Presented By
PatelBindiyaRamesh
M.Pharm – (I semister)
(Pharmaceutics)
Under the guidance of
Dr.K. H.Ramteke
(M.Pharm, Ph....
Aim & objective
What is nano sponge ?
Introduction
Advantages
Disadvantages
Factors influencing the formation of nanospong...
AIM : To review and study nanosponge as a novel
& targeted drug delivery system.
To discuss nanosponges with their...
Ad...
Nanosponges are tiny sponges with a size of about a virus
(250nm – 1μm), which consist of cavities that can be filled with...
Targeting the drug delivery has long been a problem for medical
researchers how to get them to the right place in the body...
A wide variety of drugs can be loaded into nanosponge for targeting drug
delivery.
These particles are capable of carrying...
The nanoscale materials are small enough to be effective in attaching to or passing
through cell membranes.
The polyester ...
The nanosponges are solid in nature and can be formulated as oral,
parenteral, topical or inhalational dosage forms.
For o...
Targeted site specific drug delivery.
Can be used to mask unpleasant flavours, odour and to convert liquid
substances to s...
Biodegradable.
Nanosponge formulations are stable over range of ph 1 to 11.
Nanosponge formulations are stable at the temp...
The main disadvantage of these nanosponges is their ability to include
only small molecules.
Dose dumping may take place.
...
Type of polymer : Type of polymer used can influence the formation as well
as the performance of Nanosponges. For complexa...
Temperature : Increasing in the temperature decreases the stability of
the drug/nanosponge complex, may be due to a result...
1
• Polymer is mixed with a suitable solvent like polar aprotic solvent.
2
• This mixture is added to excess quantity of t...
Nanosponges are obtained by reacting cyclodextrin with a cross-
linker such as di isocianates, diaryl carbonates, dimethyl...
• In this method, nanosponges can be obtained by reacting polymers
with cross-linkers in the absence of solvent and under ...
Organic internal phase containing
drug & polymer in solvent is added to
External phase containing emulsifying
agent
Than m...
Suspend the
nanosponges in water
and sonicate to avoid
the presence of
aggregates
then centrifuge the
suspension to
obtain...
Author Aim Method used Result
CH.N.V.
Raja*, G.
Kiran
kumar,
Kotapati
anusha
Fabrication And
Evaluation Of
Ciprofloxacin L...
20
Author Aim Method used Result
E. K. PATEL*
and RJ.
OSWAL
Nanosponge for
delivery of calcium
in
hyperphosphatemia
Hyper ...
Particle Size Determination : Particle size can be determined by laser
light diffractometry or Zeta seizer.
Loading Effici...
UV spectroscopy is used to carry out the saturated solution interaction
study.
Increasing concentrations of nanosponge sol...
Bulk volume – True volume
% Porosity (E) = ------------------------------------------ x 100
Bulk volume
Zeta potential :
Z...
 Diffraction peaks for a mixture of compounds are useful in
determining chemical decomposition and complex formation.
 C...
25
Marking of the cylinder at a specified
time point
Percentage of swelling = --------------------------------------------...
• In vitro release kinetics experiments are performed using a multi-
compartment rotating cell; an aqueous dispersion of n...
Spontaneous.
Carcinogen-induced.
Gems (genetically engineered mouse models).
–transgenic
–knockout
–regulatable transgenic...
Spontaneous model
Some strains of laboratory animals are susceptible to spontaneously
developing certain types of tumor.
A...
Marketed preparation
Paclitaxel, camptothecin, tamoxifen, econazole nitrate, peroxidase
29
Drug Administration
route
Trade...
Cancer.
Oxygen delivery systems.
As a carrier for biocatalysts and in the delivery
and release of enzymes, proteins, vacci...
The nanosponges have the ability to include either lipophilic or hydrophilic
drugs and release them in a controlled and pr...
REFERENCES
G. Yadav., H. Panchory., Nanosponge: A Boon To The Targeted Drug Delivery
System, Journal Of Drug Delivery And ...
33
of 33

Nanosponge: Versatile Drug Delivery System

Nanosponges are tiny sponges with a size of about a virus (250nm – 1μm), which consist of cavities that can be filled with a wide variety of drugs.
