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Proniosomes- A Promising
Drug Carrier
Prepared by
Siddhartha Mukherjee
M.Pharm(Pharmaceutics), Semester-II
Dept. of Pharmaceutics, Amity Institute of Pharmacy, Amity University,
Noida
SCHEME OF PRESENTATION
• Introduction
• Necessity
• Advantages over similar dds
• Formation methodology
• Characterization & evaluation
• Stability studies
• Applications
• Conclusion
• References
INTRODUCTION
• Proniosome is dry formulation using a suitable carrier coated
with non-ionic surfactants and can be converted into
niosomes immediately before use by hydration.
• These proniosome-derived niosomes are as good as or even
better than conventional niosomes.
• Approaches to stabilize niosomal drug delivery system
without affecting its properties of merits have resulted in the
development of promising drug carriers
Preparation of Niosomes from
Proniosomes by hydration
 Prepared proniosome powder is weighed and filled in screw
cap vials. Water or saline at 80°C is added and the vials
capped.
 The vials are attached to a vortex mixer and agitated for 2
minutes to get niosomal suspension.
ADVANTAGES
• Proniosomes - dry formulations of surfactant coated
carrier- rehydrated by brief agitation in water.
• Minimizes problems of niosome physical stability such
as, aggregation, fusion and leaking of entrapped drug.
• Additional convenience in transportation, distribution,
storage and dosing.
• Can carry both hydrophilic drugs and hydrophobic
drugs.
• Extensively used in various drug delivery systems like
drug targeting controlled release and permeation
enhancement of drugs
DISADVANTAGES
• Complex process
• During hydration to niosomes, the complete drug
entrapment may not be possible, some times Hence
the amount of the un entrapped dug should be
analyzed
Methods of Preparation
• Slurry method
• Co-acervation phase separation
• Slow spray-coating method
8
Slurry Method
10g Maltodextrin
As
a carrier
in
250ml RBF
Entire
14.5ml volume
Of
surfactant solution
Formation of Slurry
Dry Proniosome powder
Stored
In
sealed container at 4o
C
9
Co-acervation Phase Separation
Method
Drug+surfactant+lipid
In
5ml glass vial
0.5ml of Alcohol
Warm at 60-70C for
5min
Mix all ingredients
Until
SAA is dissolved
Aq.0.1%
glycerol
soln
A clear soln,
converted to proniosomal gel
On cooling
Warm on
water bath
Slow spray coating method
• This method involvs preparation of proniosome by
spraying surfactant in organic solvent onto sorbitol
powder and then evaporating.
• The surfactant coating on the carrier is very thin and
hydration of this coating allows multilamellar
vesicles as the carrier dissolves.
• The resulting niosomes are very similar to the
conventional niosomes but are more uniformely
distributed
Characterization of
Proniosomes
• Measurement of angle of repose
• Scanning electron microscopy (SEM)
• Optical microscopy
• Measurement of vesicle size
• Drug content
• Entrapment efficiency
• In-vivo release studies
• Stability studies
ANGLE OF REPOSE
The angle of repose of dried proniosomes was measured by funnel
method. The funnel, which was fixed at a position and the
proniosomal powder was poured into it so that the outlet orifice of
the funnel is 10 cm above the level of surface. The powder flowed
down from the funnel to form a cone on the surface and then angle
of repose was further calculated by measuring the height of the cone
and the diameter of its base.
SEM
Particle size of proniosomes is a factor of prime importance. The
surface morphology and size distribution of proniosomes were
studied by SEM. A double-sided tape that was affixed on aluminum
stubs and the proniosomal powder was spread on it. The aluminum
stub was placed in a vacuum chamber of scanning electron
microscope (XL 30 ESEM with EDAX, Philips, Netherlands)
SEM Image
SEM images of pure maltodextrin proniosomes
OPTICAL MICROSCOPY
• Optical Microscopy designed for viewing samples by
transmitted light magnification is carried out by means of
two lenses: objective lens which creates an image at
infinity weak tube lens which then forms a real image in
its focal plane
Vesicle size determination by Optical microscopy
 ENTRAPMENT EFFICIENCY
Separation of unentrapped drug from the niosomal suspension was
carried out by exhaustive dialysis method and centrifugation
method. Theniosomal suspension was taken into a dialysis tube to
which osmotic cellulose membrane was securely attached to one
side, the dialysis tube was suspended in 100 ml saline buffer at
certain pH, which was stirred on a magnetic stirrer. The niosomal
suspension and the unentrapped drug were seperated into the
medium through osmotic cellulose membrane. After 6 h of
exhaustive dialysis, optical density values were noted and the
estimation of the entrapped drug was carried out by UV
spectrophotometric method. Entrapment Efficiency was calculated
using the formula.
 DRUG CONTENT
Proniosomes equivalent to 100 mg were taken in a standard volumetric
flask. They were lysed with 50 ml methanol by shaking for 15 min.
