This document discusses topical drug delivery systems and methods for evaluating different topical dosage forms. It begins by defining the two basic types of topical delivery as external and internal. It then lists several advantages of topical drug delivery systems, such as avoiding first-pass metabolism and providing localized treatment. Potential disadvantages include skin irritation and poor drug permeability. The document describes common topical dosage forms like ointments, creams, emulsions, pastes, and gels. It provides details on evaluation methods for things like penetration rate, absorption, irritation effects, rheology, thermal stability, and drug content of different dosage forms. Evaluation methods for specific forms like powders, suspensions, aerosols, and suppositories are
Mucoadhesive drug delivery system interact with the mucus layer covering the mucosal epithelial surface, & mucin molecules & increase the residence time of the dosage form at the site of the absorption.
Mucoadhesive drug delivery system is a part of controlled delivery system.
Since the early 1980,the concept of Mucoadhesion has gained considerable interest in pharmaceutical technology.
combine mucoadhesive with enzyme inhibitory & penetration enhancer properties & improve the patient complaince.
MDDS have been devloped for buccal ,nasal,rectal &vaginal routes for both systemic & local effects.
Hydrophilic high mol. wt. such as peptides that cannot be administered & poor absorption ,then MDDS is best choice.
Mucoadhesiveinner layers called mucosa inner epithelial cell lining is covered with viscoelasticfluid
Composed of water and mucin.
Thickness varies from 40 μm to 300 μm
General composition of mucus
Water…………………………………..95%
Glycoproteinsand lipids……………..0.5-5%
Mineral salts……………………………1%
Free proteins…………………………..0.5-1%
The mechanism responsible in the formation of mucoadhesive bond
Step 1 : Wetting and swelling of the polymer(contact stage)
Step 2 : Interpenetration between the polymer chains and the mucosal membrane
Step 3 : Formation of bonds between the entangled chains (both known as consolidation stage)
Electronic theory
Wetting theory
Adsorption theory
Diffusion theory
Fracture theory
Advantages over other controlled oral controlled release systems by virtue of prolongation of residence of drug in GIT.
Targeting & localization of the dosage form at a specific site
-Painless administration.
-Low enzymatic activity & avoid of first pass metabolism
If MDDS are adhere too tightlgy because it is undesirable to exert too much force to remove the formulation after use,otherwise the mucosa could be injured.
-Some patient suffers unpleasent feeling.
-Unfortunately ,the lack of standardized techniques often leads to unclear results.
-costly drug delivery system
In this slide contains introduction, copmpression, consolidation, compaction, heckel plots and equation, interpretation and application.
Presented by: NARAYAN SINGH UDIT (Department of pharmaceutics).
RIPER, anantapur
Mucoadhesive drug delivery system interact with the mucus layer covering the mucosal epithelial surface, & mucin molecules & increase the residence time of the dosage form at the site of the absorption.
Mucoadhesive drug delivery system is a part of controlled delivery system.
Since the early 1980,the concept of Mucoadhesion has gained considerable interest in pharmaceutical technology.
combine mucoadhesive with enzyme inhibitory & penetration enhancer properties & improve the patient complaince.
MDDS have been devloped for buccal ,nasal,rectal &vaginal routes for both systemic & local effects.
Hydrophilic high mol. wt. such as peptides that cannot be administered & poor absorption ,then MDDS is best choice.
Mucoadhesiveinner layers called mucosa inner epithelial cell lining is covered with viscoelasticfluid
Composed of water and mucin.
Thickness varies from 40 μm to 300 μm
General composition of mucus
Water…………………………………..95%
Glycoproteinsand lipids……………..0.5-5%
Mineral salts……………………………1%
Free proteins…………………………..0.5-1%
The mechanism responsible in the formation of mucoadhesive bond
Step 1 : Wetting and swelling of the polymer(contact stage)
Step 2 : Interpenetration between the polymer chains and the mucosal membrane
Step 3 : Formation of bonds between the entangled chains (both known as consolidation stage)
Electronic theory
Wetting theory
Adsorption theory
Diffusion theory
Fracture theory
Advantages over other controlled oral controlled release systems by virtue of prolongation of residence of drug in GIT.
Targeting & localization of the dosage form at a specific site
-Painless administration.
-Low enzymatic activity & avoid of first pass metabolism
If MDDS are adhere too tightlgy because it is undesirable to exert too much force to remove the formulation after use,otherwise the mucosa could be injured.
-Some patient suffers unpleasent feeling.
-Unfortunately ,the lack of standardized techniques often leads to unclear results.
-costly drug delivery system
In this slide contains introduction, copmpression, consolidation, compaction, heckel plots and equation, interpretation and application.
Presented by: NARAYAN SINGH UDIT (Department of pharmaceutics).
RIPER, anantapur
Phase solubility analysis and pH solubility profileMohit Angolkar
A Brief presentation on the topic- phase solubility analysis and pH solubility profile, which covers the following aspects:
- Solubility introduction
- importance of solubility
- factors influencing solubility
- Phase solubility analysis introduction
- method of analysis
- purification technique
- introduction to pH solubility profile.
