Design, characterization, and evaluation of intranasal delivery of ropinirole-loaded mucoadhesive nanoparticles for brain targeting.

Context: Parkinson disease (PD) is a common, progressive neurodegenerative disorder, characterized by marked depletion of striatal dopamine and degeneration of dopaminergic neurons in the substantia nigra.

Objective: The purpose of the present study was to investigate the possibility of targeting an anti-Parkinson's drug ropinirole (RH) to the brain using polymeric nanoparticles.

Materials And Methods: Ropinirole hydrochloride (RH)-loaded chitosan nanoparticles (CSNPs) were prepared by an ionic gelation method.

Formulation of extended release cefpodoxime proxetil chitosan-alginate beads using quality by design approach.

The purpose of this work was to develop and characterize chitosan-alginate beads for the extended delivery of cefpodoxime proxetil (CFP), to understand the impact of formulation and process parameters on the critical quality attributes (CQAs) using a quality-by-design approach. For this, a study was performed with various formulation and process parameters to determine their impact on CQAs of beads, which were determined to be time for 80% of the drug released (T80%), particle size, and encapsulation efficiency. The beads of CFP were optimized using a three-factor, three-level Box-Behnken design.

Pharmacoscintigraphic evaluation of potential of lipid nanocarriers for nose-to-brain delivery of antidepressant drug.

Efficacy of antidepressants relies upon their continued presence at the site of action (brain) over a prolonged period of time. The BBB restricts the access of antidepressants to the brain on oral as well as intravenous administration. Direct delivery (by-passing the BBB) of antidepressant drugs can increase the CSF concentration with concomitant reduction in dose and side effects.

Formulation, development and optimization of raloxifene-loaded chitosan nanoparticles for treatment of osteoporosis.

Context: Osteoporosis (OP) is a disease of skeletal system and is associated with fragility fracture at the hip, spine and wrist. Various drugs have been used to treat OP. One of them is raloxifene hydrochloride (RLX), a second-generation selective estrogen receptor modulator (SERM) approved by the USFDA.

Nanoethosomes mediated transdermal delivery of vinpocetine for management of Alzheimer's disease.

Aim: To develop and statistically optimize nanoethosomal formulation for transdermal delivery of vinpocetine as an anti-Alzheimer's drug.

Materials And Methods: Box-Behnken experimental design was applied for optimization of nanoethosomes. The independent variables were phospholipid (X), Tween 80 (X) and Ethanol (X) while entrapment efficiency (Y), particle sizes (Y), elasticity (Y) and flux (Y) were the dependent variables.

Donepezil nanosuspension intended for nose to brain targeting: In vitro and in vivo safety evaluation.

The present study was to develop donepezil loaded nanosuspension for direct olfactory administration which reaches the brain and determining safety profile in Sprague-Dawley rats. Nanosuspension was prepared by ionic-crosslinking method. The developed nanosuspension was intranasally instilled into the nostrils of rats with the help of cannula (size 18/20) so that drug reached into the brain directly via nose to brain pathway.

Lipid drug conjugate nanoparticle as a novel lipid nanocarrier for the oral delivery of decitabine: ex vivo gut permeation studies.

The purpose of this study was to develop lipid drug conjugate (LDC) nanoparticles of decitabine (DCB) using stearic acid as a lipid to increase the permeability of the drug along with its protection from chemical degradation. The LDC was prepared by salt formation of DCB with stearic acid and followed by cold homogenization technique to produce the LDC nanoparticles. The role of key independent variables influencing on dependent variables were determined by using a Box-Behnken design.

Intranasal infusion of nanostructured lipid carriers (NLC) containing CNS acting drug and estimation in brain and blood.

The present study was aimed to evaluate the nanostrucured lipid carriers (NLC) containing duloxetine (DLX-NLC) for intranasal infusion through the nasal cavity of rat. The in vivo nasal infusion studies were performed using Wistar rats and the amount of DLX permeated and its amount in brain and blood was estimated. The effects on absorption rate and type of drug delivery systems (nanocarriers and drug solution) for nose to brain/blood permeation were assessed.

