Newer drug delivery systems aim to maintain constant drug levels in the blood for longer periods of time using various prolonged release preparations and targeted delivery methods. Prolonged release parenteral preparations include portable insulin pumps, implantable intrathecal pumps for chronic pain, and transdermal drug delivery patches. Nanoparticles, liposomes, monoclonal antibodies, and other advanced targeted delivery systems can selectively deliver drugs to specific tissues and organs to improve efficacy and reduce side effects.

1. NEWER DRUG DELIVERY
SYSTEMS
Dr.Reshmi.T.R,

2. Definition
Therapeutic systems that incorporate drugs in
a dosage form that releases the medication
• at a predetermined rate
• over an extended period of time
• from a single application

3. Demerits of conventional
dosage forms
Large amount of drug delivered
Repeated dosage necessary
Less patient compliance
Fluctuation in drug concentration in blood

4. Aims of NDDS
• Maintain constant blood levels for longer
period of time
• Decrease frequency of administration
• Improves patient compliance
• Reduce the GI S/E

5. Types of NDDS
•Prolonged release parenteral preparations
•Local Drug delivery systems
•Targeted delivery systems
•Some more NDDS

6. PROLONGED RELEASE
PARENTERAL PREPARATIONS
1.Portable pumps
2.Implantable pumps
3.Pens
4.Pellets
5.Dermojet
6..Trandermal delivery system
7.Patient Controlled Analgesia(PCA)

7. Portable pumps
Insulin Pump
Releases small amount of insulin all day
Steady glucose
Batterypowered device

8. Parts of the pump
Parts:
Pump
Insulin Reservoir
Computer chip
Infusion set

9. Insulin flows from pump
Infusion set canula
INSULIN PUMP

10. Recent Developments
• Pump software
• Alarms
• Interface to computer
• Bluetooth remote
• Touch bolus

11. Implantable pumps
Intrathecal pump
Deliver drug intrathecal space

12. Parts:
Metal pump with reservoir to store drug and
catheter to deliver drug

13. • Surgical procedure
• Catheterspine
PumpSubcutaneou
s
Drug delivered through
catheter to intrathecal
space

14. Catheter in intrathecal space

15. • Indications:
• Chronic pain
• Cancer
• Multiple sclerosis
• Chronic pancreatitis
• Drugs:
• Morphine
• Baclofen

16. Pens
Insulin pens –
Parts: Cartridge , dial, pen needle
Injected S/C with needle

17. Pellets
Eg: NORPLANT
Contraceptive
6 silicon capsules of 36mg levonorgestrel

18. Surgical procedure~15mnts
IncisionInsert capsules
subdermally in fanlike shape
Action in 24 hrs
Removal: 2nd
incision

19. Dermojet
• Needle not used
• High velocity jet of
drug from microfine
orifice
• s/c tissue
• Mass inoculation

20. Treatment of keloids and hypertrophic scars
with Intralesional dermojet injections of
Bleomycin
Dermojet treatment using Triamcinolone for
alopecia areata

21. Transdermal drug delivery
system
• Adhesive patches
• drugs delivered at constant rate into systemic
circulation

22. • Layers:
• Drug in reservoir
• Occlusive backing film
• Rate controlling micropore
• Adhesive with priming dose
• Protective peel off strip

24. Advantages
Steady plasma conc
Bypass First pass metabolism
Effect lasts for 1-7 days
Convenient
Less side effects

25. Disadvantages
• Local irritation
Erythema
• Minimised by changing the site of
application

26. DRUGS:
• Hyoscine - 1st
used
In motion sickness
• GTN , fentanyl , nicotine , clonidine , estradiol

27. Sites
Chest , abdomen ,upper arm ,lower back,
buttock, mastoid region

28. Patient Controlled Analgesia
• To administer pain medications
• Patient control dose and amount
• Drugs:
• Morphine
• Bupivacaine
• Indications:Post op pain, cancer pain

29. Patient Controlled Analgesia

30. ]
Patient Controlled Epidural Analgesia
PCEA

31. Local Drug delivery systems

32. 1.Ocular drug Delivery systems:
Deliver steady concentration
In ocular tissues
Ocusert
Lacrisert
SODI