Drug excipient incompatibilities are major concerns in formulation development.
Selection of the proper excipient during preformulation studies is of prime importance.
Phase solubility analysis and pH solubility profileMohit Angolkar
A Brief presentation on the topic- phase solubility analysis and pH solubility profile, which covers the following aspects:
- Solubility introduction
- importance of solubility
- factors influencing solubility
- Phase solubility analysis introduction
- method of analysis
- purification technique
- introduction to pH solubility profile.
Drug excipient incompatibilities are major concerns in formulation development.
Selection of the proper excipient during preformulation studies is of prime importance.
Preformulation and physicochemical property of the drugSHIVANEE VYAS
“It is the study of the physical and chemical properties of the
drug prior to compounding process”.
Preformulation commences when a newly synthesized drug shows sufficient pharmacologic promise in animal models towarrant evaluation in man.
These studies should focus on physicochemical properties of new compound that affect drug performance & development of efficaciouss dosage form.
This properties may provide;
A rationale for formulation design
Support the need for molecular modification.
1. Evaluation of
topical dosage
forms
Zohre jelodarian
School of pharmacy , Kermanshah University of Medical Sciences , Krmanshah , Iran
2. Topical delivery includes two
basic types of product:
1. External topicals that are
spread, sprayed, or otherwise
dispersed on to cutaneous
tissues to cover the affected
area.
2. Internal topicals that are
applied to the mucous
membrane orally, vaginally or
on anorectal tissues for local
activity.
3. Advantages of Topical Drug
Delivery Systems
Avoidance of first pass metabolism.
Convenient and easy to apply.
Avoidance of the risks and inconveniences of
intravenous therapy and of the varied conditions of
absorption, like pH changes, presence of enzymes,
gastric emptying time etc.
Achievement of efficacy with lower total daily
dosage of drug by continuous drug input.
Avoids fluctuation in drug levels, inter- and
intrapatient variations.
4. Ability to easily terminate the medications, when
needed.
A relatively large area of application in comparison
with buccal or nasal cavity
Ability to deliver drug more selectively to a specific
site.
Avoidance of gastro-intestinal incompatibility.
Providing utilization of drugs with short biological
half-life, narrow therapeutic window.
Improving physiological and pharmacological
response.
Improve patient compliance.
Provide suitability for self-medication.
5. Disadvantages of Topical Drug Delivery
Systems
• Skin irritation of contact dermatitis may occur
due to the drug and/or excipients.
• Poor permeability of some drugs through the s
kin.
• Possibility of allergenic reactions.
• Can be used only for drugs which require very
small plasma concentration for action
• Enzyme in epidermis may denature the drugs
• Drugs of larger particle size not easy
to absorb through the skin
8. The layers of epidermis
o Stratum Germinativum
(Growing Layer)
o Malpighion Layer (pigment
Layer)
o Stratum Spinosum (Prickly
cell Layer)
o Stratum Granulosum
(Granular Layer)
o Stratum Lucidum
o Stratum Corneum (Horny
Layer)
9. Evaluation Of Topical Dosage Form
21-day cumulative
irritancy patch
test
Draize-shelanski
repeat-insult
patch test
Kligman
Evalution of patch “maximization”
test
10. Evaluation Of Topical Dosage Form
Penetration
Evaluation of
ointments
Rate of release of
medicaments
Absorption of
medicaments into
blood stream
Irritant effect
11. Evaluation Of Topical Dosage Form
Evaluation of
Rheology
cream
Sensitivity
Biological
testing
12. Evaluation Of Topical Dosage Form
Phase separation
Globule size
Evaluation of
emulsions Rheological
properties
Effect of thermal
stresses
13. Evaluation Of Topical Dosage Form
Abrasiveness
Evaluation of paste
Particle size
Cleansing property
Consistency
pH of the product
Foaming character
Limit test for arsenic and lead
Volatile matters and moisture
Effect of special ingredients
14. Evaluation Of Topical Dosage Form
Shade control and lighting
Pressure testing
Evaluation of powder
Breakage test
Flow property
Particle size and abrasiveness
Dispersion of color
15. Evaluation Of Topical Dosage Form
Evaluation Sedimentation
suspension volume
Rheologic
methods
Electrokinetic
techniques
Particle size
changes
16. Evaluation Of Topical Dosage Form
Flame projection
Flash point
Vapor pressure
Density
Moisture
Evaluation of aerosol Aerosol valve discharge rate
Spray patterns
Dosage with metered valves
Net contents
Foam stability
Particle size determination
17. Evaluation Of Topical Dosage Form
Antiseptic
property
Evaluation Determination of
of lotion alcohol content
18. Evaluation Of Topical Dosage Form
Drug content
Evaluation of
gel Homogeneity of drug
content
Measurement of pH
Viscosity
Spreadability
Extrudability