Manju novel drug delivery

Novel drug delivery

1. Dr Manjuprasad Moderator:Dr Princy Palatty NOVEL DRUG DELIVERY SYSTEM 1

2. OVERVIEW Introduction Need for novel drug delivery system Types Advantages Disadvantages 2

3. 3 INTRODUCTION: Method of drug delivery can have a significant effect on its efficacy. Some drugs have an optimum concentration range within which maximum benefit is derived, and concentrations above or below this range can be toxic or produce no therapeutic benefit at all. From this, new ideas on controlling the  pharmacokinetic ,pharmacodynamics , non-specific toxicity, immunogenicity, biorecognition , and efficacy of drugs were generated.

4. 4 Ideal characteristics: Convenient to administer Economical Should not require special skills Should not cause pain Continuous absorption of drug Minimal frequency of administration Should not be embarassing

5. 5 CONVENTIONAL DRUG DELIVERY Enteral Parenteral- injections -inhalation -transdermal -transmucosal Local

6. NEED FOR NOVEL DRUG DELIVERY To maximize therapeutic effect To minimize adverse effects To increase bioavailability To minimize drug degradation To improve compliance To reduce the overall health cost 6

7. C LASSIFICATION Drug vehicles Drug devices 7

8. DRUG VEHICLES MICROSPONGES: Biologically porous inert particles, made up of synthetic polymers with the capacity to store a volume of an active agent upto their own weight eg: Retin A for acne vulgaris Carac containing flurouracil for actinic keratosis 8

9. IMMUNOCONJUGATES Monoclonal antibodies are conjugated with drug/radioisotopes ex: Ibritumomab tiuxetan - they carry Cancer killing radioactive particles directly to cancer cells of non-hodgkins lymphoma Attacks cancer cells minimizing harm to healthy tissues 9

10. BACTERIOPHAGE The phages are loaded with a large payload of a cytotoxic drug by chemical conjugation.   the drug hygromycin conjugated to the phages by a covalent amide bond, or the drug doxorubicin conjugated to genetically-engineered cathepsin-B sites on the phage coat. 10

11. VESICULAR SYSTEM LIPOSOMES Liposomes are small vesicles, formed of a bilayer of phospholipid, encapsulating an aqueous space of about 0.03 to 10 microns The most common vehicle currently used Non toxic, non hemolytic, non immunogenic even on repeated injection Produced by sonication of an aqueous suspension of phospholipids 11

12. Liposome 12

13. VIROSOMES A  virosome  is a drug or vaccine delivery mechanism consisting of unilamellar phospholipid membrane vesicle incorporating virus derived proteins to allow the virosomes to fuse with target cells. Virosomes are not able to replicate. This strategy has been proposed for immunization Can be administered via mucosa, intradermal, IM routes Eg: HIV1 13

14. CHOCLEATES Stable particles derived from liposomes Composed mainly of charged phosphatidyl serine Chocleate delivery have shown potentiate use of Amphotericin B Factor V111 14

15. COBOSOMES Similar to chocleates But have a multilayered structure of continuous lipid bilayer and have self assembly like cube They are biocompatible and show bioadhesive property ideal for oral administration eg: oral administration of cubosomes loaded with insulin ( exp was done in rats) 15

16. ETHOSOMES AND TRANSFEROSOMES They are like liposomes with increased flexibility due to addition of ethanol or surfactant They are specifically designed for skin delivery Ethosomes eg: Minoxidil, acyclovir Transferosome eg: oestradiol, norgestrel,insulin 16

17. eLIPOSOMES  defined as a liposome with internal emulsion droplets.  The enclosed emulsion droplets in an eLiposome add the ability to further control the location and time of release from the liposome with ultrasound.  Eg: Doxorubicin 17

18. CYCLODEXTRINS  family of compounds made up of sugar molecules bound together in a ring  3 types: alpha, beta and gamma Beta cyclodextrin is ideal due to large cavity size They can act as permeation enhancer to improve the drug absorption Eg: dexamethasone, nitroglycerin, nimesulide , iodine 18

19. 19 DENDRIMERS Highly branched synthetic Macromolecules Biocompatible and biodegradable Serve as a hub onto which a large number of drugs can be delivered Eg:5-FU methotrexate

20. 20 Resealed Erythrocytes Advantages Easy isolation Non immunogenic Large volume of drug can be given

21. 21 Protection from premature degradation Minimum toxic side effects Biodegradable Applications Oxygen deficiency therapy Delivery of antiviral agents Delivery of anticancer drugs

22. OSMOTIC PUMPS small tablet shaped units consisting of drug and osmotic substance in two different chambers Coated with semipermiable membrane which has minute laser drilled holes for drug release Eg: iron prazosin 22

23. DRUG DEVICES Drug eluting stents Normal metal stents coated with a pharmacological agent Agents are Sirolimus , Paclitaxel Sirolimus is an antiproliferative agent 23

24. 24 Used in Percutaneous coronary Interventions Reduces chances of restenosis from 25% to 50%

25. HORMONAL IUCDs These are 3 rd generation IUCDs They release hormone slowly into the uterine endometrium Used as contraceptives , DUB 25

26. Progestasert coated with natural progesterone Releases progesterone @65 micrograms/day Mirena Coated with levonorgestrel Releases the drug @20micrograms/day 26

