INVITRO STUDIES OF

NOVEL DRUG DELIVERY SYSTEMS

Presented by Ashok kumar V 1 M.Pharm Dept. of pharmaceutics VIPS

CONTENTS

OCULAR DRUG DELIVERY SYSTEMSMICROSPHERESCOLON SPECIFIC DRUG DELIVERY SYSTEMSGASTRORETENTIVE DRUG DELIVERY SYSTEMSCOSMECEUTICALS

INVITRO STUDIES NOVEL DRUG DELIVERY SYSTEMS

Novel drug delivery system is a system for delivery of drug other than conventional drug delivery system.

For orally administered immediate release solid drug products, the test is referred to as a “dissolution” test, since the drug is intended to dissolve rapidly in the test medium.

For non-oral dosage forms the test is referred as “drug release test” or “in vitro release test”.

OCULAR DRUG DELIVERY SYSTEMS

INVITRO EVALUATION

Bottle method Mod.rotat.PaddleApparatus method

FlowThro.DevicesMod.rotat.Basketmethod

•Cultured bottle(PH.buffer.ph 7.4)•Shaken in thermostatical controlled(37°c) water bath.•Sampling done app. Intervals• D.C was analyased spectroscopically

•Dosage form placed in basket assembly.•Temp - 37±0.5°c.•Rpm-50•Sampling done app.Intervals •D.C was analyased spectroscopically

•Diffusion cells are placed.•Rpm-50.•Temp- 37±0.5°c.•Sampling•Analysis.

•Glass dissolution cell.Pump.Water bath.Reservoir.•Dosage form placed into reservoir.•Dissol.medium was circulated continuosly.•Temp- 37±0.5°c.•Sampling•Analysis.

MICROSPHERES Microspheres are characteristically free flowing powders consisting of

proteins or synthetic polymers which are biodegradable in nature and ideally having a particle size less than 200 μm.

Drug loading Physical entrapment. Chemical linkage Surface adsorption.

Dosage forms containing Microspheres(Transdermal/buccal fomulations)

INVITRO EVALUATION

Beaker method(buccal/transdermal)

Interface diffusion system(solid dosage forms)

Modified K C cell

•Dosage form is adhered to bottom of beaker.•Vol.buffer medium- (50-500ml).•Rpm- 60-300.• Sampling done app. Intervals.• D.C was analyased spectroscopically.

•CompartmentsA – (oral cavity) – dosage form in buffer soln.B – (buccal membrane) – in 1 octanol.C – ( body fluids) – 0.2 M Hcl.D – (protein binding) – in 1 octanol.

•Receptor- distilled water upto 50 ml.•Dosage form is fitted in between receptor and donor compartment.•Temp- 37±0.5°c.•Stirrer – 30 strokes / min.

COLON SPECIFIC DRUG DELIVERY SYSTEMS( CODESTM )

Drugs release from this systems is trigrred by colonic microflora coupled with ph sensitive polymers.

System is useful for treating colon related diseases Crohn’s disease. Ulcerative colitis. Colon cancer.

CODES™ configuration consists of a core tablet coated with 3 layers of polymer.

Outer coating( acid-soluble polymer- Eudragit E). Next coating( HPMC polymer). Core (active ingredient, one or more polysaccha-rides). The colonic bacteria enzymatically degrades the polysaccharide and releases drug.

INVITRO EVALUATION

By USP TYPE 2 & 3

Parameter

USP Apparatus II

USP Apparatus III

Dissolution medium

Buffers (pH 1.2, 6.8, and 5.0)

Buffers (pH 1.2, 6.8, and 5.0)

Temperature 37.0 ± 0.5oC 37.0 ± 0.5oC

Initial volume 900 mL 250 mL

Paddle/dip speed† 100 rpm 15 dpm

Drawn volume 5.4 mL 6.0 mL

Running time 1 hr in pH 1.2, 4 hrs in pH 6.8, and 4 hrs in pH 5.0 .

