Doxazosin Research Articles

Structure based release kinetics analysis of doxazosin mesylate sustained-release tablets using micro-computed tomography

The structures of solid dosage forms determine their release behaviors and are critical attributes for the design and evaluation of the solid dosage forms. Here, the three-dimensional (3D) structures of doxazosin mesylate sustained-release tablets (DM SRT) as reference listed drug (RLD) and a generic preparation were parallelly assessed by micro-computed tomography (micro-CT). There were no significant differences observed in the release profiles between the RLD and the generic formulation in the conventional dissolution, but the generic preparation released slightly faster in media with ethanol for an alcohol-induced dose-dumping test. With their 3D structures obtained via micro-CT determination, the unique release behaviors of both RLD and the generic were investigated for samples from dissolution tests to reveal the effects of internal fine structure on the release kinetics. The structural parameters for both preparations were similar in conventional dissolution test, whilst the dissolutions in ethanol media of RLD were more or less distinguished from that of generic preparations, attributing to their static and dynamic structures. Furthermore, the findings revealed that the presence of ethanol accelerated the dissolution and induced changes in the internal structure of both the RLD and the generic preparations. Moreover, the structure parameters like volume and area of outer contour, remaining solid volume and cavity volume were not equivalent between the two formulations in 40 % ethanol. In conclusion, the structure data obtained from this study provided valuable insights into the diverse release behaviors observed in various modified-release formulations in drug development and quality control.

Sustained release microneedle patch for pronounced systemic delivery of doxazosin mesylate

Introduction: Microneedle patch is one of the fascinating drug delivery approaches that offers low invasiveness and a painless physical application to enhance the delivery of micro and macro-molecules into the skin. Methods: Variable contents of chitosan and polyvinyl alcohol were used for the development of doxazosin mesylate containing sustained release microneedle patches via solvent casting technique. The prepared patches were evaluated for microscopic evaluation, mechanical strength, drug loading (%) and Fourier transform infrared spectroscopy (FTIR) etc. The skin penetration study was performed by using pig ear skin and results were captured through confocal microscopy. Ex-vivo release study and pharmacokinetic evaluation were also performed. Results: Sharp needle tips with a height of 600µm and a base of 200µm were confirmed through microscopic examination. Optimized formulation (SRF-6) exhibited loading of 92.11% doxazosin mesylate with appreciable strength up to 1.94N force. Ex-vivo release studies revealed 87.24% release within 48 hours. Moreover, the pharmacokinetic parameters in case of optimized patch formulation (SRF-6) were markedly improved i.e. MRT (19.46 h), AUC (57.12 μg.h /mL), Cmax (2.16 µg /mL), tmax (10.10 h) and t1/2 (6.32 h) as compared to commercially available tablet. Biocompatibility of the developed patches was validated from skin irritation studies. Conclusion: Results confirmed the successful fabrication of microneedle patch having sufficient strength and effective penetration ability into the skin to ensure controlled release of incorporated drug for the intended duration. It can be employed as an efficient carrier system for other therapeutics those are prone to bioavailability issues due to first pass effect after their oral administration.

Suppression of TNBC metastasis by doxazosin, a novel dual inhibitor of c-MET/EGFR

BackgroundTriple-negative breast cancer (TNBC) is characterized by aggressive growth and a high propensity for recurrence and metastasis. Simultaneous overexpression of c-MET and EGFR in TNBC is associated with worse clinicopathological features and unfavorable outcomes. Although the development of new c-MET inhibitors and the emergence of 3rd-generation EGFR inhibitors represent promising treatment options, the high costs involved limit the accessibility of these drugs. In the present study, we sought to investigate the therapeutic potential of doxazosin (DOXA), a generic drug for benign prostate hyperplasia, in targeting TNBC.MethodsThe effect of DOXA on TNBC cell lines in vitro was evaluated in terms of cell viability, apoptosis, c-MET/EGFR signaling pathway, molecular docking studies and impact on cancer stem cell (CSC)-like properties. An in vivo metastatic model with CSCs was used to evaluate the efficacy of DOXA.ResultsDOXA exhibits notable anti-proliferative effects on TNBC cells by inducing apoptosis via caspase activation. Molecular docking studies revealed the direct interaction of DOXA with the tyrosine kinase domains of c-MET and EGFR. Consequently, DOXA disrupts important survival pathways including AKT, MEK/ERK, and JAK/STAT3, while suppressing CSC-like characteristics including CD44high/CD24low subpopulations, aldehyde dehydrogenase 1 (ALDH1) activity and formation of mammospheres. DOXA administration was found to suppress tumor growth, intra- and peri-tumoral angiogenesis and distant metastasis in an orthotopic allograft model with CSC-enriched populations. Furthermore, no toxic effects of DOXA were observed in hepatic or renal function.ConclusionsOur findings highlight the potential of DOXA as a therapeutic option for metastatic TNBC, warranting further investigation.

Oral bioavailability enhancement of doxazosin mesylate: Nanosuspension versus self-nanoemulsifying drug delivery systems.