Preparation, characterization, in vivo biodistribution and pharmacokinetic studies of donepezil-loaded PLGA nanoparticles for brain targeting.

Objective: Alzheimer's disease (AD) is a progressive neurodegenerative disorder manifested by cognitive, memory deterioration and variety of neuropsychiatric symptoms. Donepezil is a reversible cholinesterase inhibitor used for the treatment of AD. The purpose of this work is to prepare a nanoparticulate drug delivery system of donepezil using poly(lactic-co-glycolic acid) (PLGA) for sustained release and efficient brain targeting.

Intranasal administration of nanostructured lipid carriers containing CNS acting drug: pharmacodynamic studies and estimation in blood and brain.

The present study was aimed to investigate and compare the efficacy of duloxetine (DLX) loaded nanostructured lipid carriers (NLC) with DLX solution pharmacodynamically following intranasal administration. The study was further conducted to estimate DLX concentration in brain and blood. DLX was administered to albino Wistar rats either intranasally or orally in solution form (DLX solution) or encapsulated in NLC (DLX-NLC).

Development and validation of a stability-indicating method for determination of free sterols in the Asian medicinal leech Hirudo manillensis.

A rapid, simple, sensitive, selective, precise and robust thin-layer chromatography densitometric method for the determination of free sterols in leech was developed and validated on silica gel layer using carbon tetrachloride-methanol-formic acid (9.5:1.5:0.

Reduced bioavailability of tamoxifen and its metabolite 4-hydroxytamoxifen after oral administration with biochanin A (an isoflavone) in rats.

The aim of this study was to investigate the effect of biochanin A (BCA) on the pharmacokinetics of tamoxifen, a substrate of P-glycoprotein (P-gp) and cytochrome 3A (CYP3A), in female rats. The tamoxifen was administered orally (10 mg/kg) without or with oral BCA (100 mg/kg) in female rats. As BCA is an inhibitor of CYP 3A and P-gp it was expected to increase the bioavailability of tamoxifen, a known substrate of CYP3A4/Pgp.

Reassessing bioavailability of silymarin.

Silymarin, a flavonolignan derived from Silybum marianum, possesses diverse pharmacological activities, including hepatoprotective, antioxidant, anti-inflammatory, anticancer, and cardioprotective. Although clinical trials have shown silymarin is safe at high doses (>1500 mg/day) in humans, the pharmacokinetic studies over the past three decades related to absorption, distribution, metabolism, and excretion of silymarin have revealed poor absorption, rapid metabolism, and ultimately poor oral bioavailability. For optimum silymarin bioavailability, issues of solubility, permeability, metabolism, and excretion must be addressed.

Liquid chromatography-mass spectrometry method for the quantification of tamoxifen and its metabolite 4-hydroxytamoxifen in rat plasma: application to interaction study with biochanin A (an isoflavone).

Tamoxifen is the agent of choice for the treatment of estrogen receptor-positive breast cancer. Tamoxifen is a substrate of P-glycoprotein (P-gp) and microsomal cytochrome P450 (CYP) 3A, and biochanin A (BCA) is an inhibitor of P-gp and CYP3A. Hence, it could be expected that BCA would affect the pharmacokinetics of tamoxifen.

High-throughput quantification of isoflavones, biochanin A and genistein, and their conjugates in female rat plasma using LC-ESI-MS/MS: Application in pharmacokinetic study.

Isoflavones containing foods and dietary supplements are widely consumed for putative health benefits (e.g. cancer chemoprevention, beneficial effects on serum lipids associated with cardiovascular health, reduction of osteoporosis, relief of menopausal symptoms).

Nanocarrier for the enhanced bioavailability of a cardiovascular agent: in vitro, pharmacodynamic, pharmacokinetic and stability assessment.

The goals of the current study were to develop and characterize a nanoemulsion of ezetimibe, evaluate its stability, lipid lowering and pharmacokinetic profile. Solubility of the drug was estimated in various oils and surfactants. Existence of nanoemulsion region was confirmed by plotting phase diagrams.

Solid dispersion as an approach for bioavailability enhancement of poorly water-soluble drug ritonavir.