1 hr in pH 1.2, 4 hrs in pH 6.8, and 4 hrs in pH 5.0 .

Medium replacement

Media refilling at 60 and 300 min.

No media refilling.

GASTRORETENTIVE DOSAGE FORMS(GRDDS)

CRDDS possessing the ability of being retained in the stomach are called

GRRDS.

TYPES FDDS Swelling and expanding system Bio / Mucoadhesive system. High density system.

Figure 1.Novel Multicompartment Dissolution Apparatus.1 - Gastric Reservoir(5L), 2 - Intestinal Reservoir(5L) A - Gastric Compartment(100ml),B - Intestinal Compartment(500ml), C - Absorption Compartmen(vol.cylinder),D and E - Magnetic stirrer with heating facility, F - filter.

ValveFlow rate-2ml/min

0.1N HCL

PH.Buffer 7.2 pH

Dosage form used - cinnarizine floating tablet. Placed in gastric compartment . Magnetic stirrers were operated at 75 rpm.

Temperature were maintained at 37 ± 0.5 °C.

Cosmeceuticals Cosmeceuticals a particular a category of personal-care products that could

be placed at the border-line between cosmetics and pharmaceuticals. Eg ; creams, ointments and lotions (vitamins).

INVITRO EVALUATION

Franz-type diffusion The skin membranes were mounted with their polycarbonate filter with the

epidermal sidefacing upward into the donor compartment. The receptor medium composition. - phosphate saline buffer pH 7.4 (8 g/L

NaCl, 0.2 g/L KCl, 0.2 g/L KH2PO4 and 1.15 g/L NaHPO4 in bi-distilled

water), 3% w/w of polysorbate-20 and 0.25% w/w of isopropanol and DTT 0.4mg/mL.

A dose of 0.5–1.0mL of the cosmetic formulation (donor) was applied to the surface of the membrane.

At time intervals of 30–60 min within 5–24 h from application, appropriate aliquots of the receptor medium was withdrawn and immediately replaced with an equal volume of fresh buffer .

FRANZ DIFFUSION CELL

REFERENCES

Kashappa Goud, H. Desai, and T.M. Pramod Kumar. Preparation and evaluation of a novel buccal adhesive system. AAPS PharmSciTech. 2004; 5(3):article 35.

Reddy, S. M., Sinha, V. R. and Reddy, S. R. (1999) Novel oral colon-specific drug delivery systems for pharmacotherapy of peptide and nonpeptide drugs. Drugs of Today. 35 (7): 537-580.

Alagusundaram.M*, Madhu Sudana Chetty.C, Umashankari.K. Microspheres as a novel drug delivery system-A review article. International Journal of ChemTech Research. Vol.1, No.3 , pp 526-534.

Hitesh A.Patel, Jayvadan K. Patel, Kalpesh N. Patel, Ravi R.Patel. Ophthalmic Drug Delivery system –A Review. Scholars Research Library. Der Pharmacia Lettre, 2010, 2(4): 100-115.

Libo Yang *, James S. Chu, Joseph A. Fix. Colon-specific drug delivery: new approaches and in vitro/invivo evaluation. Int J of Pharm 235 (2002) 1–15.

Rajesh K. Parikh,Dhaivat C. Parikh,Renish R. Delvadia, and Sanjay M. Patel. A Novel Multicompartment Dissolution Apparatus for Evaluation of Floating Dosage Form Containing Poorly Soluble Weakly Basic Drug. Dissolution Technologies FEB 2006;pg 14-19.

Jinhe Li, Libo Yang, Sheila M. Ferguson, Tom J. Hudson, Shunsuke Watanabe , Masataka Katsuma . In Vitro Evaluation of Dissolution Behavior for a Colon-Specific Drug Delivery System (CODES™) in Multi-pH Media Using United States Pharmacopeia Apparatus II and III. AAPS Pharm SciTech 2002; 3 (4) article 33.pg 1-9.

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