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SKIN
• The skin can be considered to have four distinct layers of tissues
including non-viable epidermis (stratum corneum), viable epidermis,
viable dermis and hypodermis (subcutaneous connective tissue).
• The epidermis is the relatively thin, tough, outer layer of the skin.
• The epidermis has keratinocytes.
• Viable Epidermis layer of the skin resides between the stratum corneum
and the dermis and has a thickness ranging from 50-100 µm. The
structure of the cells in the viable epidermis is physiochemically similar
to other living tissues. Cells are held together by tonofibrils. The water
content is about 90%. The dermis, the skin's next layer, is a thick layer
of fibrous and elastic tissue (made mostly of collagen, elastin and
fibrillin) that gives the skin its flexibility and strength.
• The dermis contains nerve endings, sweat glands and oil glands, hair
follicles, and blood vessels. The subcutaneous tissue also known as
hypodermis is not actually accepted as a true part of the structured
connective tissue.
EMULGELS
• Emulgel are also called as gellified emulsions. Emulsion in gel have
emerged as one of the most interesting topical drug delivery system
as it has dual release system i.e. emulsion and gel.
• Emulgel are emulsion, either oil-in-water or water-in-oil type, which are
gelled by mixing with a gelling agent.
• An emulsion may be defined as a dispersion of two or more mutually
insoluble liquids, one in other.
• The liquid are typically water and oil.
• A gel is apparently solid, jelly like material formed from a colloidal
solution.
• Both oil-in-water and water-in-oil type of emulsion are used as vehicle to
deliver various drugs to the skin. They also have a high ability to penetrate
the skin.
• The presence of gelling agent in water phase converts a classical emulsion
into an emulgel.
• Emulgel for dermatological use have several favorable properties such as
being thixotropic, greaseless, easily spreadable, easily removable,
emollient, non-staining, water soluble, longer shelf life, bio friendly,
transparent and pleasing appearance.
ADVANTAGES DISADVANTAGES
High Stability Drugs with large particle size do not
get absorbed through skin easily.
Gels due to their vast polymeric three
dimensional structure show better
loading capacity.
.Some drugs show poor permeability
through skin.
Easy production Bubble formation may occur during
formulation of emulgel
Low cost formulation
Emulgels act as a dual control
preparation and thus is good for
release of drugs with short half life.
Emulgels improve patient
compliance as they can be self
applied and medication can be
terminated whenever required.
REVIEW OF LITERATURE
• Amin et al., (2021) developed sustained release pellets of lornoxicam
using Eudragit RLPO and Eudragit RSPO to reduce the dosing
frequency.
• Yeteng et al., (2020) prepared Lornoxicam loaded cellulosic
microsponge gel formulation with sustained anti-inflammatory effects
that are required to manage arthritic pain.
• Misal and Chemate, (2019) formulated fast dissolving tablets of
Lornoxicam already used the therapeutic molecule to enhance
effectiveness and to avoid side effects (gastric irritation) of the drug.
• Ansari and Sharma, (2018) prepared mouth dissolving tablets of
Lornoxicam using KYRON T-314 (Polacrillin Potassium) as a novel
superdisintegrant.
• Nagesh et al., (2017) developed bilayer tablet of Lornoxicam using
superdisintegrant Kyron 314 for snappy release layer Polyox 303 for
supporting release layer.
• Yarraguntla et al., (2016) developed and evaluated nanocrystals of
lornoxicam to improve solubility by converting pure drug of
lornoxicam which is in micronized form to nanosized form.
RESEARCH ENVISAGED
• Ivermectin is a mixture of 22, 23-dihydroavermectin B1a and 22, 23-
dihydroavermectin B1b. It is a poorly soluble compound that belongs to
BCS class II drug.
• When gels and emulsions are used in combined form the dosage forms
are referred as Emulgels. Emulgels are also called as creamed gel, quasi
emulsion, gelled emulsion.
• Emulgels for dermatological use have several favorable properties such
as being thixotropic, greaseless, easily spreadable, easily removable,
emollient, nonstaining, long shelf life, bio-friendly, transparent and
pleasing appearance.
• Therefore topical treatment can be beneficial to avoid the systemic side
effects.
• Furthermore, parasites for scabies, onchocerciasis also resides in the
deep skin layer (epidermis and dermis) and subcutaneous tissues.
• The aim of this study was to develop emulgels which can be used as
vehicles for the topical delivery of ivermectin.
