of Clobetasol Propionate Transferosomal Gel ShriRam College of Pharmacy
  • 2. Content… Literature Review Material and Methods Drug and Excipient Introduction Experimental Work Result
  • 4. • The development of topical medicine administration has received a lot of attention over the past few decades since it offers a variety of benefits. A typical adult's skin has a surface area of around 2 mm, weighs 3 kg, and gets roughly one-third of the blood that the body circulates. • Topical delivery of drug means the application of drug to skin for the localized effect, and in transdermal drug delivery system (TDDS) skin is used as a potential route for the delivery of the systemic action of drugs.
  • 5. • TDDS is One of the medication delivery method that has excellent patient compliance. Some potential benefits of transdermal route over other traditional routes, such as oral route and parenteral route, include avoiding first-pass metabolism, predictable and extended duration of activity, minimizing undesirable side effects, improving physiological and pharmacological response, utility of short half-life drugs, avoiding the fluctuation in drug levels, inter-patient variations, and most importantly, it provides patients convenience.
  • 6. • The major obstacle to dermal and transdermal drug delivery is the permeation characteristics of the stratum corneum, which limits drug transport, making this route of administration frequently insufficient for the medical use. • Stratum corneum is one of the top layer of the epidermis consists of keratinized, flattened remnants of once actively dividing epidermal cells, i.e. impermeable in water and behaves as tough flexible membrane. • Many technologies and systems have been investigated to evade this barrier including the electrophoresis, iontophoresis, chemical permeation enhancers, microemulsions, sonophoresis, and as well as utilizing vesicular systems such as liposome, niosome, ethosome, and transferosome, and the most promising technique to formulate novel vesicular carrier for delivery through the skin as it delivered drug at sustained or controlled manner.
  • 7. Schematic representation of the two microroutes of penetration
  • 9. • Transferosomes enjoy a benefit as phospholipids vesicles utilized for transdermal medication conveyance. Due to their self optimized and super adaptable film properties, they progressively convey drug either into or through the skin, relies upon the decision of organization or application, alongside high productivity. Transferosomes are better than the standard liposomes in versatile property and along these lines more appropriate for the skin entrance. Transferosomes pressing themselves along the intracellular fixing lipid of the layer corneum and defeat the skin infiltration trouble.
  • 10. • Transferosomes have high vesicle deformability, which allows the section because of the mechanical pressure of encompassing, in a self- collecting way. Adaptable nature of transferosomes layer is accomplished by expansion of reasonable surface-dynamic segments in phospholipids in legitimate proportion. • Adaptability in transferosomes layer diminishes the danger of vesicle burst in the skin and allows transferosomes to follow the normal water slope across the epidermis when applied under nonocclusive condition. • Transferosomes precipitously enter the flawless layer corneum alongside two courses in the intracellular lipid that contrast in their bilayers properties.
  • 12. Aim and Objectives Aim: Formulation development and evaluation of clobetasol Propionatetransferosomal gel Objectives:  Preformulation study  Formulation of candy  Evaluation of candy  Stability study of candy.
  • 14. Plan of Work 1. Literature review 2. Based on Drug 3. Based on Formulation 4. Selection of Drug and Polymer 5. Preformulation study of Drug • Organoleptic characterization • FT-IR spectroscopy • UV-visible spectroscopy • Melting point • Partition coefficient • Solubility
  • 15. Plan of Work 5. Preformulation study of Drug • Organoleptic characterization • FT-IR spectroscopy • UV-visible spectroscopy • Melting point • Partition coefficient • Solubility
  • 16. Plan of Work 6. Preparation of Transferosomal Gel Characterization of TransferosomalMorphology • Vesicle size and size distribution • Entrapment efficiency (%) • In vitro release study • Preparation of transferosomal gel • Evaluation of transferosomal gel • Percentage drug content • Percentage drug release • Drug release kinetic study
  • 17.
  • 18. • Appearance: CP occurs as a white, almost white or cream-coloured, crystalline powder and is odourless. • Melting Range: CP has a melting range of approximately 195.5-197.0°C. • Solubility: Clobetasol propionate Drug is soluble in organic solvents such as), ethanol • (C2H5OH), Dimethyl Sulfoxide (DMSO) and Dimethyl Formamide (DMF), which should be purged with as an inert gas. The solubility of clobetasol propionate in ethanol is approximately 1 mg/ml and approximately 25 mg/ml in DMSO and DMF38. • LogP: 2.48 (LogP)
  • 19. S. No. MATERIALS MANUFACTURER 1. Phospholipids Lipoid, Germany. 2. Clobetasol propionate Leisha pharam Pvt. Ltd. Bhiwadi 3. Cholesterol Thomas baker (chemical), Mumbai. 4. Ethanol Changshu yangquan chemical, China. 5. Methanol Finar Pvt.Lltd. Ahmedabad 6. Span 80 Avarice Laboratories Pvt. Ltd, G.B nagar, India. 7. Tween 20 Molychem, Mumbai. 8. Tween 80 Thomas baker (chemical), Mumbai. 9. Sodium chloride Thomas baker (chemical), Mumbai. 10. Disodium hydrogen phosphate Thomas baker (chemical), Mumbai. 11. Potassium dihydrogen phosphate Molychem, Mumbai. Material and Methods
  • 20. S. No. INSTRUMENTS MANUFACTURER 1. UV/VIS Spectrophotometer UV-1700 Shimadzu 2. Weighing balance Shimadzu 3. Microscope Kyowa Getnar 4. pH meter Lab india pH/con meter 5. Centrifuge machine Remi 6. Sonicator Digital ultrasonic cleaner 7. FTIR FTIR-8400S Shimadzu, japan 8. Rota evaporator Super scientific pvt. ltd, vadodara 9. Particle size and zeta potential Malvern Material and Methods
  • 21. Experimental Work • Preformulation studies • Organoleptic properties • Melting point • Solubility • Drug- excipients compatibility study • Partition coefficient studies • Physical appearance • Vesicles size, polydispersity index, and zeta potential • Entrapment efficiency determination
  • 22. Formulation Clobetasol Propionate (w/w) Soya Lecithin (%w/w) Surfactant (%w/w) Tween 80 Span 80 Tween 20 CT1 0.05% 80 20 - - CT2 0.05% 80 - 20 CT3 0.05% 80 - - 20 CT4 0.05% 90 10 - - CT5 0.05% 70 30 - - CT6 0.05% 60 40 - - CT7 0.05% 50 50 - -
  • 23. Formulation code Clobetasol propionate containing transferosome Carbapol concentration %w/w) CT1G1 Equivalent to 0.05% 0.5 CT1G2 Equivalent to 0.05% 1 CT1G3 Equivalent to 0.05% 1.5 CT1G4 Equivalent to 0.05% 2
  • 25. 8.1 Preformulation studies 8.1.1 Preparation of standard curve of clobetasol propionate in methanol Table 6: Absorbance of different dilutions of drug at 238 nm in methanol Con.(µg/ml)Absorbance 1 0.036±0.031 2 0.147±0.009 3 0.251±0.083 4 0.360±0.0047 5 0.457±0.0018 6 0.545±0.056 7 0.638±0.037 8 0.744±0.006 9 0.852±0.0918 10 0.948±0.052
  • 26. y = 0.1002x - 0.0532 R² = 0.9994 0 0.1 0.2 0.3 0.4 0.5 0.6 0.7 0.8 0.9 1 0 5 10 15 Absorbance Con.( µg/ml) Absorbance Linear (Absorbance)