The solution was diluted to 100 ml with methanol. Then 10 mlof
this solution was diluted to 100 ml with saline phosphate buffer at
certain pH. Aliquots were withdrawn and absorbance was measured
at a certain wavelength and drug content was further calculated from
the calibration curve.
 RELEASE STUDIES
The release of the drug from the proniosomal formulations was
determined using different techniques such as Franz diffusion cell,
Keshary-Chien diffusion cell, Cellophane dialyzing membrane,
United states pharmacopeia (USP) dissolution apparatus Type-1,
spectrapor molecular porous membrane tubing.
STABILITY STUDIES
International conference on harmonization (ICH) guidelines
suggests stability studies for the dry proniosome powders
meant for reconstitution should be studied for accelerated
stability at 40°C/75% relative humidity as per international
climatic zones and climatic conditions (WHO, 1996). For long
term stability studies the temperature is 25°C/60% RH for the
countries in zone I and II and for the countries in zone III and
IV the temperature is 30°C/65% Relative humidity (RH).
Product should be evaluated for appearance, color, assay, pH
preservative content, particulate matter, sterility, and
pyrogenicity.
APPLICATIONS
MARKET FORMULATION
• Using their in-depth knowledge of cellular
organisation, Lancôme Laboratories have created
Multi-Tension Technology, to strengthen the skin's
natural protein network, thereby promoting firmness
and elasticity for immediate results.
CONCLUSION
 It is concluded that the concept of incorporating the drug into
niosomes for a better targeting of the drug at appropriate tissue
destination is widely accepted by researchers and
academicians.
 Proniosomes based niosomes are thoughts to be better
candidates drug delivery as compared to liposomes due to
various factors like cost, stability etc.
 Various types of drug deliveries can be possible using
proniosomes based niosomes like targeting, ophthalmic ,
topical, transdermal etc.
More researches have to be made in this field to come out with
all the potential in this novel drug delivery system.
REFERENCES
• Vyas S.P., Khar R.K., Targeted & Controlled Drug Delivery:
Novel Carrier Systems. Pg no. 249-279
• Malhotra M., Jain N.K., Niosomes As Drug Carriers. Pg no.
81-86
• Li Q, Li Z, Zeng W, et al. Proniosome-derived niosomes for
tacrolimus topical ocular delivery: in vitro cornea permeation,
ocular irritation, and in vivo anti-allograft rejection. Eur J
Pharm Sci. 2014;62:115–123.
• Alsarra IA, Bosela AA, Ahmed SM, Mahrous GM. (2005).
Proniosomes as a drug carrier for transdermal delivery of
ketorlac. Eur J Pharm Biopharm, 59, 485–490.
Promising Proniosomes Drug Carrier

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Promising Proniosomes Drug Carrier

  • 1. Proniosomes- A Promising Drug Carrier Prepared by Siddhartha Mukherjee M.Pharm(Pharmaceutics), Semester-II Dept. of Pharmaceutics, Amity Institute of Pharmacy, Amity University, Noida
  • 2. SCHEME OF PRESENTATION • Introduction • Necessity • Advantages over similar dds • Formation methodology • Characterization & evaluation • Stability studies • Applications • Conclusion • References
  • 3. INTRODUCTION • Proniosome is dry formulation using a suitable carrier coated with non-ionic surfactants and can be converted into niosomes immediately before use by hydration. • These proniosome-derived niosomes are as good as or even better than conventional niosomes. • Approaches to stabilize niosomal drug delivery system without affecting its properties of merits have resulted in the development of promising drug carriers
  • 4. Preparation of Niosomes from Proniosomes by hydration  Prepared proniosome powder is weighed and filled in screw cap vials. Water or saline at 80°C is added and the vials capped.  The vials are attached to a vortex mixer and agitated for 2 minutes to get niosomal suspension.