33. Ocusert
• Consists of:
• Central reservoir of Drug enclosed in
microporous membrane

34. • Ocusert Pilocarpine:
• First in the category
• 2 types:
• Pilo 20 and Pilo 40
• Pilocarpine alginate core
sandwiched in Ethylene vinyl
Acetate membranes

35. Placed under eyelid
Pilocarpine dissolve In lacrimal fluid
Released through rate controlling membrane
Lasts 7 days

36. • Side effects
• Miosis
• Myopia
• Drawback:
• Non biodegradable
• Require removal

37. • Lacrisert
• Erodible insert
• Used in dry eye
syndrome
Rod shaped
Made of hydroxy propyl cellulose
Inserted into inferior fornix

38. • Inserted into inferior fornix
• Imbibes water from conjunctiva
Form a hydrophilic film which stabilise tear film
Hydrates cornea

39. Insertion of Lacrisert

40. SODI
• Soluble Ocular Dug Insert
• First developed for cosmonauts
• Small oval thin film
• Made of Acrylamide Vinyl Pyrolidene Ethylacrylate
• Available for around 20 ophthalmology drugs
• Ex:Ciprofloxacin

41. Progetasert
• T shaped IUCD
• progesterone at constant rate
65microgram/day * 1 yr

42. Drug Eluting Stents
Metallic stents covered with drug
Drug gradually released
Prevent restenosis in MI
Eg: Sirolimus,Paclitaxel

43. Targeted Drug Delivery
Systems
Selective delivery of drugs to specific regions
Improve safety & efficacy
Reduce s/e

44. Types

45. Vesicular Drug Delivery
systems
Highly ordered assemblies of lipid bilayer
Can incorporate both hydrophilic and
lipophilic drugs
• Eg:
• Liposomes
• Niosomes

46. LIPOSOMES
• Concentric shells of Phospholipids in
watery medium
• Vehicle for targeted delivery

47. Spherical vesicles – 2layers Pospholipid
Cholesterol
Size – nm to several mms
Water soluble drugs- trapped in central
aqueous
compartment.
Lipid soluble drugs- in lipid bilayer

48. • Examples:
• Anticancer drugs
Doxorubicin
• Antifungal drugs
Amphotericin B

49. Multilamellar
Vesicles
(MLV)
Several lipid
bilayers
Single
Unilamellar
Vesilces
(SUV)
Single lipid
layer:25nm
Large Unilamellar
vesicles
(LUV)
Single lipid
layer:100nm
CLASSIFICATION OF LIPOSOMES

50. Mechanism
• Lipid bilayer fuse with cell membrane
• Release contents cytoplasm

51. Types of Liposomes

53. Niosomes
• Bilayer of non ionic surface active agents

54. Liposome
• More expensive
• Less stable
• From phospholipids
• Relatively more toxic
Niosome
• Cheaper
• More stable
• from uncharged
surfactant
• Relatively safer

55. Other vesicular drug delivery
systems
Genosomes For cell specific gene
transfer
Hemosomes Hb containing liposomes to
carry O2
Photosomes Photolyase incorporated
liposomes for
photodynamic therapy
Ethosomes With polar core for water
soluble drugs

56. MONOCLONAL ANTIBODIES
• Antibodies produced by a single clone
directed against single antigenic
determinent
• Hybridoma technologylarge scale
production of Mab

57. • Hybridoma:by fusing B lymphocytes with myeloma cells
• Myeloma cell grown in culture deficient in HGPRTenzyme
• Prevent formation of Ig
• Myeloma cell +B lymphocytesHybridoma
Placed in HAT(Hypoxanthine Aminopterine Thymidine )medium and cloned
Hybridomas survive and replicate
Monoclonal antibodies formed are purified for clinical use

60. Name of Monoclonal antibody ends with mab
Letter before mabsource

61. • Letter before the previous
wordsTherapeutic use
• Tutumor
• Vivirus
• Cicirculation
Tu Tumour
Vi Virus
Ci Circulation

62. Examples
Rituximab Chimeric
Treat tumour-Hodgkins
lymphoma
Palivizumab Humanised
RSV(virus)

63. NANOMEDICINE
• Nanoparticles used as drug delivery
vehicles
• Size< 100 nm
• Taken up by cells more efficiently

64. • A nano meter =one billionth of a meter =
250 millionths of an inch.
Different from properties of the bulk material.