Published on: Mar 3, 2016
Published in: Health & Medicine      
Source: www.slideshare.net


Transcripts - Nanosponge: Versatile Drug Delivery System

  • 1. Presented By PatelBindiyaRamesh M.Pharm – (I semister) (Pharmaceutics) Under the guidance of Dr.K. H.Ramteke (M.Pharm, Ph.D.) Dept. of Pharmaceutics PE Society’s Modern college of pharmacy (for ladies), Moshi, Pune. NANOSPONGE A BOON TO THE TARGETED DRUG DELIVERY SYSTEM 1
  • 2. Aim & objective What is nano sponge ? Introduction Advantages Disadvantages Factors influencing the formation of nanosponges Method of preparation Evaluation of nanosponges Literature survey Application Conclusion Referencea Contents... 2
  • 3. AIM : To review and study nanosponge as a novel & targeted drug delivery system. To discuss nanosponges with their... Advantages & disadvantages, Factors influencing there formation,  Method of preparation, Characterization, and Applications. OBJECTIVE 3
  • 4. Nanosponges are tiny sponges with a size of about a virus (250nm – 1μm), which consist of cavities that can be filled with a wide variety of drugs. The sponge acts as a three-dimensional network or scaffold, which consist of the backbone known as long-length polyester. It is mixed in solution with cross-linkers to form the polymer. What Is Nano Sponge ??? 4
  • 5. Targeting the drug delivery has long been a problem for medical researchers how to get them to the right place in the body and how to control the release of the drug to prevent overdose. The development of new and complex molecules called Nanosponges has the potential to solve these problems. Nanosponge is a novel and emerging technology which play a vital role in targeting drug delivery in a controlled manner. Nanosponges are a new class of materials and made of microscopic particles with few nanometres wide cavities in which a large variety of substances can be encapsulated. Introduction 5
  • 6. A wide variety of drugs can be loaded into nanosponge for targeting drug delivery. These particles are capable of carrying both lipophilic and hydrophilic substances and of improving the solubility of poorly water soluble molecule. Nanosponges are tiny mesh like structures is about the size of a virus with a backbone of naturally degradable polyester. They cross link segments of the polyester to form a spherical shape that has many pockets / cavities where drug can be stored. Cont… 6
  • 7. The nanoscale materials are small enough to be effective in attaching to or passing through cell membranes. The polyester is biodegradable, so it breaks down gradually in the body & releases its drug payload in a predictable fashion. These tiny sponges can circulate around the body until they encounter the specific target site and stick on the surface and begin to release the drug . As compared to other nanoparticles, nanosponges are porous, non toxic and stable at high temperatures up to 300oC. Cont … 7
  • 8. The nanosponges are solid in nature and can be formulated as oral, parenteral, topical or inhalational dosage forms. For oral administration, these may be dispersed in a matrix of excipients, diluents, lubricants which is suitable for the preparation of tablets or capsules. For parenteral administration, these can be simply mixed with sterile water, saline or other aqueous solutions. For topical administration, they can be effectively incorporated into topical hydro gel. Cont… 8
  • 9. Targeted site specific drug delivery. Can be used to mask unpleasant flavours, odour and to convert liquid substances to solids. Less harmful side effects (since smaller quantities of the drug have contact with healthy tissue). Nanosponge particles are soluble in water, so the hydrophobic drugs can be encapsulated within the nanosponge, after mixing with a chemical called an adjuvant reagent. Particles can be made smaller or larger by varying the proportion of cross-linker to polymer. 9
  • 10. Biodegradable. Nanosponge formulations are stable over range of ph 1 to 11. Nanosponge formulations are stable at the temperature up to 130˚c These formulations are compatible with most vehicles and ingredients. These are self sterilizing as their average pore size is 0.25μm where bacteria cannot penetrate. These formulations are free flowing and can be cost effective Improved stability, increased elegance and enhanced formulation flexibility. 10
  • 11. The main disadvantage of these nanosponges is their ability to include only small molecules. Dose dumping may take place. May retard the release. Materials Used For Preparation Of Nanosponges DISADVANTAGE Polymers : Hyper cross linked polystyrenes, ethyl cellulose, 2- hydroxy proply β – cyclodextrins, poly valerolactone, Eudragit RS 100, acrylic polymers Cross linkers : Dichloromethane, diphenyl carbonate, acrylamido, glutarldehyde, Carboxylic acid dianhydride , 11