  • 5. ADVANTAGES • Proniosomes - dry formulations of surfactant coated carrier- rehydrated by brief agitation in water. • Minimizes problems of niosome physical stability such as, aggregation, fusion and leaking of entrapped drug. • Additional convenience in transportation, distribution, storage and dosing. • Can carry both hydrophilic drugs and hydrophobic drugs. • Extensively used in various drug delivery systems like drug targeting controlled release and permeation enhancement of drugs
  • 6. DISADVANTAGES • Complex process • During hydration to niosomes, the complete drug entrapment may not be possible, some times Hence the amount of the un entrapped dug should be analyzed
  • 7. Methods of Preparation • Slurry method • Co-acervation phase separation • Slow spray-coating method
  • 8. 8 Slurry Method 10g Maltodextrin As a carrier in 250ml RBF Entire 14.5ml volume Of surfactant solution Formation of Slurry Dry Proniosome powder Stored In sealed container at 4o C
  • 9. 9 Co-acervation Phase Separation Method Drug+surfactant+lipid In 5ml glass vial 0.5ml of Alcohol Warm at 60-70C for 5min Mix all ingredients Until SAA is dissolved Aq.0.1% glycerol soln A clear soln, converted to proniosomal gel On cooling Warm on water bath
  • 10. Slow spray coating method • This method involvs preparation of proniosome by spraying surfactant in organic solvent onto sorbitol powder and then evaporating. • The surfactant coating on the carrier is very thin and hydration of this coating allows multilamellar vesicles as the carrier dissolves. • The resulting niosomes are very similar to the conventional niosomes but are more uniformely distributed
  • 11. Characterization of Proniosomes • Measurement of angle of repose • Scanning electron microscopy (SEM) • Optical microscopy • Measurement of vesicle size • Drug content • Entrapment efficiency • In-vivo release studies • Stability studies
  • 12. ANGLE OF REPOSE The angle of repose of dried proniosomes was measured by funnel method. The funnel, which was fixed at a position and the proniosomal powder was poured into it so that the outlet orifice of the funnel is 10 cm above the level of surface. The powder flowed down from the funnel to form a cone on the surface and then angle of repose was further calculated by measuring the height of the cone and the diameter of its base. SEM Particle size of proniosomes is a factor of prime importance. The surface morphology and size distribution of proniosomes were studied by SEM. A double-sided tape that was affixed on aluminum stubs and the proniosomal powder was spread on it. The aluminum stub was placed in a vacuum chamber of scanning electron microscope (XL 30 ESEM with EDAX, Philips, Netherlands)
  • 13. SEM Image SEM images of pure maltodextrin proniosomes
  • 14. OPTICAL MICROSCOPY • Optical Microscopy designed for viewing samples by transmitted light magnification is carried out by means of two lenses: objective lens which creates an image at infinity weak tube lens which then forms a real image in its focal plane Vesicle size determination by Optical microscopy
  • 15.  ENTRAPMENT EFFICIENCY Separation of unentrapped drug from the niosomal suspension was carried out by exhaustive dialysis method and centrifugation method. Theniosomal suspension was taken into a dialysis tube to which osmotic cellulose membrane was securely attached to one side, the dialysis tube was suspended in 100 ml saline buffer at certain pH, which was stirred on a magnetic stirrer. The niosomal suspension and the unentrapped drug were seperated into the medium through osmotic cellulose membrane. After 6 h of exhaustive dialysis, optical density values were noted and the estimation of the entrapped drug was carried out by UV spectrophotometric method. Entrapment Efficiency was calculated using the formula.
  • 16.  DRUG CONTENT Proniosomes equivalent to 100 mg were taken in a standard volumetric flask. They were lysed with 50 ml methanol by shaking for 15 min. The solution was diluted to 100 ml with methanol. Then 10 mlof this solution was diluted to 100 ml with saline phosphate buffer at certain pH. Aliquots were withdrawn and absorbance was measured at a certain wavelength and drug content was further calculated from the calibration curve.  RELEASE STUDIES The release of the drug from the proniosomal formulations was determined using different techniques such as Franz diffusion cell, Keshary-Chien diffusion cell, Cellophane dialyzing membrane, United states pharmacopeia (USP) dissolution apparatus Type-1, spectrapor molecular porous membrane tubing.
  • 17. STABILITY STUDIES International conference on harmonization (ICH) guidelines suggests stability studies for the dry proniosome powders meant for reconstitution should be studied for accelerated stability at 40°C/75% relative humidity as per international climatic zones and climatic conditions (WHO, 1996). For long term stability studies the temperature is 25°C/60% RH for the countries in zone I and II and for the countries in zone III and IV the temperature is 30°C/65% Relative humidity (RH). Product should be evaluated for appearance, color, assay, pH preservative content, particulate matter, sterility, and pyrogenicity.
  • 19. MARKET FORMULATION • Using their in-depth knowledge of cellular organisation, Lancôme Laboratories have created Multi-Tension Technology, to strengthen the skin's natural protein network, thereby promoting firmness and elasticity for immediate results.
  • 20. CONCLUSION  It is concluded that the concept of incorporating the drug into niosomes for a better targeting of the drug at appropriate tissue destination is widely accepted by researchers and academicians.  Proniosomes based niosomes are thoughts to be better candidates drug delivery as compared to liposomes due to various factors like cost, stability etc.  Various types of drug deliveries can be possible using proniosomes based niosomes like targeting, ophthalmic , topical, transdermal etc. More researches have to be made in this field to come out with all the potential in this novel drug delivery system.
  • 21. REFERENCES • Vyas S.P., Khar R.K., Targeted & Controlled Drug Delivery: Novel Carrier Systems. Pg no. 249-279 • Malhotra M., Jain N.K., Niosomes As Drug Carriers. Pg no. 81-86 • Li Q, Li Z, Zeng W, et al. Proniosome-derived niosomes for tacrolimus topical ocular delivery: in vitro cornea permeation, ocular irritation, and in vivo anti-allograft rejection. Eur J Pharm Sci. 2014;62:115–123. • Alsarra IA, Bosela AA, Ahmed SM, Mahrous GM. (2005). Proniosomes as a drug carrier for transdermal delivery of ketorlac. Eur J Pharm Biopharm, 59, 485–490.