PLAN OF WORK
• Literature Review
• Selection of dosage form
• Selection of drug candidate
• Procurement of drug & excipients
• Pre-formulation studies
 Physical appearance
 Solubility study
 Melting Point
 Determination of absorption maxima (max)
 Calibration curve of drug
• Formulation development
 Preparation of emulsion
 Formulation of ivermectin emulgel
• Evaluation of emulgel
 Physical characteristic
 Determination of pH
 Washability
 Extrudability study
 Spreadability
 Viscosity
• In-vitro drug release studies
• Drug Release Kinetics study
DRUG PROFILE
Lornoxicam (chlortenoxicam) is a new nonsteroidal anti-inflammatory drug
(NSAID) of the oxicam class with analgesic, anti-inflammatory and
antipyretic properties. Lornoxicam differs from other oxicam compounds in
its potent inhibition of prostaglandin biosynthesis, a property that explains the
particularly pronounced efficacy of the drug.
Used for the treatment of acute mild to moderate pain, as well as pain and
inflammation of the joints caused by certain types of rheumatic diseases.
Mol. Weight: 371.81
Chemical Formula: C13H10ClN3O4S2
IUPAC Name: 6-chloro-4-hydroxy-2-methyl-1, 1-dioxo-N-pyridin-2-
ylthieno [2, 3-e] thiazine-3-carboxamide
PREFORMULATION STUDIES
A) Organoleptic properties: -
Table : List of Sensory characters
Table : Solubility of Lornoxicam
Color Slightly yellow powder
Odor Odorless
Taste Bitter
S. No. Solvent used Solubility of Lornoxicam
1. Water Soluble
2. 0.1 N HCl Soluble
3. Ethanol Freely soluble
4. Methanol Soluble
5. Chloroform Sparingly soluble
6. Phosphate buffer pH 7.4 Soluble
7. 0.1 N NaoH Sparingly soluble
Table : Melting point of Lornoxicam
S. No. Standard melting point of Lornoxicam Observed melting point of
Lornoxicam
1. 198oC 194-196oC
Table: Determination of moisture content of Lornoxicam
S. No. KF Factor Amount of KF Reagent consumed Moisture content
1 0.580 0.1ml 0.058
Figure: FT-IR spectra of Lornoxicam
Figure: Determination of max of Lornoxicam
Determination of max of Lornoxicam
Table : Calibration curves of Lornoxicam
S. No. Concentration (µg/ml) Mean absorbance
1 0 0
2 5 0.204
3 10 0.421
4 15 0.616
5 20 0.817
6 25 0.997
Figure : Calibration curves of Lornoxicam
PREPARATION AND
CHARACTERIZATION
Formulation Lornoxicam
(mg)
Carbomer
941
Liquid
paraffin
Span
20
Tween
20
Propylene
glycol
water
F1 250 0.5 5 2 5 5 100
F2
250
0.5 5 2 10 5 100
F3
250
1.0 10 4 5 5 100
F4
250
1.0 10 4 10 5 100
F5
250
1.5 5 2 5 5 100
F6
250
1.5 5 2 10 5 100
RESULT AND DISCUSSION
SUMMARY AND CONCLUSION
Different formulation of Lornoxicam emulgel using Carbomer 941, Liquid
paraffin, Span 20, Tween 20 and Propylene glycol. The prepared formulation
were evaluated for Physical characteristic,Determination of pH , Washability,
Extrudability study, Spreadability, Viscosity and In-vitro drug release studies. It
can be concluded from the above results and discussion that Lornoxicam
emulgel formulations prepared with Carbopol 941, Liquid paraffin, Span 20,
Tween 20 and Propylene glycol showed acceptable physical properties, drug
content and drug release. Theoptimized batch of emulgel F-4 Showed, since it
showed the highest drug release in both type of gelling agent.
REFERENCES
• Alexander A, Khichariya A, Gupta S, Patel RJ, Giri TK, Tripathi DK.
Recent expansions in an emergent novel drug delivery technology:
Emulgel. Journal of Controlled Release. 2013 Oct 28;171(2):122-32.
• Bhanu PV, Shanmugam V, Lakshmi PK. Development and optimization of
novel diclofenac emulgel for topical drug delivery. Int J Comp Pharm.
2011;2(9):1-4.
• Shen Y, Ling X, Jiang W, Du S, Lu Y, Tu J. Formulation and evaluation of
Cyclosporin A emulgel for ocular delivery. Drug delivery. 2015 Oct
3;22(7):911-7.
• Wakhet S, Singh VK, Sahoo S, Sagiri SS, Kulanthaivel S, Bhattacharya
MK, Kumar N, Banerjee I, Pal K. Characterization of gelatin–agar based
phase separated hydrogel, emulgel and bigel: A comparative study. Journal
of Materials Science: Materials in Medicine. 2015 Feb;26(2):1-3.
• Ashara KC, Paun JS, Soniwala MM, Chavada JR, Mori NM. Micro-
emulsion based emulgel: a novel topical drug delivery system. Asian
pacific journal of tropical disease. 2014 Jan 1;4:S27-32.
• Koshani R, Tavakolian M, van de Ven TG. Natural emulgel from
dialdehyde cellulose for lipophilic drug delivery. ACS Sustainable
Chemistry & Engineering. 2021 Mar 15;9(12):4487-97.

