International Journal of Applied Pharmaceutics, 2025
Objective: This study aims to enhance the pharmacokinetics and pharmacodynamics of levomilnacipra... more Objective: This study aims to enhance the pharmacokinetics and pharmacodynamics of levomilnacipran by developing a nanostructured lipid carrier for nasal delivery, bypassing the blood-brain barrier via olfactory and trigeminal pathways to improve drug availability in treating depression. Methods: The solvent diffusion approach was used to create levomilnacipran nanostructured lipid carriers (LEV-NLC), which was then tuned for different physicochemical properties. The rat model was used to assess the antidepressant effects of optimised levomilnacipran, in conjunction with biochemical assessment of brain monoamines. In addition, this estimated various pharmacokinetic parameters by measuring levomilnacipran levels in brain and blood plasma at different time intervals. Results: The optimized LEV-NLC showed a particle size of 121 nm, zeta potential of-25 mV, and entrapment efficiency of 88%. Transmission electron microscopy (TEM) analysis revealed spherical nanoparticles with uniform morphology. In vitro release studies demonstrated sustained drug release, with cumulative LEV release of 77.21±3.87% at pH 7.4 and 76.32±3.54% at pH 6.0 over 24 h. Pharmacokinetic analysis showed enhanced bioavailability for LEV-NLC (62%) compared to LEV solution (28%), based on plasma AUC values. In behavioural studies, LEV-NLC significantly reduced immobility (by 101 counts), and increased swimming time (by 128 s), climbing time (by 50 s), and locomotor activity (by 193 counts), indicating antidepressant-like effects. Neurochemical analysis revealed significantly increased serotonin (P<0.01) and noradrenaline (P<0.05) levels in the LEV-NLC group, while dopamine levels showed a non-significant increase (P>0.05). Conclusion: The pharmacokinetic profile of levomilnacipran in the brain and the brain/blood ratio at various time points were both enhanced by the nose-to-brain delivery of the NLC. Therefore, the intranasal administration of levomilnacipran NLC may hold promise as a treatment for depression.
Current Issues in Pharmacy and Medical Sciences, 2025
The current review focuses on the potential of solid lipid nanoparticulate systems for effective ... more The current review focuses on the potential of solid lipid nanoparticulate systems for effective targeted delivery to the brain. The challenges in delivering the drug to the brain are discussed, as are brain targeting strategies and possible mechanisms. The benefits of using solid lipid nanoparticles as carriers to deliver the drug into the brain are also addressed. Furthermore, the physical and chemical properties of solid lipid nanoparticles are considered with regard to solving the important challenges raised in developing the appropriate brain targeting formulations. The authors conclude that a thorough examination of the technology's potential use concerning the current state of brain medication research is urgently required.
International Journal of Nutrition, Pharmacology, Neurological Diseases, 2024
The blood-brain barrier (BBB) protects the central nervous system, one of the body's most fragile... more The blood-brain barrier (BBB) protects the central nervous system, one of the body's most fragile microenvironments, by controlling its homeostasis. The BBB is a very complex system that strictly restricts the transport of ions from the blood to the brain of a confined amount of tiny molecules and a much lower number of large molecules, defending the brain from diseases and injuries. However, the BBB severely inhibits drug transport to the brain, hindering the treatment of various neurological problems. As a result, numerous techniques are under development to improve drug delivery across the BBB. This review summarizes the anatomical and physiological characteristics of the barriers and the current drug delivery strategies for the brain. Although these methods provide many fascinating possibilities for targeting and brain delivery, only a few have progressed to the point where they can be used safely and effectively in humans. In addition, concerted efforts using a variety of other methodologies will enable the translation of preclinical findings into tangible clinical applications in the targeted delivery of drugs.
Aim: To evaluate the anti-amnesia effect of Bauhinia purpurea in Scopolamine induced amnesia in r... more Aim: To evaluate the anti-amnesia effect of Bauhinia purpurea in Scopolamine induced amnesia in rats. Materials and Methods: A total of 30 rats were divided into 5 groups 6 rats in each. Group I considered as normal control. Group II served as negative control. Group III, IV and V were treated with Donepezil (3 mg/kg), ethanolic extract of Bauhinia purpurea 200mg/kg and 400 mg/kg respectively for 14 consecutive days followed by single administration of Scopolamine (3 mg/kg) to all the groups except group I. Cognitive performance was assessed by the Morris water maze, elevated plus maze and passive avoidance paradigm. Acetyl cholinesterase enzyme level, biochemical markers such as lipid peroxidation, reduced glutathione and β amyloid 1 42 level, Neurotransmitters including dopamine and serotonin and histopathological study of rat brain were estimated. Results: Bauhinia purpurea and Donepezil rats showed significant increase in escape latency, step-through latency and decreased transfer latency in respective cognitive models of the Morris water maze, passive avoidance test and elevated plus maze. Additionally, Bauhinia purpurea extract remarkably promoted the cholinergic neurotransmission, decreasing β amyloid protein and protected against the oxidative stress damage as indicated by, increasing reduced glutathione level, lowering the level of lipid peroxidation, restored dopamine and serotonin level in the brain. Furthermore, histopathological studies revealed the reversal of neuronal damage in the treatment group compared to Scopolamine treated rats. Conclusion: Bauhinia purpurea extract showed promising antiamnesia activity against scopolamine induced amnesia in rats. This could be attributed to its brain acetyl cholinesterase level, β amyloid level inhibition, antioxidant activity and alteration in neurotransmitters level.
Aim: The aim of the present study was to prepare acyclovir (ACV)-loaded solid lipid nanoparticles... more Aim: The aim of the present study was to prepare acyclovir (ACV)-loaded solid lipid nanoparticles (SLNs) to sustain the release of the drug. Materials and Methods: ACV SLNs were prepared by an emulsification and low-temperature solidification method. The nanoparticles were further characterized for particle size, zeta potential, surface morphology, drug entrapment efficiency, and in vitro drug release behavior. Results: The results revealed that this method is reproducible, more feasible and led to the entrapment of drug with an expected sustained release. The nanoparticle precipitated was with particle size of 180 nm, zeta potential of −25 mV, and spherical in shape. The entrapment efficiency noted was 78%. In vitro release was about 78% release in 35 h, which indicated that the ACV-loaded SLNs provide sustained release and release behavior was in accordance with zero-order kinetics. Conclusion: ACV-loaded SLNs may be a good choice for the improvement of bioavailability and reduction in toxicity with a good sustain release over a long period.
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Papers by Parthiban R