Formulation and evaluation of Duloxetine loaded bio-nano suspension for brain specificity via acoustic meatus

Abstract

Research articlethe deeper parts of the auricle are supplied by the vagus nerve [X] (the auricular branch) and the facial nerve [VII] (which sends a branch to the auricular branch of the vagus nerve [X]). (4) These unique features serve as a drug delivery platform for effective delivery of API molecules.The economic cost of depression and its treatment are estimated at $6 billion in Canada, US$ 83 billion and £118 billion. Depression is a chronic, recurring and potentially life-threatening illness that affects up to 20% of the population across the globe. The etiology of the disease is suboptimal concentrations of the monoamine neurotransmitters serotonin (5-HT) and norepinephrine (NE) in CNS. It is also due to consequence of dysfunctional endocrine, immune and neurotransmitter systems.Duloxetine is an antidepressant that blocks the reuptake of both serotonin (5-HT) and norepinephrine (NE) by presynaptic transporters and also has low affinity for muscarinic cholinergic, histamine H1, 1 adrenergic as well as serotonin and dopamine receptors (5). Duloxetine exhibits seven to nine-fold greater potency at blocking ligand binding to the serotonin transporter (SERT) than the norepinephrine transporter (NET) and is about 3.5 times more potent at blocking [3H] 5-HT uptake than that of [3H] NE. (6). Duloxetine shows a very different distribution pattern. Very low concentrations in the cerebrospinal fluid is seen may be due to the fact that the drug crosses the bloodcerebrospinal fluid barrier much worse than other antidepressants do, suggesting a low ability of duloxetine to enter the brain. Alternatively, low drug concentrations may be interpreted in a sense of a missing residence time in cerebrospinal fluid due to active transport mechanisms out of this environment either back into the bloodstream or into the brain. (7) Aim of the research was to design a suitable formulation loaded with Duloxetine using a novel biopolymer from kernels of Prunus amygdalus as a bio-retardent and stabilizer for delivering nanosized Duloxetine molecule through trans acoustic epithelial route for improved therapeutic efficacy of API. Material and MethodsDuloxetine was obtained as a gift sample from INTAS Dehradun. Biomaterial was obtained from the local market; remaining materials used were of analytical grade. Satheesh Madhav, Director, DIT University, Makkawala, P.O Bhagwantpura-248009, Dehradun, Uttrakhand, India, Tel: +91 9760203573; Fax no: 3000309; Email: satheesh_madhav@yahoo.com AbstractThe aim of the current research work was to formulate drug loaded nano-suspension using novel bioexcepient isolated from kernels of Prunus amygdalus and to explore the capability of external acoustic meatus as novel acoustic drug delivery system. The biomaterial was extracted by simplified economical process and was further purified by hot dialysis method. The isolated biomaterial was subjected to various physicochemical evaluations along with spectral analysis including UV, IR, Mass, NMR, SEM. The bio-nano suspension formulated with the n...

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“…The particle size of the formulated bionanosuspension was evaluated by measuring the % transmittance as well as with the help of measuring zeta particle size as well as zeta potential. 7 The particle size for the zetasizer shows the particle size of 615nm which confirms it nano particle size range for the best formulation PF4. The stability of bionanosuspension was also showed significant with -20.1 mV zeta potential.…”

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“…In this method, the biopolymer as bio stabilizer cum bioretardant was mixed with other ingredients like a preservative, surface active agent like PVA, nanosizent with the distilled water to make a well-dispersed suspension [14]. Then the mixture was subjected to bath sonication for 10-15 cycles to formulate the nanosized drug-loaded bionanosuspension [4,15].…”

“…Madhav and Raina [15], developed and evaluated duloxetine loaded bionanosuspension. The bionanosuspension was prepared by using the biopolymer isolated form Prunus amygdalus seeds.…”

“…The prepared bionanosuspension was then evaluated for different parameters like particle size, entrapment efficacy, dispersibility, zeta potential, in-vitro release and in-vitro kinetic study and also invivo study for the determination of the amount of duloxetine reached to brain via external acoustic meatus. Madhav and Raina [15], explored the feasibility of external acoustic meatus for targeting of escitalopram bionanosuspension to brain. The research reveals that escitalopram loaded bionanoparticles were found to be targeted to brain via external acoustic meatus administration.…”

“…The research reveals that Piper nigrum can be safely used for development of bionanosuspension for targeting to brain via external acoustic meatus. Madhav and Raina [15], described about the preparation of duloxetine loaded bionanogel for brain targeting via external acoustic meatus. In the research work the biopolymer was isolated form Tagetes papatule and its ability in developing the duloxetine loaded bionanogel for brain targeting.…”