Permeation enhancer of Transdermal drug delivery system

PRESENTED BY CHETAN DIGAMBAR PATIL

1. Presented by Guided by Patil Chetan Digambar Mr. Samir Shaik F Y.M.Pharm ( sem 1 st ) Asst. Professor & PG Teacher Dept. Of Pharmaceutics Dept of Pharmaceutics ROLL NO 10 Permeation Enhancer of Transdermal Drug Delivery System SHREE SURESHDADA JAIN INSTITUTE OF PHARMACEUTICAL EDUCATION AND RESEARCH, JAMNER 2023-24

2. Introduction Definition of TDDS Transdermal therapeutic are defined as self contained discrete dosage form which when applied to the intact skin deliver the drugs, through the skin, at a controlled rate to the systemic circulation.

3. Permeation enhancers: These are the compounds which promote skin permeability by altering the skin as a barrier to the flux of a desired penetrant (drug).These are also known as accelerants / sorption promoters Ideal properties: 1 Should work rapidly. 2. The activity and duration of effect should be both predictable and reproducible 3. should not have pharmacological activity 4. Should work unidirectionally (prevent loss of endogenous material from body 5. When removed form skin, the barrier properties should return both rapidly and fully.

4. IMPORTANCE OF PERMEATION ENHANCER Increase Drug Absorption Broader Drug Options Patient compliance- Steady Drug Release Avoidance of First Pass Metabolism Reduce frequency of administered Targeted Therapy. CHALLENGES OF PERMEATION ENHANCER 1) Skin Barrier Resistance 2) Variable Skin Type 3) Safety Concern 4) Chemical Stability 5); Patient Compliance 6) Regulatory Approvals 7) Interaction with Excipients

5. ClassificaTion of Penetration Enhancer IN TDDS A..PHYSICAL PENETRATION ENHACER :- 1.Electeroporation 2. Iontophoresis 3. Ultrasound 4. Laser radiation and photochemical waves 5. Microneedle –based devices B. CHEMICAL PENETRATION ENHANCER :- 1. Sulphoxide 2. Surfactants 3. Adhesives 4. Alcohols ,fatty alcohols & glycols

6. A.PhysicAl penetration Enhancer :- 1. Electroporation :- Electroporation involves the application of high voltage pulses to induce skin perturbation Highvoltages (≥100 V) and short treatment durations (milliseconds) are most frequently employed . The technology has been successfully used to enhance the skin permeability of molecules with differing lipophilicity and size . ( small molecules , proteins and peptides,) 2. IontoPhoresis :- This method involves enhancing the permeation of a topically applied therapeutic agent by the application of a low-level electric current, either directly to the skin or indirectly .Via the dosage form . Applications :- The main advantage of iontophoresis in diagnosing cystic fibrosis and recently for monitoring blood glucose level . Schematic Representation of IontoPhoresis patch

7. 3. Ultrasound ( Sonophoresis ) :- Ultrasound involves the use of ultrasonic energy to enhance the transdermal delivery of solutes either simultaneously or through pretreatment, and is frequently referred to as sonophoresis . The proposed mechanism behind the increase in skin permeability is attributed to the formation of gaseous cavities within the intercellular lipids on exposure to ultrasound, resulting in disruption of the stratum carenum . 4. Laser Radiation and Photochemical waves :- Lasers have been used in clinical therapies for decades, and therefore their effects on biological membranes are well documented Lasers are frequently used for the treatment of dermatological conditions such as acne and to confer facial rejuvenation, where the laser radiation destroys the target cells . .Such direct and controlled exposure of the skin to laser radiation results in ablation of the stratum corneum without significant damage to the underlying epidermis .

8. Schematic Representation of the Mechanism of this action of micro-needle-based devices 5. MICRONEEDLE – BASED DEVICES :- These microneedles of length 50 to 110 mm will penetrate the stratum corneum and epidermis to deliver the drug from the reservoir. The reservoir may contain drug, solution of drug, gel, or solid particulates, and the various embodiments of the invention include the use of a membrane to separate the drug from the skin and control release of the drug from its reservoir

9. B.Chemical penetration Enhancer 1. Sulphoxide and simillar Chemicals :- It is a powerful aportic solvent which binds with hydrogen rather than with water. It is colorless, odorless, and is hydroscopic, and is often used in many areas of pharmaceutical sciences as a ‘universal solvent.’ Dmso alone has been applied topically to treat systemic inflammation. The mechanism of sulphoxide penetration enhancers widely used to denature proteins and on application toskin has been change the intercellular keratin conformation . 2. Surfactants :- Surfactants are added to formulations in order to solubilise lipophilic active ingredients, and so they have potential to solubilise lipids within the stratum corneum. Sls is a powerful irritant and increase the transepidermal water loss in human volunteers in vivo, and both anionic and cationic surfactants swell the stratum corneum and interact with intercellular keratin.

10. 3. Adhesive :- Adhesive are in contact between the skin and transdermal system .It carries the drug which is dissolved or dispersed in solition or suspension form . Example is polyacrylates, silicones 4. Alcohols , fatty alcohols and Glycols :- Ethanol is commonly used in many transdermal formulations and is often the solvent of choice for use in patches. It is also commonly employed as a cosolvent with water for ensuring sink conditions during in vitro permeation experiment. When using an ethanol water cosolvent vehicle, the enhancement effect of ethanol appears to be concentration dependent..

11. Reference Prafull P. Patil, Dr.Md.Rageeb md usman & Dr.Sayaji sarode , “ A textbook of drug delivery system ,” by PV publication . Y.Madhusudan Rao & A.V.Jithan , “Advances In Drug Delivery “ Volume III , by Pharmamed Press . https://www.google.com.Net/ankitarai710/penetration-enhancer-with-their-examples-55729514 Https://permegear.Com/?Mdocs-file=8947 .