Ranolazine is (±)-n-(2,6-dimethylphenyl)-4-[2-hydroxy-3-(2-methoxyphenoxy)propyl]-1-piperazine acetamide, used in the treatment of chronic stable angina in patients who have an inadequate response to traditional anti-anginals (like β blockers, nitrates etc). its log p value is 1.6. it is bcs class 2nd drug, having bioavailability of 35-45 % only. the drug is metabolized by cytochrome p450 (cyp3a4) enzymes and to a lesser extent by cyp2d6, with 5% excreted unchanged by the kidney. short biological half life (7 hrs) causes difficulties in maintaining the desired concentrations in the blood, determined the need for the development of an sustained release formulation which may be achieved by vesicular drug delivery system like proniosomes. a steady-state concentration is generally achieved within 3 days of 500–1000 mg/bid. the presently preferred route of administration for ranolazine is oral. ranolazine is available as film-coated sustained-release 500 mg tablets, a hard gelatin capsule filled with a powder mix or granulates, or a soft gelatin capsule (soft-gel) filled with a solution or suspension. vesicular system includes liposomes, virosomes, niosomes, proniosomes transferosomes, proteasomes, sphingosomes, archaesome and ethosomes etc. in past few decades vesicles have become the important vehicles of choice in drug delivery. vesicles are colloidal particles in which a concentric bilayer made-up of amphiphilic surfactant molecules surrounds an aqueous core. encapsulation of drug in vesicular structures can be predicted to prolong the existence of drug in systematic circulation and perhaps, reduce the toxicity if selective uptake can be achieved. drug delivery systems using colloidal particulate carriers such as liposomes or niosomes offers distinct advantages over conventional dosage forms. these carriers can act as drug reservoirs, and modification of their composition or surface can adjust the drug release rate and/or the affinity for the target site. proniosomes behave invivo like liposomes as they are able to prolong the circulation of encapsulated drug altering its organ distribution and metabolic stability and release drug at a slow rate to sustain the drug effect. moreover, they can increase solubility of poorly soluble compounds, providing a tangible strategy to overcome formulation problems of many therapeutic molecules with low solubility. in the present study the ranolazine containing proniosomes based on surfactant like span 20, 60 and tween 20 and cholesterol and maltodextrin were developed. the selected proniosomal formulation was further incorporated in hpmc k100m (2%) based gel for external application. the developed proniosomes were evaluated for production yield; particle size, zeta potential, entrapment analysis, sem, and xrd analysis. the hpmc based gel were invitro evaluated for ph, viscosity measurement, drug release study, gel strength measurement and exvivo diffusion study through albino rat skin. formulation containing tween 20 (150 mg), cholesterol (100 mg) and maltodextrin (400 mg) showed best result. hence it was selected for the stability study and which was observed to be stable for three months without any changes in its size, zeta potential, entrapment efficiency and drug release study.
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