Presentationon

Formulation and Evaluation of Novel Anti-inflammatory Transdermal Drug Delivery System

presented by Sunita Thakur

(Enrollment no: 1512202007)

Prof. P.K Sharma Dr. Md. Aftab Alam Dean, Asst. Prof.School of Medical and Allied Sciences, School of Medical& Allied Sciences,Galgotias University, Greater Noida Galgotias University, Greater Noida (Guide) (Co-Guide)

Department of Pharmacy School of Medical and Allied Sciences

GALGOTIAS UNIVERSITYYamuna Expressway, G.B Nagar (U.P)

TABLE OF CONTENTS

S. NO. TITLE

1. INTRODUCTION

2. LITERATURE REVIEW

3. AIM AND OBJECTIVE 4. RATIONALE OF THE STUDY

5. PLAN OF WORK : RESEARCH ENVISAGED 6. EXPECTED OUTCOMES

7. CONCLUSION 8. REFERENCES

INTRODUCTION Transdermal therapeutic delivery may be defined as a

self contained, discrete dosage forms which, when applied to the intact skin, deliver the drug, via the skin at control rate for the systemic effect. (Gannu, R. et al., 2007)

Examples-1. Transderm-Nitro Nitroglycerin once a day medication for

angina (Novartis).2. Transderm-Scop Scopolamine for 72 hrs in treatment of

motion sickness (Novartis).3. Trans-Ver-Sal Salicylic acid for topical keratolytic action

(Doak)4. Antihypertensive, antiangina, antihistamine, anti-

inflammatory, analgesic and steroids. (Kumar P, et al.,2004).

Components of TDDS Patches-

Backing Layer Drug Membrane Adhesive Liner

FORMULATION APPROCHES-

MEMBRANE

MODERATED

1.Membrane type-( Sonam M. Ghandhi, 2013)

2.ADHESIVE DIFFUSION TYPE-

ADHESIVE

TYPE

FORMULATION APPROCHES-

3.MATRIX-DISPERSION TYPE-

MATRIX

TYPE

FORMULATION APPROCHES-

FORMULATION APPROCHES-

MICRO-RESERVOIR

SKIN –AS A SITE FOR TDDS- (Saurabh Ravi, et al., 2011)

The following routes are observed in transportation of penetrant through skin barrier: (1) Across the intact horny layer, (2)Through the hair follicles with the associated sebaceous glands, or (3) Via the sweat glands

Routes of Penetration

PROCESS OF TRANSDERMAL PERMEATION-(Bary B.W, et al., 1983)

Permeation EnhancersThe ideal enhancer should have the following conditions:(BaryB.W, et al., 1983)1. Non-pharmacological activities.2. Nontoxic, non-allergenic, and non-irritating.3. Rapid-acting with predictable and reproducible activity.4. When removed from the skin surface, the penetrability of the

skin should recover immediately.5. Cosmetically acceptable with suitable skin . e.g.These include water, pyrolidones, fatty acids and alcohols,

azone and its derivatives, alcohols and glycols, essential oils, terpenes and derivatives, sulfoxides like dimethyl sulfoximide and their derivatives, urea and surfactants.

Avoids first pass metabolism Avoids gut associated

metabolism Avoids pain associated with

injection Continuous “ sustained release”

drug delivery with infrequent dosing

Potential zero-order drug delivery

Easy to terminate therapy

Drug that require high blood levels cannot be administeredAdhesive may not adhere well to all types of skinDrug or drug formulation may cause skin irritation or sensitizationUncomfortable to wearMay not be economicalOnly relatively potent drugs.Only small and lipophillic drugs are administered.

ADVANTAGES DISADVANTAGES

ADVANTAGES AND DISADVANTAGES-

Characteristics of Drug for TDDS- Small daily dose < 10 mg- potent . Examples include

testosterone, scopolamine, nitroglycerin, fentanyl, clonidine and 17 ß Estradiol

Molecular weight should be < 500 Da High Partition coefficient Water soluble at physiological pH Non-irritating, non-sensitizing, non-allergenic Good stability

Criteria for Selection of drug candidate for transdermal drug delivery system:

a) Adequate skin permeability: Drugs with low molecular weight Drugs with low melting point Drugs with moderate oil and water solubility b) Adequate skin acceptability: Non-irritating drugs. Non-toxic drugs.Non-metabolizing drugs. c) Adequate clinical need: Need to prolong administration Need to reduce side effects on target tissues Need to increase patient compliance.

Criteria for selection of polymer :-

criteria should be satisfied for a polymer to be used in TDDS :

a) Molecular weight, chemical functionality of the polymer should be such that the

specific drug diffuses properly and gets released through it.

b) The polymer should be stable.

c) The polymer should be nontoxic

d) The polymer should be easily of manufactured

e) The polymer should be inexpensive

f) The polymer and its deagration product must be non toxic or non-antagonistic to

the host.

g) Large amounts of the active agent are incorporated into it.

Marketed Preparation -Product name Drug Manufacturer Uses

Alora Estradiol Theratech Hormone Replacement

Androderm Testosterone GlaxoSmithKline Hypogonadism

Catapres TTS Clonidine Alza/ Boehinnger Hypertension

Combipatch Estradiol Noven Hormone Replacement

Deponit Nitroglycerin Schwarz Pharma Angina Pectoris

Duragesic Fentanyl Jansen Pharmaceutical

Severe Pain

Estroderm Estradiol Novartis Post-menstrual Syndrome.

LITERATURE REVIEW-S.no.

Author’s Name Year Workdone

1. Chinchole P. et al., 2016 States that TDDS facilitate the delivery of API of drug through skin & can improve therapeutic efficacy and safety ,also describes various types of TDDS patches .

