Semi Solid Dosage Forms

Vandana B. Patravale
Professor of Pharmaceutics
Department of Pharmaceutical Sciences and Technology
Institute of Chemical Technology, Matunga
Mumbai-400019

Email: vb.patravale@ictmumbai.edu.in, vbp_muict@yahoo.co.in

Website: www.vbpgroup-ict.in
Differentiate between terms-

Topicals

Dermatologicals

Transdermals
 The Global Topical Drug Delivery Market
Market Investments
250 11.5
11.21
205.1
200 11

f 9.2% .5%
G R o 10.5
o f3
150
C A R
G
Billion $

Billion $
101.7
10 CA
100
9.44
9.5

50
9

0 8.5
2016 2024 2013 2018

Fastest growing market sector: Skin infections, Hospital care

http://www.micromarketmonitor.com/market-report/topical-drug-delivery-reports-4242454697.html
http://databridgemarketresearch.com/reports/global-topical-drug-delivery-market-trends-forecast-2024/
Sectional View: Skin
 Sectional View: Skin
Component Key features Major function and barrier
mechanisms
Keratinocytes Keratin synthesis Thermoregulation, protection
(90% of against chemicals and microbes,
epidermal cytokines production in response to
cells) Lamellar granules releasing injury
hydrophobic sealant Water repellent barrier
Intercellular desmosomal Topical Application
connection Restricts entry of foreign molecules,
reflection of UV radiation
Epidermal infections
Viable Synthesis of defensins and Antimicrobial function against gram- and conditions
epidermal cells cathelicidins - positive and gram-negative Sunscreens
pheromones / chemo organisms Moisturisers
attractants for APC cells fungi and viruses Cleansing creams
Cold creams
Melanocytes Melanin synthesis and melanin Skin colouration, protection against T
(8% of granule transport to nuclear DNA damage by UV
epidermal keratinocytes radiation,protection towards
cells) Lagerhans cells
Lagerhans cells Immune response Protection against microbes

Merkel cells Formation of tactile disc in Sensation and underlined protection

connection with sensory
neurons
 Sectional View: Skin

Component Key features Major function and barrier

mechanisms
Papillary region Tactile receptors, Sensation and underlined protection,
areolar connective tissue elasticity

Reticular region Connective tissue, Elasticity, stretch, immune response,

fibroblast, collagen, elastic nutrient supply
fibres, T cells, vascular and
lymphatic network

Dermal Application

Vaccines
Anaesthetics
 Sectional View: Skin

Component Key features Major function and barrier

mechanisms
Subcutaneous Areolar and adipose Skin anchoring, thermoregulation
region tissue, vascular network
Sustained Delivery approach

Depot
Oily injections
Sectional View: Skin

Transdermal Application

Semisolids
Transdermal Patches
Desired systemic uptake

Component Key features Major function and barrier

mechanisms
Hair Keratinized hair shaft Protection, release of sweat
and sebum

Sebaceous Sebum secretion Protection against chemicals

glands and microbes
Sudoriferous Sweat secretion Thermoregulation, skin pH
glands regulation, microbial resistance

Nails Dead keratinized cell Protection against trauma

plate
 Skin: An Innate Barrier

What are the possible drug permeation pathways?

 Drug in Topical Dosage Form

Diffusion of drug to skin surface

Transepidermal pathway Transfollicular pathway

Partitioning in stratum corneum Partitioning into sebum

Diffusion through lipoprotein matrix Diffusion through sebaceous pore

in stratum corneum

Partitioning and diffusion via viable epidermis

Partitioning and diffusion via upper dermal region

Capillary uptake and systemic dilution

 Skin: An Innate Barrier

What are the possible drug delivery pathways?

 Ultrasound/
Microprocessor Pulse electrode/magnet

+ -
D+ D+ X- D D
Transappendageal

Transcellular

Intercellular

Passive drug delivery

Ointments
Solutions Gels Sponge
Emulsions Aerosol Swab
Creams Powders
Suspensions Spray Tape
Lotions
Pastes Patch

Formulation controlled delivery

 Ultrasound/
Microprocessor Pulse electrode/magnet

+ -
D+ D+ X- D D

Passive drug delivery

Ointments
Solutions Gels Sponge
Emulsions Aerosol Swab
Creams Powders
Suspensions Spray Tape
Lotions
Pastes Patch

Formulation controlled delivery

 Ultrasound/
Microprocessor Pulse electrode/magnet

+ -
D+ D+ X- D D

Active drug delivery

Injections

Device controlled delivery

Reversible, minute, short period skin damage
 Ultrasound/
Pulse electrode/magnet
Intravenous
Microprocessor
Subcutaneous
Intramuscular
+ -
D Intradermal
D
D+ D+ X-
Epidermis

Dermis

Subcutaneous
Tissue

Subcutaneous
adipose
tissue

Muscles and veins

 Ultrasound/
Microprocessor Pulse electrode/magnet

+ -
D+ D+ X- D D

Active drug delivery

Microneedles

Device controlled delivery

Reversible, minute, short period skin damage
 Ultrasound/
Microprocessor Pulse electrode/magnet

+ -
D+ D+ X- D D

Active drug delivery

Needle free
Injections

Device controlled delivery

Reversible, minute, short period skin damage
 Ultrasound/
Microprocessor Pulse electrode/magnet

+ -
D+D+ D+D+ X- D D

X- X-

Active drug delivery

Iontophoresis

Device controlled delivery

Reversible, minute, short period skin damage
 Ultrasound/
Microprocessor
Pulse electrode/magnet/laser

+ -
D+ D+ X- DD DD

Active drug delivery

Electroporation
Sonophoresis
Thermal methods
Magnetism
Laser ablation
Device controlled delivery
Reversible, minute, short period skin damage
 Delivery of API into the skin
at the target site

Physical and chemical

Cosmetically elegant
stability

Excipients: Dosage Form:

Regulatory and disease Patient and disease
condition compliant Successful condition compliant
Topical
Dermatological
Formulation
Factors Affecting Skin Permeation

Vehicle Related

Skin Related

Drug Related
 Drug Related Factors

• Solubility
• Log P
• Molecular Weight and Size
• Melting Point
• Crystal Form
• pH and Ionization
 Skin Related Factors

• Age
• Thickness
• Gender
• Site of application
• Skin hydration
• Skin condition
• Skin pathological state
• Skin pH
• Skin microcirculation
• Biotransformation in skin
• Skin temperature
 Vehicle Related Factors

• Concentration of drug
• pH of vehicle
• Type of vehicle
• Structure of vehicle
• Permeation enhancer
• Thermodynamic activity
 ADVANTAGES OF TOPICAL DELIVERY
Ø Avoidance of First pass metabolism
Ø Convenient to use and easy to apply
Ø Easily to terminate the medication
Ø Drug delivered selectively to a specific site
Ø The gastro-intestinal incompatibility will be avoided
Ø Provides drugs utilization with short biological half-life and
narrow therapeutic window
Ø Better patient compliance
Ø Provides effectiveness in low doses and by continuous drug
input
Ø Large area of application available compared to other routes
 DISADVANTAGES

ØPossibility of local skin irritation at the site of

application
ØContact dermatitis due to some drug/excipients may
occur
ØSome drugs with poor permeability are difficult to
penetrate via the skin
ØDrugs with larger sizes are difficult to penetrate
ØDrugs with high dose are poor candidates