  • 12. Type of polymer : Type of polymer used can influence the formation as well as the performance of Nanosponges. For complexation, the cavity size of nanosponge should be suitable to accommodate a drug molecule of particular size. Type of drugs : Molecules to be complexed with nanosponges should have certain characteristics mentioned below 1. Molecular weight between 100 – 400 Da . 2. Drug molecule consists of less than five condensed rings . 3. Solubility in water is less than 10mg/mL . 4. Melting point of the substance is below 250°C. Factors influencing the formation of nanosponges 12
  • 13. Temperature : Increasing in the temperature decreases the stability of the drug/nanosponge complex, may be due to a result of possible reduction of drug/nanosponge interaction forces. Method of preparation : The method of loading the drug into the nanosponge can affect Drug/Nanosponge complexation. Degree of substitution : The complexation ability of the nanosponge may be greatly affected by type, number and position of the substituent on the parent molecule. 13
  • 14. 1 • Polymer is mixed with a suitable solvent like polar aprotic solvent. 2 • This mixture is added to excess quantity of the cross-linker preferably in cross-linker/polymer molar ratio of 1:4. 3 • Action is carried out at temperature ranging from 10°C to the reflux temperature of the solvent, for time ranging from 1 to 48 hr 4 • After completion of the reaction, the solution is cooled at room temperature and the product is added to large excess of distilled water. 5 • The recovery of the product is done by filtration under vacuum. METHOD OF PREPARATION 1. Solvent method 14
  • 15. Nanosponges are obtained by reacting cyclodextrin with a cross- linker such as di isocianates, diaryl carbonates, dimethyl carbonate, diphenyl carbonate, and carbonyl diimidazoles. The average diameter of a Nanosponge is below 1 µm but fractions below 500 nm can be selected. 2. Hyper Cross- Linked β- Cyclodextrins CYCLO DEXTRI N CROSS- LINKER IN SOLVENT NANOSPONGE 15
  • 16. • In this method, nanosponges can be obtained by reacting polymers with cross-linkers in the absence of solvent and under sonication. • The nanosponges obtained by this method will be spherical and uniform in size. 4. Ultrasound-Assisted synthesis 16
  • 17. Organic internal phase containing drug & polymer in solvent is added to External phase containing emulsifying agent Than mixture is stirred at 1000-2000 rpm for 3 hrs at RT Formed nanosponge were filtered, washed & dried at RT 3. Emulsion Solvent Diffusion Method 17
  • 18. Suspend the nanosponges in water and sonicate to avoid the presence of aggregates then centrifuge the suspension to obtain the colloidal fraction Separate the supernatant and dry the nanosponge by freeze drying Prepare aqueous suspension of Nanosponge and disperse the excess amount of the drug and maintain the suspension under constant stirring at specific time for complexation solvent evaporation or by freeze drying Nanosponges Loading Of Drug Into Nanosponges After complexation, separate the uncomplexed (undissolved) drug by centrifugation Then obtain the solid crystals of nanosponges by 18
  • 19. Author Aim Method used Result CH.N.V. Raja*, G. Kiran kumar, Kotapati anusha Fabrication And Evaluation Of Ciprofloxacin Loaded Nanosponges For Sustained Release Solvent method Formulated NS loaded with Ciprofloxacin antibiotic resulted in sustained release. Among all batches (F5) is considered as the best entrapped (90.80%) NS with greater % drug release (99.4%). Roberta Cavalli, Ansari Khalid Akhter, Agnese Bisazza Nano sponge formulation as oxygen delivery system Hyper Cross- Linked β- Cyclodextrins NS were able to encapsulate, store & release oxygen for prolonged time. US enhanced release & permeation of oxygen. NS is suitable carrier & act as oxygen reservior. Literature surveys 19
  • 20. 20 Author Aim Method used Result E. K. PATEL* and RJ. OSWAL Nanosponge for delivery of calcium in hyperphosphatemia Hyper Cross- Linked β- Cyclodextrins SEM – roughly spherical shape, porous in nature & mean particle size - 400nm. zeta potential is high enough. encapsulation efficiencies – 81 – 95 % Renuka Sharma , Roderick B. Walker and Kamla Pathak * Evaluation of the Kinetics and Mechanism of Drug Release from Econazole nitrate Nanosponge Loaded Carbapol Hydrogel Emulsion solvent method A sustain release topical DDS of econazole nitrate developed as o NS hydro gel offered solubilising matrix for poorly soluble drug. Served as a local depot for sustain drug release.
