Pharmacosomes

PHARMACOSOMES AS A TOOL FOR DRUG DELIVERY

1. PHARMACOsoMES PRESENTED BY TAMANNA AFNAN 1 ST YEAR (2 nd SEM), ROLL NO-19HMPS12 SUB- MOLECULAR PHARMACEUTICS HIMALAYAN PHARMACY INSTITUTE 1

2. CONTENT: Introduction Definition Components Importance Advantage Disadvantage Formulation Application Evaluation Conclusion Reference 2

3. INTRODUCTION Pharmacosome is a lipid based vesicular system have been developed in controlled and targeted drug delivery system. The term “pharmacosomes” comes from the Greek word pharmakon (drug) and soma (carrier). Pharmacosomes are the colloidal dispersions of drugs covalently bound to lipids and may exist as ultrafine vesicular, micellar or hexagonal aggregates, depending on the chemical structure. it deliver the drug to the target site at predetermined rate Pharmacosomes are amphiphilic complexes of drugs with lipids. The drugs bound either covalently, electrostatically or by hydrogen bonds to lipids. Pharmacosomes have been prepared for various non steroidal anti-inflammatory drugs, cardiovascular and antineoplastic agents. 3

4. Pharmacosome may be defined as a neutral molecule possessing both positive and negative charge, having water-loving and fat-loving properties, and an optimum ratio of polyphenol with phospholipids in a complex form. The drugs are present in a dispersion form in these lipoidal drug delivery system conjugated by electron pair sharing and electrostatic forces or by forming a hydrogen bond with lipids. Components of pharmacosomes: - Drugs Solvents Lipid Fig:1 - Pharmacosome 4

5. IMPORTANCE OF PHARMACOSOMES :- Pharmacosomes are suitable for incorporating both hydrophilic and lipophilic drug in vesicular system. Quick onset of action. Targeting the drug directly to the site of action . Reducing the toxic effect. Prohibition of drug leakage. To control the stability of the whole system . The pharmacokinetic parameters can be optimized for In-vivo testing. 5

6. Advantages:- Pharmacosomes are zwitter ionic, amphiphilic of polyphenolic compounds with PLs ,so it can deliver both hydrophilic and lipophilic drug. High and predetermined drug loading. Deliver drug directly to the site of infection. Reduction in adverse effects and toxicity. Stable and efficient due to covalent linkage. Size, functional groups (drug molecule), chain length (lipids) decides the degradation velocity into active drug molecule. Entrapment efficiency is not only high but predetermined, because drug itself in conjugation with lipids forms vesicles. 6

7. Disadvantages:- It requires surface and bulk interaction of lipids with drugs. It requires covalent bonding to protect the leakage of drugs. On storage, there is fusion and aggregation, as well as chemical hydrolysis. A compound can be synthesised depending on the amphiphilic nature . 7

8. FORMULATION OF PHARMACOSOMES:- 1.Solvent Evaporation Technique ( Hand-shaking method):- Drug+ lipid is dissolved in a volatile organic solvent. solvent is evaporated using rotatory evaporator in round bottom flask a thin film of solid mixture deposited on the walls of flask. The dried film hydrates with aqueous medium vesicular suspension is formed Fig-Hand shaking method -- 8

9. 2.Ether injection technique:- the drug lipid complex is dissolved in ether solvent. This mixture is then slowly injected into a heated aqueous agent vesicles are formed Fig: ether injection method 9

10. 3. Anhydrous co-solvent lyophilization method:- drug and phospholipids dissolved in solution of dimethyl sulfoxide containing glacial acetic acid mixture is agitated clear liquid is formed(freeze dried overnight) Complex is formed(flushed with nitrogen) Stored at 4 C vesicles are formed 10

11. APPLICATION:- Pharmacosomes demonstrate a wider stability profile and greater shelf life. Pharmacosomes have the capacity to increase drug absorption and its transport. Pharmacosomes can improve the rate of permeation by improving the membrane fluidity. Pharmacosomes have achieved a new level by enhancing therapeutic effects of several drugs like pindolol derivative. Pharmacosomes can be used for the development of novel ophthalmic dosage forms. Reduced haemolytic reaction. Enhance bioavailability of aspirin-phospholipid complex and reduced gastrointestinal toxicity. Pharmacosomes of 3,5-dioctanoyl-5-fluoro-2-deoxyuridine and observed good targeting efficiency ,and improved drug potential to pass through blood brain barrier . 11