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Pawan ppt.pptx

  • 2. SKIN • The skin can be considered to have four distinct layers of tissues including non-viable epidermis (stratum corneum), viable epidermis, viable dermis and hypodermis (subcutaneous connective tissue). • The epidermis is the relatively thin, tough, outer layer of the skin. • The epidermis has keratinocytes. • Viable Epidermis layer of the skin resides between the stratum corneum and the dermis and has a thickness ranging from 50-100 µm. The structure of the cells in the viable epidermis is physiochemically similar to other living tissues. Cells are held together by tonofibrils. The water content is about 90%. The dermis, the skin's next layer, is a thick layer of fibrous and elastic tissue (made mostly of collagen, elastin and fibrillin) that gives the skin its flexibility and strength. • The dermis contains nerve endings, sweat glands and oil glands, hair follicles, and blood vessels. The subcutaneous tissue also known as hypodermis is not actually accepted as a true part of the structured connective tissue.
  • 3. EMULGELS • Emulgel are also called as gellified emulsions. Emulsion in gel have emerged as one of the most interesting topical drug delivery system as it has dual release system i.e. emulsion and gel. • Emulgel are emulsion, either oil-in-water or water-in-oil type, which are gelled by mixing with a gelling agent. • An emulsion may be defined as a dispersion of two or more mutually insoluble liquids, one in other. • The liquid are typically water and oil. • A gel is apparently solid, jelly like material formed from a colloidal solution. • Both oil-in-water and water-in-oil type of emulsion are used as vehicle to deliver various drugs to the skin. They also have a high ability to penetrate the skin. • The presence of gelling agent in water phase converts a classical emulsion into an emulgel. • Emulgel for dermatological use have several favorable properties such as being thixotropic, greaseless, easily spreadable, easily removable, emollient, non-staining, water soluble, longer shelf life, bio friendly, transparent and pleasing appearance.
  • 4. ADVANTAGES DISADVANTAGES High Stability Drugs with large particle size do not get absorbed through skin easily. Gels due to their vast polymeric three dimensional structure show better loading capacity. .Some drugs show poor permeability through skin. Easy production Bubble formation may occur during formulation of emulgel Low cost formulation Emulgels act as a dual control preparation and thus is good for release of drugs with short half life. Emulgels improve patient compliance as they can be self applied and medication can be terminated whenever required.
  • 5. REVIEW OF LITERATURE • Amin et al., (2021) developed sustained release pellets of lornoxicam using Eudragit RLPO and Eudragit RSPO to reduce the dosing frequency. • Yeteng et al., (2020) prepared Lornoxicam loaded cellulosic microsponge gel formulation with sustained anti-inflammatory effects that are required to manage arthritic pain. • Misal and Chemate, (2019) formulated fast dissolving tablets of Lornoxicam already used the therapeutic molecule to enhance effectiveness and to avoid side effects (gastric irritation) of the drug. • Ansari and Sharma, (2018) prepared mouth dissolving tablets of Lornoxicam using KYRON T-314 (Polacrillin Potassium) as a novel superdisintegrant. • Nagesh et al., (2017) developed bilayer tablet of Lornoxicam using superdisintegrant Kyron 314 for snappy release layer Polyox 303 for supporting release layer. • Yarraguntla et al., (2016) developed and evaluated nanocrystals of lornoxicam to improve solubility by converting pure drug of lornoxicam which is in micronized form to nanosized form.
  • 6. RESEARCH ENVISAGED • Ivermectin is a mixture of 22, 23-dihydroavermectin B1a and 22, 23- dihydroavermectin B1b. It is a poorly soluble compound that belongs to BCS class II drug. • When gels and emulsions are used in combined form the dosage forms are referred as Emulgels. Emulgels are also called as creamed gel, quasi emulsion, gelled emulsion. • Emulgels for dermatological use have several favorable properties such as being thixotropic, greaseless, easily spreadable, easily removable, emollient, nonstaining, long shelf life, bio-friendly, transparent and pleasing appearance. • Therefore topical treatment can be beneficial to avoid the systemic side effects. • Furthermore, parasites for scabies, onchocerciasis also resides in the deep skin layer (epidermis and dermis) and subcutaneous tissues. • The aim of this study was to develop emulgels which can be used as vehicles for the topical delivery of ivermectin.