27. LASER ASSISTED TRANSDERMAL DRUG DELIVERY It creates aqueous micropores not deeper than the epidermis with the help of laser scanner Active transdermal delivery is the only way forward to apply large molecule drugs through skin 27

28. Norplant Norplant  is a form of birth control  developed by Sheldon J. Segal and Horatio B. The original Norplant consisted of a set of six small (2.4 mm × 34 mm) silicone capsules, each filled with 36 mg of levonorgestrel  implanted subdermally in the upper arm and effective for five years 28

29. 29 Norplant II , consists of two small (2.5 mm × 43 mm) silicone rods each containing 75 mg of levonorgestrel,  being effective for five years

30. OCUSERT Pilocarpine is available in an ocusert form Used in the treatment of glaucoma Pilocarpine is sandwiched between 2 layers of ethylene-vinyl acetate membrane Contains alginic acid which serves as carrier for pilocarpine Impregnated with titanium dioxide – makes it easier for patient to see 30

31. It is placed in the cul de sac where it floats with tears Tears penetrates the microporous membrane & releases pilocarpine Pilocarpine can also be given through contact lenses 31

32. 32 INTRANASAL DRUG DELIVERY TO BRAIN Drug substances can be transferred along the olfactory nerve, bypassing BBB & entering the brain directly Olfactory transport is along olfactory nerve cells or along perineural space into the CSF Immediate drug delivery, sometimes faster than IV route Eg: NGF, erythropoetin and IGF

33. 33 MICROCHIPS They hold drug in a reservoir Implanted into the body under LA Released with the help of hand held wireless device Important in chronic conditions that require careful monitoring & precise therapy Compliance is improved Eg: PTH for osteoporosis

34. 34 PATIENT CONTROLLED ANALGESIC SYSTEM PCAS refers to electronically controlled, infusion pumps Delivers an amount of intravenous analgesics Handled by the patient himself Narcotics are the most common analgesics administered Used in cancer treatment & post operative pain

35. 35 Fentanyl given in a lollipop formulation

36. 36 DRUG ELUTING MICRO STENTS Microstents were coated with a polymer-drug compound and is implanted in the angle of iris and cornea Diffusion controlled release of paclitaxel or mitomycin is used to avoid blocking of stent

37. IONTOPHORESIS  The use of an electric current to introduce the ions of a medicament into bodily tissues An adhesive patch containing thin electrode and drug containing gel in contact with the skin Depending upon the dose and energy the drug either can act locally or can be carried into blood stream Eg: pilocarpine 37

38. 38 USG guided transdermal drug delivery Eg: Proteins (tPA,) Insulin Vaccines

39. 39 INSULIN DELIVERY INSULIN PENS Lesser Injection pain Convenient & easy to handle More accurate dosing Easier to use with visual & fine motor impairments Disadvantages Expensive and 2 different insulin cannot be mixed

40. 40 IMPLANTABLE INSULIN PUMPS 1.Open loop 2.Closed loop: Also called as artificial pancreas Main purpose of its development was for the management of Type1 DM Works on the principle of continuous glucose monitoring of blood, changes on which feedback will be sent to insulin pump and thus control of blood sugar

41. 41 INSULIN INHALERS Inhalable insulin was available from September 2006 to October 2007 in the United States as a new method of delivering insulin, but was found that injectable forms are more efficient in controlling blood sugars than inhalable form so was discontinued

42. 42 On 9/13/2011 it was announced that a form of inhalable insulin, aerosolized insulin, applied deep into the nostrils may delay the onset of Alzheimer's disease found to have betterment in memory and mood

43. 43 ORAL INSULIN : A chemical make-up that protects insulin during passage through the gastrointestinal tract. Absorption enhancers so that insulin could be absorbed by the intestine Rapidly acting insulin is used

44. 44 VACCINE : Scientists have developed worlds first drug that decreases destruction of islet cells Drug is a peptide prepared by modifying a fragment of protein

45. 45 RECTAL DELIVERY : bypass of the hepatic first pass metabolism The delivery is safe from presence of diet and encounters less degrading enzymes. INSULIN PATCHES : designed to release insulin slowly and continuously.

46. 46 RECENT TRENDS OF NANOTECHNOLOGY

47. 47 MECHANICAL DRILLING of a small tumor mass by Nano Robots

48. 48 A MICROSCOPIC MACHINE roaming through the blood stream and taking samples for identification and determining concentration of different compounds

49. 49 MEDICAL NANO DEVICES could augment the immune system by finding and disabling unwanted bacteria and viruses

50. 50 A NANO ROBOT nibbling on a atheromatous plaque in a blood vessel

51. 51 Clot Inducing Medical Robots are shown in various stages of clot netting deployment

52. 52 Search for the ideal drug delivery system is on…… SUMMARY

53. 53 REFERENCES Goodman & Gillman 12 th edition Target and controlled drug delivery system –novel carrier system Y S Vyas Controlled and novel drug delivery system -Sanjay Jain Verma RK., Mishra B., Garg S. Osmotically Controlled Oral Drug Santini, J. T., Cima M.J. & Langer, R. “A controlled release microchip.” Articles from wikipedia , pubmed

54. 54 THANK YOU