12. Example of Drugs effect after incorporation in pharmacosomes Amoxicillin (Enhanced protection of cells treatment of peptic ulcers in male rats) Bupranolol hydrochloride (Augmented lymphatic transport and affect intraocular pressure) Cytarabin (Biological activity was enhanced) Dermatan sulphate(Biological activity was enhanced and improved bioavailability) Pindolol diglyceride (Plasma concentration improved up to three to five folds) Paclitaxel(Biological activity was enhanced) 12

13. EVALUATION OF PHARMACOSOME 1.Solubility:- To determine the change in solubility due to complexation, solubility of drug acid and drug-Peptide complex was determined in pH 6.8 phosphate buffer and n-octanol by the shake-flask method. Drug acid (50 mg)is added to Phosphate buffer pH 6.8 (50mL) then stirred for 15 minutes. The suspension was then transferred to a 250 mL separating funnel with 50 mL n-octanol and was shaken well for 30 minutes. Then the separating funnel was kept still for about 30 minutes .Concentration of the drug was determined from the aqueous layer spectrophotometrically. 13

14. Drug content:- To determine the drug content in pharmacosomes ( eg : diclofenac-PC complex), a complex equivalent to 50 mg diclofenac was weighed and added into a volumetric flask with 100 mL of pH 6.8 phosphate buffer. Then the volumetric flask was stirred continuously for 24 h on a magnetic stirrer. At the end of 24 h, suitable dilutions were made and measured for the drug content at 276 nm UV spectrophotometrically. Surface Morphology : To detect the surface morphology of the pharmacosomes, it was recorded on a scanning electron microscope. 14

15. Differential scanning calorimetry(DSC):- Thermograms of drug acid, phosphatidylcholine (80 %) and the drug -PC complex were recorded using a Differential Scanning Calorimeter The thermal behaviour was studied by heating 2.0 ± 0.2 mg of each individual sample in a covered sample pan under nitrogen gas flow. The investigations were carried out over the temperature range 25–250 °C at a heating rate of 10 °C min. XRPD:- The crystalline state of drug in the different samples was evaluated using X-ray powder diffraction. The X-ray generator was operated at 40 kV tube voltages and 40 mA tube current, using lines of copper as the radiation source. The scanning angle ranged from 1 to 60°. In-vitro-study:- Dissolution study is carried out 15

16. CONCLUSION:- Pharmacosomes is not only having high entrapment efficiency but it can be predetermined, because drug itself in conjugation with lipids forms vesicles. The approach of pharmacosomal drug delivery possesses many advantages over conventional vesicular systems. Hence, pharmacosomes have immense potential in improving the drug delivery in case of both natural and synthetic active constituents. Current research trends include cellular targeting using different approaches like PEGylation, biotinylation, and so forth. 16

17. REFERENCE:- Ali Gamal Ahmed Al- kaf et al., “A REVIEW ON PHARMACOSOMES: AN EMERGING NOVEL VESICULAR DRUG DELIVERY SYSTEM” Volume 2, Issue 1, 2017 , Universal Journal of Pharmaceutical Research. Thakur Sonam et al., ”PHARMACOSOMES: AN OVERVIEW” Volume 5 Issue 2; March-April; 2017; Page No.01-07 International Journal of Pharmaceutical and Biological Science Archive. Archana Pandita and Pooja Sharma “Pharmacosomes: An Emerging Novel Vesicular Drug Delivery System” for Poorly Soluble Synthetic and Herbal Drugs”1 August 2013 Hindawi Publishing Corporation, ISRN Pharmaceutics Sonam Ranga, Amit Kumar “A Review on Pharmacosomes “Nov;2013,RESEARCH AND REVIEWS: JOURNAL OF PHARMACEUTICS AND NANOTECHNOLOGY 17

18. THANK YOU 18