Doxazosin mesylate (DOX) is an antihypertensive drug that possesses poor water solubility and, hence, poor release properties. Both nanosuspensions and self-nanoemulsifying drug delivery systems (SNEDDS) are becoming nanotechnology techniques for the enhancement of water solubility of different drugs. The study's goal was to identify the best drug delivery system able to enhance the release and antihypertensive effect of DOX by comparing the physical characteristics such as particle size, zeta potential, entrapment efficiency, release rate, and main arterial blood pressure of DOX-loaded nanosuspensions and SNEDDS in liquid and solid form. DOX nanosuspension preparation had a particle size of 385±13 nm, poly-dispersity index of 0.049±3, zeta potential of 50 ± 4 mV and drug release after 20 min (91±0.43 %). Liquid SNEDDS had a droplet size of 224±15 nm, poly-dispersity index of (0.470±0.01), zeta potential of -5±0.10 mV and DR20min of 93±4 %. Solid SEDDS showed particle size of 79±14 nm, poly-dispersity index of 1±0.00, a zeta potential of -18 ±0.26 mv and DR20min of 100 ±2.72 %. Finally, in terms of the mean arterial blood pressure lowering, solid SNEDDS performed better effect than both liquid SNEDDS and nanosuspension (P >0.05).

Autophagy induction using Resveratrol enhances the anti-cancer efficacy of Doxazosin in breast cancer cells.

The combination of anti-cancer drugs improves effectiveness compared to the mono-therapy scenario by targeting key pathways synergistically or in an additive way. Doxazosin (DOX) and Resveratrol (RES) are reported to have an anti-cancer impact against different cancer cells. Aim: To evaluate the anti-cancer properties of Doxazosin and Resveratrol, each alone or in combination, in inhibiting breast cancer cell proliferation. Methods: MCF-7 cancer cells were seeded to a confluent monolayer and treated with 100, 50, 25, 12.5, 6.25, and 3.12 µM of each drug alone and as a combination. Cytotoxicity was evaluated using dimethyl thiazolyl diphenyl tetrazolium salt (MTT) assay and colony formation assay. The immunocytochemistry technique was conducted to evaluate caspase-3 and GABARAP expression. Results: All the drugs have a significant effect on cancer cell proliferation. The combination treatment of Doxazosin-Resveratrol has a more cytotoxic effect than each drug alone, as well as in colony formation of MCF-7 cancer cells. In combination treatment, caspase-3 had a higher expression pattern than other treatments. Resveratrol treatment elevated GABARAP expression in cancer cells, indicating the induction of the autophagy process. Conclusion: Although each drug has its characteristic result of a cytotoxic effect, the combination of Doxazosin and Resveratrol synergizes the inhibition of MCF-7 cancer cell proliferation. Keywords: Resveratrol; Doxazosin; combination; MCF-7; Autophagy.

Development of Doxazosin mesylate liquisolid system for improved manufacturing processability and bioavailability: in vitro and in vivo evaluation for tailored hypertension treatment approach with modified dissolution rates

In the present research, an attempt was made to optimize the blends of different carriers Neusiln US2, Avicel PH101, and Fujicalin SG by individually blending with each of coating materials Aerosil 200 and Syloid 244 FP that were proposed to contribute to a modified drug dissolution rates of Doxazosin mesylate (DX) through a liquisolid polymer matrix system. The liquisolid formulations were prepared using selected solvent, carriers, and coats by varying drug to polymer ratios. Further formulations were investigated for pre-compression processability by Heckel plot analysis, elastic recovery studies, and post-compression characteristics. In case of carriers, compared to Avicel PH101 highest flowable values (ф) were observed for Neusilin US2 and Fujicalin SG whereas, for coat these values were highest for Aerosil 200 than Sylloid 244 FP. Liquisolid compact with Fujicalin SG and Aerosil 200 exhibited fast release (FR) of 78% in 20 minutes. The liquisolid compact with Neusilin US2 and Syloid 244 FP exhibited prolonged release (PR) of 60% in 240 minutes. DSC and XRD analysis showed loss of DX crystallinity which was confirmed by SEM analysis indicating DX detention within the liquisolid system, in a molecularly dispersed solubilized form. The in vivo studies of DX liquisolid FR formulation exhibited 1.89 fold increase in the oral bioavailability which was 1.69 fold for DX PR formulation compared to pure DX which demonstrated a promising tailored hypertension treatment approach.

Mechanical, optical, and physicochemical properties of HPMC-based doxazosin mesylate orodispersible films

In this study, orodispersible films formed from hydroxypropyl methylcellulose (HPMC) E6 (2, 2.5, and 3%) and plasticizers ((glycerin (Gly), propylene glycol (PP), or polyethylene glycol (PEG)), containing doxazosin mesylate, were prepared by the solvent casting method and characterized. Design of experiments (DoE) was used as a statistical tool to facilitate the interpretation of the experimental data and allow the identification of optimal levels of factors for maximum formulation performance. Differential scanning calorimetry (DSC) curves and X-ray powder diffraction (XRPD) diffractograms showed doxazosin mesylate amorphization, probably due to complexation with the polymer (HPMC E6), and the glass transition temperature of the polymer was reduced by adding a plasticizer. Fourier transformed infrared (FTIR) spectroscopy results showed that the chemical structure of doxazosin mesylate was preserved when introduced into the polymer matrix, and the plasticizers, glycerin and PEG, affected the polymer matrix with high intensity. The addition of plasticizers increased the elongation at break and adhesiveness (Gly > PEG > PP), confirming the greater plasticizer effect of Gly observed in DSC and FTIR studies. Greater transparency was observed for the orodispersible films prepared using PP. The addition of citric acid as a pH modifier was fundamental for the release of doxazosin mesylate, and the desirability formulation had a release profile similar to that of the reference product.

