THEME: "Exploring the Challenges in Pre & Post Formulations and Drug Delivery Systems"
University of Swabi, Pakistan
Title: Chloroform-injection (CI) and Spontaneous-phase-transition (SPT) are Novel Methods; Simplifying the Fabrication Liposomes with Versatile Solution to Cholesterol Contents and Size Distribution
Mr. Muhammad Ijaz Khan is
Assistant Professor in the Department of Pharmacy University of Swabi, KPK,
Pakistan. He served various Pharmaceutical industries for 14 years before
joining the academia. His professional skills include formulation development
of various dosage forms, their validation and scale-up to commercial batch
production. He has keen interest in natural medicines and their targeted
delivery strategies. His research interest areas include neuroprotectives
regimens for neurodegenerative diseases. He believes in targeted drug
deliveries to overcome toxicities and improve amelioration. His key interests
include monocytes mediated drug cargo to the brain in the treatment of
neurodegenerative diseases. Unconventionally, he believes in the simplification
of complicated scientific approaches to make them available for global
humanity.
Statement of the Problem: Intricate formulation
methods and/or use of sophisticated equipment limit the prevalence of liposomal
dosage-forms. Simple techniques are developed to assemble amphiphiles into
globular lamellae while transiting from immiscible organic to the aqueous phase.
Methodology & Theoretical Orientation: Various
parameters are optimized by injecting chloroform solution of amphiphiles into
the aqueous phase and subsequent removal of the organic phase. Further
simplification is achieved by reorienting amphiphiles through a spontaneous
phase transition in a swirling biphasic system during evaporation of the
organic phase under vacuum. Findings: Although
the chloroform injection yields smaller size and PDI yet spontaneous phase
transition method overrides simplicity and productivity. The size distribution
of liposomes and solid/solvent ratio in both or any phases of formulation show
direct relation. Surface charge dependant large unilamellar vesicles with a
narrow distribution have PDI <0.4 in 10 µM saline. As small and monodisperse
liposomes are prerequisites in targeted drug delivery strategies. Hence the
desired size distribution <200 d.nm and PDI <0.15 is obtained through
serial membrane-filtration method. Phosphatidylcholine/water 4 µmol/ml is
achieved at a temperature of 10°C below the phase-transition temperature of
phospholipids ensuing suitability for thermolabile entities and high entrapment
efficiency. Both methods furnish the de-novo rearrangement of amphophiles into
globular lamellae aiding in the larger entrapped volume. The immiscible organic
phase facilitates faster and complete removable of the organic phase. High
cholesterol content (55.6 mol%) imparts stability in primary hydration medium
at 5+3°C for 6 months in light-protected type-1 glass vial. Conclusion & Significance: Collectively the
reported methods are novel, scalable, time-efficient yielding high productivity
in simple equipment.