Ritonavir is an antiretroviral drug characterized by low solubility and high permeability which corresponds to BCS class II drug. The purpose of the study was to develop solid dispersion by different methods and investigate them for in vitro and in vivo performance for enhancing dissolution and bioavailability, respectively. Since the drug possesses food-related absorption, the effect of biorelevant media (FaSSIF and FeSSIF state) on dissolution behavior was also studied.

Patented bioavailability enhancement techniques of silymarin.

The present article dwells in reviewing critically the patents published mainly on the new emerging trends and techniques for increasing the bioavailability of silymarin, the polyphenolic fraction obtained from the seeds of Silybum marianum. The use of this herb for treating various ailments like hepatitis, cirrhosis, jaundice, mushroom and toxin poisoning is well known. But the potential use of this herbal drug is limited due to the poor absorption and poor bioavailability after oral administration The belief that the natural medicines are much safer than synthetic drugs, has gained popularity in recent years and led to tremendous growth of phytopharmaceutical usage and thus the need of improving the bioavailability by various means like complexation, derivatization, solubilization, targeted delivery, controlled delivery and many other miscellaneous techniques.

Development and evaluation of novel buccoadhesive wafers of nimodipine for treatment of hypertension.

Buccoadhesive wafers (BW) containing Nimodipine (N) were prepared using the solvent casting method. Chitosan lactate was used as the mucoadhesive polymer with different ratios to PVP K-30 in preparation of the sustained release layer. Sodium carboxymethyl cellulose low viscosity (SCMC LV) in different ratios with Eudragit-RS30D was used in preparation of the immediate release layer of (BW).

Novel nanoemulsion for minimizing variations in bioavailability of ezetimibe.

The objectives of the present study were to develop an optimal nanoemulsion of ezetimibe and evaluate its stability, lipid lowering and pharmacokinetic potential. Solubility of ezetimibe was determined in various vehicles. Pseudoternary phase diagrams were constructed to determine the existence of nanoemulsion region.

Study of surfactant combinations and development of a novel nanoemulsion for minimising variations in bioavailability of ezetimibe.

The present study aimed at developing an optimal nanoemulsion of ezetimibe and evaluating its stability, pharmacodynamic and pharmacokinetic potential. Solubility of ezetimibe was determined in various vehicles. Surfactants and cosurfactants were grouped in two different combinations to construct pseudoternary phase diagrams.

Chemical permeation enhancers for transbuccal drug delivery.

Importance Of The Field: The buccal drug delivery system has been accepted as a potential non-invasive route of drug administration, with the advantages of avoidance of the first-pass metabolism, sustained therapeutic action and better patient compliance. However, transmucosal delivery of drugs by means of the buccal route is still very challenging. The main obstacles derive from the limited absorption area and from the barrier properties of the mucosa that have to be overcome for successful delivery drug molecules to the systemic circulation by this route.

Novel buccal adhesive system for anti-hypertensive agent nimodipine.

Novel buccal adhesive system (NBAS) containing Nimodipine (N) was prepared and evaluated by different parameters such as weight uniformity, thickness, hardness, surface pH, swelling index, mucoadhesive strength (MS), in vitro drug release and ex vivo drug permeation. Different formulations containing 5-20% Carbopol 934 (CP) and SCMC HV in sustained release part and sodium alginate:chitosan lactate in different ratios (1:1, 2:1, 1:2, and 3:1) in fast release part were prepared and tested. NBAS containing CP 5% and SCMC HV and sodium alginate: chitosan lactate 1:1 was selected as a suitable formula based on the (MS) and the release profile.

Development and evaluation of buccal bioadhesive tablet of an anti-emetic agent ondansetron.

The aim of the present study was to develop and evaluate a buccal adhesive tablet containing ondansetron hydrochloride (OH). Special punches and dies were fabricated and used while preparing buccal adhesive tablets. The tablets were prepared using carbopol (CP 934), sodium alginate, sodium carboxymethylcellulose low viscosity (SCMC LV), and hydroxypropylmethylcellulose (HPMC 15cps) as mucoadhsive polymers to impart mucoadhesion and ethyl cellulose to act as an impermeable backing layer.