  • 21. Particle Size Determination : Particle size can be determined by laser light diffractometry or Zeta seizer. Loading Efficiency : The loading efficiency (%) of Nanosponge can be determined by, Actual drug content Loading Efficiency = ---------------------------------- X 100 Theoretical drug content EVALUATION OF NANOSPONGES 21
  • 22. UV spectroscopy is used to carry out the saturated solution interaction study. Increasing concentrations of nanosponge solutions (1– 80 ppm) are added to fixed concentrations of the drug. The samples are kept overnight for interaction and finally filtered solutions are scanned for λmax and absorbance is measured. Drug loading is interpreted by taking scans of the formulation in the UV range and analyzing the shift of the absorbance maxima in the spectra compared to pure drug. • Saturation state interaction 22
  • 23. Bulk volume – True volume % Porosity (E) = ------------------------------------------ x 100 Bulk volume Zeta potential : Zeta potential of any system under investigation is a measure of the surface charge. SEM and TEM : These tools are employed to evaluate the particle shape and size and to get morphological information related to the drug delivery system Fourier transform-infrared spectroscopy (FTIR) : It serves as a major tool to determine the presence of functional groups. Porosity : Percent porosity is given by equation 23
  • 24.  Diffraction peaks for a mixture of compounds are useful in determining chemical decomposition and complex formation.  Complex formation of the drug with nanosponges alters the diffraction patterns and also changes the crystalline nature of the drug. Thermo gravimetric analysis (TGA)  These studies are carried out to understand the melting point, thermo stability and crystalline behaviour of the particle. Powder X-ray diffraction (P-XRD) 24
  • 25. 25 Marking of the cylinder at a specified time point Percentage of swelling = -----------------------------------------------------x 100 Initial marking before soaking Mass of the hydro gel after 72 hrs Percentage of water uptake = -----------------------------------------------x 100 Initial Mass of dry polymer Swelling and water uptake
  • 26. • In vitro release kinetics experiments are performed using a multi- compartment rotating cell; an aqueous dispersion of nanosponges (1 mL) containing the drug is placed in the donor compartment, while the receptor compartment, separated by a hydrophilic dialysis membrane, is filled with phosphate buffer at pH 7.4 or pH 1.2. • Each experiment is carried out for 24 h. • At fixed times, the receptor buffer is completely withdrawn and replaced with fresh buffer. The amount of drug in the medium is determined by a suitable analytical method and drug release is calculated to determine the release pattern. Drug release kinetics In vitro diffusion model 26
  • 27. Spontaneous. Carcinogen-induced. Gems (genetically engineered mouse models). –transgenic –knockout –regulatable transgenic CELL LINES HT-29 cell line MCF-7 cell line In vivo models 27
  • 28. Spontaneous model Some strains of laboratory animals are susceptible to spontaneously developing certain types of tumor. Advantages  may mimic some types of human diseases  can use to study early disease.  can use for prevention.  includes elements of progression Disadvantages  Variability of disease progression.  Large animal numbers needed.  Long time to develop disease.  penetrance (not all animals get disease). 28
  • 29. Marketed preparation Paclitaxel, camptothecin, tamoxifen, econazole nitrate, peroxidase 29 Drug Administration route Trade name Market Dexamethasone Dermal Glymesason Japan Iodine Topical Mena-gargle Japan Alprostadil I.V Prostavastin Europe, Japan, USA Piroxicam Oral Brexin Europe Temoxifen Oral - - Other examples patented drugs used in nanosponge preparation
  • 30. Cancer. Oxygen delivery systems. As a carrier for biocatalysts and in the delivery and release of enzymes, proteins, vaccines and antibodies. Harvesting of rare Cancer Marker from Blood. Solubility enhancement. Topical drug delivery system. Antiviral application. More effectiveness than direct injection. APPLICATION 30
  • 31. The nanosponges have the ability to include either lipophilic or hydrophilic drugs and release them in a controlled and predictable manner at the target site. By controlling the ratio of polymer to the cross-linker the particle size and release rate can be modulated. Nanosponges enable the insoluble drugs and protect the active moieties from physicochemical degradation and controlled release. Because of their small size and spherical shape nanosponges can be developed as different dosage forms like parenteral, aerosol, topical, tablets and capsules. Thus, the nanosponge drug delivery system is a boon in the area of targeted and site specific drug delivery system. CONCLUSION 31
  • 32. REFERENCES G. Yadav., H. Panchory., Nanosponge: A Boon To The Targeted Drug Delivery System, Journal Of Drug Delivery And Therapeutics; 2013, Volume 3(4), Pg. No. 151-155. F. Trotta., R. Cavalli., Characterization And Applications Of New Hyper Cross - Linked Cyclodextrin, Composite Interfaces, 2009, Volume 16, Pg. No. 39-48. G. Jilsha., Vidya Viswanad., Nanosponges: A Novel Approach Of Drug Delivery System; Int. J. Pharm. Sci. Rev. 2013 Res Volume 19 (2), Pg. No.119-123. C. U. Shah, Cyclodextrin Based Nanosponges For Pharmaceutical Use: A Review; Acta Pharm. 2013, Volume 63, Pg. No. 335-358. S.P. Vyas, R.K. Khar. Targeted And Controlled Drug Delivery- Novel Carrier Systems. Molecular Basis Of Targeted Drug Delivery. Cbs Publishers And Distributors. New Delhi. 2008: Pg. No. 38- 40. S. Subramanian, A. Singireddy., Nanosponges: A Novel Class Of Drug Delivery System; J Pharm Pharmaceut Sci: 2012, Volume 15(1), Pg. No. 103-111. 32
  • 33. 33

Related Documents