65. Why Nanoparticles?
• Can easily reach tiny capillaries and
secluded areas of body
• High surface to volume ratiodissolution
rate high
• Eg: Nanosuspensions of Paclitaxel and
Cyclosporine has better dissolution rate

66. • Targeted delivery-depend on particle
size,charge preferentially absorb on
certain organs and tissues

67. Passive targeting
Spontaneous accumulationin leaky vasculature
Physiology of diseased tissuepH,temperature
Eg: Cancer cells—Pores,bloated gap
junctionsEnhanced permeability and Retention
effect(EPRE)Nanoparticles gather in tumor interstitium

68. Active targeting
• Moieties like Antibodies/lipids coupled to
drug or delivery systems
• Straps nanodevices to receptor expressed
at target site

69. Advantages
• Precision administration
• Small dosagesLess side effects

70. Gold Nanoparticles
Absorb Xrays
Use:Contrast
agenteffective RT
Antibacterial
therapyspecific Ab
selectively kill bacteria

71. Nanoerythrosomes
• Resealed erythrocytes
used
• Selective for liver and
spleen
• Use:
• Liver disease,Enzyme
disorders

72. NANOROBOTS
Introduce into body to detect
and repair damages
Use ultrasonic signals
and chemical sensors

73. • Uses of nanorobots:
• Atherosclerosis:Targeted at plaques
• Cancer:Attack tumors using Ultrasonic
signals
• Deliver medicine directly to diseased
organs
• Diabetes and Hypertension:Nanorobots
with sensors used

74. Quantum dots
Photodetector device
•Use:
•Chemotherapy illuminating
cancer cells
•Surgeons can see glowing
tumor and remove

75. Carbon Nanotubules
• Cylindrical shape
• Made of graphite,allotope
of carbon
• Use :
• Cancer
• Gene therapy
• Bronchial Asthma

76. Miscellaneous NDDS

77. Sustained release
drugs
Sustained release
drugs ProdrugsProdrugs
Prolonged release oral preparationsProlonged release oral preparations

78. Sustained release preparation
• Release medication in a predetermined
manner over extended period of time
• Eg:Diclofenac SR

80. Advantages
• Therapeutic effect for longer duration
• Less frequency of administration
• Less fluctuation
• Lesser side effects

81. Prodrugs
Inactive compoundBiotransform after
administrationActive compound

82. Examples of Prodrug :
To increase DOA Esters of Penicillin
To cross BBB  L-dopa in Parkinsonism
For site specific actionMethanamine in UTI

83.  Advantages :
 More stable
 Better bioavailability
 Less S/E
 Overcome bitter taste
 Improves Bioavailabilty

84. Newer Prodrugs
Clostridia Directed Enzyme
Prodrug therapy(CDEPT)
• Use Clostridia to convert
prodrug to active form
• Eg:Nitroreductase in
chemotherapy
Antibody directed Enzyme
Prodrug therapy(ADEPT)
• Use antibodies
• Increase tumour
selectivity
• Eg:Azathioprine

85. Novel Colon Drug Delivery
System
• CODESTM
• Uses Enteric coated Tablet
• Covered with:Lactulosecoated with acid
soluble Enteric coatingcoated with
Enteric coated material

86. • Outermost layer protects in
stomachdissolves after gastric
emptying
• Second layerprotective in alkaline pH of
Small Intestine
• Colon:Bacterial flora lowers the pH by
reacting with lactulosedrug released

87. Iontophoresis
• Mild electric current is applied for transport
of drugs across skin
• Eg:vasopressin,dexomethasone

88. • Dendrimer
• 3D structure(like tree)
• Nanoscale
• Uses:
• Gene delivery
• Anticancer drugs
• Nanoshells
• Can absorb light to
get heated up
• Lethal to cells
• Used in cancer
treatment

89. Osmotic Drug Delivery
System
• GITS
• Controlled delivery depending on Osmotic
pressure of drug
• Eg:Nifedipine GITS

90. Inhalable Insulin
• Available in Powdered form
• Delivered with Nebuliser
• Marketed by Pfizer in the name Exubera
• And Mannkind in the name Alfrezza