Bilosomes and emulsomes.pptx

Targeted drug delivery systems

1. Bilosome and Emulsomes Presented by- Parimal Hadge PE/2019/311 Sub-; PE-650

2. Contents 2/1/2021 2

3. Biosomes and Emulsomes Bilosomes 2/1/2021 3 Introduction Biosomes are consist of deoxycholic acid incorporated into membrane of neosomes .(Bile salt commonly use as penetration enhancer and increase bioavailability..) Biosomes are specialized delivery vehicles which protect vaccines from being broken down into the stomach , thereby enabling the oral delivery of vaccines as an alternative to administrating treatment by injection. In 2004, Mann et.al. developed nonionic surfactant vesicles, having liposomes use structures and stabilize then with bile salt for oral delivery of vaccine hence called BILOSOME. Different from liposomes and niosomes . Not only prevent antigen from degradation but also enhanced mucosal penetration. Developed as novel lipoidal vesicular system with internal solid fat core surrounded by phospholipid bilayer. This technology is designed to act as vehicle for poorly soluble drugs. The drug is enclosed in the emulsomes and provide prolong existence of drug in systemic circulation. Emulsomes

4. Bilosome and Emulsomes 2/1/2021 4

5. Advantages 2/1/2021 5 Non invasive system offer user acceptance and compliance. Less toxicity envelope suitable for wide range of therapeutic agents . The conventional injection method suffer from high relative cost and requires trained person to administer treatment. Immune response can be manipulated by controlling size and carrying vesicles. Allow small quantity of antigen to be effective and also increases efficacy of antigen which are weak when injected. They do not requires the use of live pathogens making them safe and effective alternative to traditional vaccines. Bilosomes removes cold chain requirement for preparation like vaccines. Emulsomes They defend drug from harsh gastric environment of stomach before oral administration because the drug is enclosed in the triglyceride lipid core. They increase the solubility and bioavailability of poorly aqueous soluble drugs. They provide significantly modify the pharmacokinetics of drugs. Emulsome based system showed excellent potential for targeting. They are economical alternative to current commercial lipid formulations because they reduce the dosing frequency of drug.

6. Preparation Methods for Bilosomes 2/1/2021 6 Reverse phase evaporation Bile salt stabilized vesicles i.e. bilosomes are prepared by a reverse-phase evaporation method or rotary film evaporator method or dry-film dispersing method. Briefly, film forming agents like soybean phosphotidylcholine , sorbitan tristearate or 1- monopalmitoyl glycerol are dissolved in organic solvents such as chloroform, ether or acetone in round bottom flask. The organic solvent is then removed under reduced pressure at specific temperature (around 40 °C) on a rotary film evaporator to form a dried thin film on the side of the flask. The anhydrous film is subsequently added with small amount of buffer solution containing specified amount of bile salt like sodium deoxycholate or sodium glycocholate to hydrate the dry film until a homogeneous dispersion is formed. Finally, this crude dispersion is extruded through a high pressure homogenizer to obtain a fine colloidal bilosomes dispersion. This colloidal dispersion is stored at 4 °C until use. Optimized colloidal dispersion of bilosomes may be obtained by tuning the homogenization parameters, phospholipid: bile salt ratio, drug: phospholipid ratio, water: organic solvent volume ratio, interior water phase pH, and the hydration buffer pH, which will also affect the particle size distribution and entrapment efficiency of bilosomes .

7. Methods 2/1/2021 7

8. Emulsomes 2/1/2021 8

9. Lipid film formation (Handshaking method) I n this method surfactants/lipids are casted as layers of film form their organic solution using flask rotary evaporator under reduce pressure (or by hand shaking) and then casted films are dispersed in aqueous medium. Upon hydration, the lipids swell and peel off from the wall of round bottom flask at temperature slightly above the phase transition temperature of surfactants used for specific period of time (time of hydration) with constant mild shaking. The mechanical energy is required for the swelling of lipid and dispersion of casted lipid film is imparted by manual by manual hand shaking or by exposing the film to a steam of water saturated nitrogen for 15 minutes followed by swelling in the aqueous medium without shaking. Hand shaking method produce multi lamellar vesicles (MLV) while non shaking method produced large unilamellar vesicles (LUVs). 2/1/2021 9 Sonication method Solid lipids Solid lipids, cholesterol, and phosphatidylcholine in different molar ratios were taken in a round-bottom flask and dissolved in a minimum quantity of chloroform containing 3 or 4 drops of methanol. To this solution, an accurately weighed quantity of drug was dissolved. The organic solvent was evaporated until complete dryness under reduced pressure using a rotary evaporator to form a thin lipid film on walls of the round bottom flask.

10. EVALUATION Dynamic light scattering instrument , Laser diffraction particle size analyzer Mean particle size is measured by Photon correlation microscopy. Polydispersity Index Dynamic light scattering instrument (DLS) Zeta Potential Dynamic light scattering instrument (DLS ) Morphology Transmission electron microscopy (TEM) Scanning electron microscopy (SEM) Entrapment efficiency percent High performance liquid chromatography (HPLC) 2/1/2021 10 The dried film was hydrated with phosphate-buffered saline pH 7.4 (10 mL) and homogenized by ultrasonication for 15 minutes at 40% frequency to obtain emulsomes of nanosize range. Particle size

11. Cont . In vitro  release Dynamic dialysis method Separation of free drug from drug-loaded vesicles Ultracentrifugation 2/1/2021 11

12. Some Bilosomes based vaccines preparations Influenza vaccine Titanous toxoid vaccine Influenza subunit Hepatitis B vaccine 2/1/2021 12 Some Emulsomes based vaccines preparations Silybin Emulsomes Case Study Amphotericin-B Emulsomes The antifungal agent, has been complexed with lipid to develop a less toxic formulation of AmB . AmB was formulated in trilaurin based nanosized lipid particles ( emulsomes ).Stabilized by soyaphosphatidylcholine as new IVDD system for macrophage targeting emulsomes prepared by cast film technique..

13. Cont. Formulation were optimized for AmB to lipid ratio , sonication time to obtain particle of nanometric size range. Emulsomes were modified by coating them with macropahges specific ligand.( O-palmitoyl mannan ) Characterization was done. They conclude that OPM coated emulsomes could fuse with macrophage of liver and spleen due to ligand receptor interaction . The praposed OPM coated emulsomes based system showed excellent potential for passive and active intramacrophage targeting, 2/1/2021 13

14. References 2/1/2021 14 Aburahma MH. Bile salts-containing vesicles: promising pharmaceutical carriers for oral delivery of poorly water-soluble drugs and peptide/protein-based therapeutics or vaccines. Drug delivery. 2016 Jul 23;23(6):1847-67. Chilkawar R, Nanjwade B, Nwaji M, Idris S, Mohamied A. Bilosomes based drug delivery system. J. Chem. Appl. 2015;2(5). Ahmad J, Singhal M, Amin S, Rizwanullah M, Akhter S, Amjad Kamal M, Haider N, Midoux P, Pichon C. Bile salt stabilized vesicles ( bilosomes ): a novel nano-pharmaceutical design for oral delivery of proteins and peptides. Current pharmaceutical design. 2017 Mar 1;23(11):1575-88. Kumar R, Seth N. Emulsomes : An emerging vesicular drug delivery system. Journal of drug delivery and therapeutics. 2013 Nov 14;3(6):133-42.

15. Thank you 2/1/2021 15