Pharmacosomes System Development

Pharmacosomes refer to complex forms of neutral molecules with positive and negative charges, hydrophilic and lipophilic properties, and an optimal ratio of polyphenols to phospholipids. The drugs in pharmacosomes exist as dispersions in these lipid-based drug delivery systems, bound by electron pair sharing and electrostatic forces or by forming hydrogen bonds with lipids. Based on years of extensive experience with drug delivery systems, CD Formulation has developed pharmacosomes-based drug delivery vesicle systems.

Fig.1 Forms and component of pharmacosomes. (Bhingare et al., 2014)

Characteristics of Pharmacosomes

• Pharmacosomes are both hydrophilic and lipophilic and readily cross cell membranes, cell walls or tissues by cytocytosis or cytoconjugation.
• The rate of degradation depends on the nature of the functional groups present in the drug molecule, the length of the fatty acid chains in the lipid.
• They can be administered by topical, oral, extravascular or intravascular routes.

Pharmacosomes System Development

Pharmacosomes provide an effective method of delivering drugs directly to the site of action, thereby reducing drug toxicity and eliminating side effects. CD Formulation can provide customized pharmacosomal products or related services to our valued customers.

Characterization of Pharmacophore

The properties of vesicles depend on their different configurations, composition, shape, retention, apparent charge and concentration.

1. Complex detection

With the help of FTIR spectroscopy, the formation of complexes or conjugates can be determined by correlating the spectra observed in complex samples with the spectra of discrete components and their mixtures.

2. Stability of drug

Once the product has been lyophilized, the spectra of the solid complex at different time points are correlated with the spectra of a dispersion in water composed of small particles and used to assess the stability of the system.

3. Morphological analysis

Scanning electron microscopy/transmission electron microscopy can be used to study the surface order of the pharmacosomes. The purity grade of the lipids used and several variables observed during the operation (preparation method, vacuum distribution and rotation speed) modify the shape and size of the pharmacosomes.

4. Solubility analysis

Changes in solubility caused by complexation can be assessed using the shake flask technique.

5. Drug-lipid compatibility analysis

Differential scanning calorimetry is a thermal analysis technique used to determine drug-lipid compatibility and its interactions.

6. Crystallographic measurements

The crystalline nature of a drug can be determined using X-ray diffraction techniques.

7. In vivo and in vitro evaluation

In vivo and in vitro evaluations are performed based on the expected therapeutic activity of the bioactive components. In vitro dissolution studies of drug-complexes and common drugs were carried out in standard dissolution apparatus on media of different pH to determine their pH-dependent dissolution profiles.

Advantages of Pharmacosomes over Other Vesicle Systems

a. The drug release process is hydrolysis rather than bilayer diffusion, surface desorption or degradation as in the case of liposomes.

b. Unlike liposomes, the encapsulation efficiency of pharmacosomes is not affected by the volume of the inclusion complex.

c. The membrane fluidity of the pharmacosomes depends on the temperature of the conjugated phase transition and does not affect the rate of release of the pharmacosomes due to the covalent binding of the drug to the lipid.

d. No drug leakage or precipitation due to covalent binding of drug to the carrier.

e. Improved bioavailability of insoluble drugs.

f. Targeted delivery to the site of infection.

g. Reduced cost of treatment.

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Reference

1. Bhingare, U., et al. (2014) Pharmacosomes: A novel drug delivery system. Int J, 3(1), 14-20.