  • 7. PLAN OF WORK • Literature Review • Selection of dosage form • Selection of drug candidate • Procurement of drug & excipients • Pre-formulation studies  Physical appearance  Solubility study  Melting Point  Determination of absorption maxima (max)  Calibration curve of drug • Formulation development  Preparation of emulsion  Formulation of ivermectin emulgel
  • 8. • Evaluation of emulgel  Physical characteristic  Determination of pH  Washability  Extrudability study  Spreadability  Viscosity • In-vitro drug release studies • Drug Release Kinetics study
  • 9. DRUG PROFILE Lornoxicam (chlortenoxicam) is a new nonsteroidal anti-inflammatory drug (NSAID) of the oxicam class with analgesic, anti-inflammatory and antipyretic properties. Lornoxicam differs from other oxicam compounds in its potent inhibition of prostaglandin biosynthesis, a property that explains the particularly pronounced efficacy of the drug. Used for the treatment of acute mild to moderate pain, as well as pain and inflammation of the joints caused by certain types of rheumatic diseases. Mol. Weight: 371.81 Chemical Formula: C13H10ClN3O4S2 IUPAC Name: 6-chloro-4-hydroxy-2-methyl-1, 1-dioxo-N-pyridin-2- ylthieno [2, 3-e] thiazine-3-carboxamide
  • 10. PREFORMULATION STUDIES A) Organoleptic properties: - Table : List of Sensory characters Table : Solubility of Lornoxicam Color Slightly yellow powder Odor Odorless Taste Bitter S. No. Solvent used Solubility of Lornoxicam 1. Water Soluble 2. 0.1 N HCl Soluble 3. Ethanol Freely soluble 4. Methanol Soluble 5. Chloroform Sparingly soluble 6. Phosphate buffer pH 7.4 Soluble 7. 0.1 N NaoH Sparingly soluble
  • 11. Table : Melting point of Lornoxicam S. No. Standard melting point of Lornoxicam Observed melting point of Lornoxicam 1. 198oC 194-196oC Table: Determination of moisture content of Lornoxicam S. No. KF Factor Amount of KF Reagent consumed Moisture content 1 0.580 0.1ml 0.058 Figure: FT-IR spectra of Lornoxicam
  • 12. Figure: Determination of max of Lornoxicam Determination of max of Lornoxicam
  • 13. Table : Calibration curves of Lornoxicam S. No. Concentration (µg/ml) Mean absorbance 1 0 0 2 5 0.204 3 10 0.421 4 15 0.616 5 20 0.817 6 25 0.997 Figure : Calibration curves of Lornoxicam
  • 14. PREPARATION AND CHARACTERIZATION Formulation Lornoxicam (mg) Carbomer 941 Liquid paraffin Span 20 Tween 20 Propylene glycol water F1 250 0.5 5 2 5 5 100 F2 250 0.5 5 2 10 5 100 F3 250 1.0 10 4 5 5 100 F4 250 1.0 10 4 10 5 100 F5 250 1.5 5 2 5 5 100 F6 250 1.5 5 2 10 5 100
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  • 22. SUMMARY AND CONCLUSION Different formulation of Lornoxicam emulgel using Carbomer 941, Liquid paraffin, Span 20, Tween 20 and Propylene glycol. The prepared formulation were evaluated for Physical characteristic,Determination of pH , Washability, Extrudability study, Spreadability, Viscosity and In-vitro drug release studies. It can be concluded from the above results and discussion that Lornoxicam emulgel formulations prepared with Carbopol 941, Liquid paraffin, Span 20, Tween 20 and Propylene glycol showed acceptable physical properties, drug content and drug release. Theoptimized batch of emulgel F-4 Showed, since it showed the highest drug release in both type of gelling agent.
  • 23. REFERENCES • Alexander A, Khichariya A, Gupta S, Patel RJ, Giri TK, Tripathi DK. Recent expansions in an emergent novel drug delivery technology: Emulgel. Journal of Controlled Release. 2013 Oct 28;171(2):122-32. • Bhanu PV, Shanmugam V, Lakshmi PK. Development and optimization of novel diclofenac emulgel for topical drug delivery. Int J Comp Pharm. 2011;2(9):1-4. • Shen Y, Ling X, Jiang W, Du S, Lu Y, Tu J. Formulation and evaluation of Cyclosporin A emulgel for ocular delivery. Drug delivery. 2015 Oct 3;22(7):911-7. • Wakhet S, Singh VK, Sahoo S, Sagiri SS, Kulanthaivel S, Bhattacharya MK, Kumar N, Banerjee I, Pal K. Characterization of gelatin–agar based phase separated hydrogel, emulgel and bigel: A comparative study. Journal of Materials Science: Materials in Medicine. 2015 Feb;26(2):1-3. • Ashara KC, Paun JS, Soniwala MM, Chavada JR, Mori NM. Micro- emulsion based emulgel: a novel topical drug delivery system. Asian pacific journal of tropical disease. 2014 Jan 1;4:S27-32. • Koshani R, Tavakolian M, van de Ven TG. Natural emulgel from dialdehyde cellulose for lipophilic drug delivery. ACS Sustainable Chemistry & Engineering. 2021 Mar 15;9(12):4487-97.