2. Bathe R. et al., 2015 Gives detail information regarding diffusion process through which drug diffuses into blood , having high conc.. On patch & low conc.. In blood, drug will keep diffusing for long period of time maintaining constant drug conc.. In blood flow.

LITERATURE REVIEW-3. Reddy V. et al., 2014 Describes briefly about the modes of drug

administration , advantages, and disadvantages of TDDS, drug penetration pathway, type of TDDS etc & considers TDDS as novel approach of delivery drug across skin.

4. Ghulaxe C. et al., 2015 Investigated with aimed to formulate transdermal film incorporated with herbal drug components and observed that well known ayurvedic drugs have been formed to be effective through modern pharmaceutical formulation techniques.

5. Sachan R. et al., 2013 Emphasized on the three generations of TDDS which start a new era of delivery of drug & proven that delivery through this technology offers significant clinical benefits over other dosage form.

6 Rastogi V. et al., 2012 Gives detailed information about main routes of drug penetration which includes the appendages, transcellular, & intercellular, permeation via rate limiting barrier stratum corneum.

LITERATURE REVIEW-

7. Anisree G. et al., 2012 Worked on Metoprolol tartrate, modifying it from conventional to TDDS successfully rectify its drawback i.e.. Due to short half life it gets metabolized via first pass metabolism.

8. Uzor P. et al., 2011 Presents a comprehensive account of various aspects of drug delivery by transdermal routes including the various chemical & physical penetration enhancers.

LITERATURE REVIEW-

AIM: Formulation and evaluation of Anti-inflammatory transdermal Patches.OBJECTIVE: To prepare transdermal patches.

To evaluate transdermal patches.  To perform in-vitro dissolution testing of prepared patches.  To perform stability studies of prepared patches.

AIM AND OBJECTIVE

 

Selection of Drug/Excipient Preformulation Studies IR Spectroscopy Melting point studies Calibration curve Solubility studies  Formulation of transdermal drug delivery system Evaluation of transdermal drug delivery system Thickness of Patch Weight Uniformity Folding Endurance Percentage moisture uptake Percentage moisture content Water vapour permeability (WVP) evaluation Uniformity of dosage unit test Stability studies Compilation of Data. Thesis writing.

RESEARCH ENVISAGED: PLAN OF WORK

The Rational approach is using skin delivery for systemic treatment. eg. Transdermal therapeutic systems provide systemic therapy for

conditions such as motion sickness, angina pectoris. By Providing smoother, continous drug delivery and steadies

plasma levels . It may reduces the incidence of side-effects. Making optimal therapeutic doses easier to attain & Potentially

improving treatment efficacy & compliance. TDDS patches are more patient and caregier friendly may enable

patients to continue treatment for longer periods. To attain greater, more sustained treatment benefits. Delivering of drugs directly to the viable skin , tissues without using

oral, systemic or other route of therapy.

Rationale of TDDS-

EXPECTED OUTCOMES

•Prepared controlled release transdermal patch may be used for providing the constant systemic effect.

•It will be able to deliver the drug in controlled manner for prolong time.

•This will reduce the dosing frequency and so it will provide better patient compliance.

CONCLUSION

Transdermal drug delivery system is a kind of delivering system which delivers the medicine to the general circulation through the skin is seen as a desirable alternative to the oral.

Intact skin is not sufficiently Permeable to the majority of drugs, hence permeation enhancement is needed.

TDDS improves the efficacy , safety and convenience of use.

REFERENCES Gannu ,R.,Vamshi Y.V,Krishan V.,Rao,Y.M, Development of

Niterndipine transdermal patches :in-vitro &Ex-vivo characterization ,current drug delivery,2007;4,pg.no-69-76.

Kumar P, Shankar C, Mishra B.; Delivery of macromolecules through skin, The Indian Pharmacist 2004, 5(3); pg.no:7-17.

Pravin Chinchole, Sagar Savale & Kambh Waelile, A novel approach on transdermal drug delivery system, World Journal of Pharmacy and Pharmaceutical Sciences, 2016; vol-5, issue 4.

Ritesh Bathe & Reni Kapoor, Transdermal drug delivery system :Formulation , development & evaluation –An overview, International Journal of Biomedical & Advance TDDS-33 research,2015; vol-6 (01), pg.no:1-10.

B. Venkateswara Reddy, S. Satyanandam , Transdermal drug delivery system – A review, International Journal of Chemistry & Pharmaceutical Sciences , 2014;vol-2(15).

Chetan Ghulaxe ,Rameshwar Verma , A Review on Transdermal Drug Delivery System , The Pharma Innovation Journal, 2015; VOL-4 (1), Pg.no:37-43.

Richa Sachan, Meenaskhi Bajpai, Transdermal drug delivery system :A Review , International Journal of Research and Development in Pharmacy & Lifesciences, 2013; vol-3(4), pg.no:748-765.

Vaibhav Rastogi, Pragya yadav, Transdermal drug delivery system: A overview, Asian Journal of Pharmaceutics, 2002.; 6(3)Pg.no:161.

Anisree G.S, Ramasamy C, John Wesely, Formulation of Transdermal drug delivery system of Metoprolol Tartrate and its evaluation , Journal of Pharmaceutical sciences & research,2012;vol-4(10).

P.F. Uzor, E.O. Omeje, C. J. Mbab, Prospective On Transdermal Drug Delivery , Journal Of Chemical & Pharmaceutical Research, 2011; Vol-3(3).

Bary B.W, Dermatological formulation: Percutaneous absorption, Marcel Dekker, 1983;Pg.no:238.

Thank you