Radiation-induced degradation of doxazosin: Role of reactive species, toxicity, mineralization and degradation pathways

State-of-the-art technologies based on advanced oxidation processes (AOPs) are currently being developed for the removal of environmental pollutants such as pharmaceuticals from water matrices. Such studies are very important and should include the impact of inorganic and organic matrix on the degradation process of pollutants. One of the AOPs that is in focus of investigations nowadays, is ionizing radiation. Doxazosin (DOX) is a widely used pharmaceutical for the treatment of hypertension, which can be potentially harmful due to its occurrence in the aquatic environment. This study reports the radiation-induced degradation of DOX in aqueous solution. Removal of 10 mg L−1 DOX reached almost 100 % at irradiation doses of 200 Gy regardless of the dose rate used. The effect of saturated solutions with N2, N2O, air and the addition of radical scavengers such as 2-PrOH and thiourea on DOX degradation was investigated. The efficiency of degradation increased in the order: thiourea < 2-PrOH < N2 < air < N2O. The effects of pH, various inorganic ions and water matrix on DOX degradation were also studied. DOX degradation was lower in underground water than in ultrapure water. Under prolonged irradiation, mineralization of about 60 % of DOX solutions was observed based on the dissolved organic carbon (DOC) evaluation. Toxicity tests with V. fischeri luminescent bacteria showed higher toxicity of samples irradiated at 500 Gy. The main degradation products were identified using LC-HRMS and degradation pathways were proposed. Overall, irradiation technology could be a promising technique for the removal of micropollutants, such as pharmaceuticals in real water matrices.

Determination of antihypertensive drugs irbesartan and doxazosin mesylate in healthcare products and urine samples using surface-enhanced Raman scattering.

In this paper, a surface-enhanced Raman scattering (SERS) strategy was constructed for the determination of antihypertensive drugs irbesartan (IRB) and doxazosin mesylate (DOX). β-Cyclodextrin-capped silver nanoparticles (CD-AgNPs) are employed as SERS-active substrate. The introduction of β-CD with hydrophobic cavity can capture drug molecules to form host-guest complex, making the drug molecules closer to the electromagnetic enhancement field of the AgNPs, thereby enhancing the SERS signal of drug molecules with low Raman cross-section. The vibrational modes of IRB and DOX are assigned by density functional theory calculations. The linear response from 3.0 × 10-7 to 1.0 × 10-5mol L-1 for IRB and 3.0 × 10-7 to 2.0 × 10-5mol L-1 for DOX and low limits of detection (LOD) 7.5 × 10-8mol L-1 for IRB and 8.6 × 10-8mol L-1 for DOX can be achieved. Meanwhile, this SERS approach can be applicable to determine IRB and DOX in commercial drug tablets, healthcare products, and human urine samples with recoveries of 90.8-115.7% and 90.0-113.5%, respectively, with relative standard deviation (RSD) less than 4.5%. This designed SERS strategy enables for the rapid determination of IRB and DOX in drug quality monitoring and illegal additives in healthcare products as well as clinical applications.

Preparation and evaluation of the doxazosin-bentonite composite as a pH-dependent controlled-release oral formulation

Bentonite (BT) is a natural clay mainly composed of montmorillonite which has exchangeable cations in the interlayer space. BT has various advantages as a pharmaceutical excipient for the formulation of drug delivery systems (DDSs), including biocompatibility and unique physicochemical properties (i.e., adsorption and pH-dependent cation exchange). However, previous studies on the application of BT for DDSs were usually limited to the characterization of the in vitro adsorption and release properties. Herein, we prepared and characterized a doxazosin-bentonite (DXBT) composite formulation for controlled oral delivery and then evaluated the pharmacokinetics of doxazosin (DX) in rats. The composition of the DXBT composite was optimized based on the adsorption efficiency and the content of DX in the DXBT composite. The change in morphology was observed by scanning electron microscopy (SEM). Intercalation of amorphous DX between the BT interlayer space was confirmed by powder X-ray diffraction (pXRD). The zeta potential of DXBT composite was higher than BT over the pH range between 1 and 8, and was positive in acidic condition and was changed to negative at pH above 4. The DXBT composite showed pH-dependent in vitro release profiles of DX, and the cumulative release amount at 24 h was higher at pH 7.8 than at pH 1.2 and 7.4 (63.9, 29.3 and 47.8%, respectively). In an in vivo pharmacokinetic study after oral administration in rats, the DXBT composite resulted in a significantly lower peak plasma concentration (Cmax) and longer terminal half-life (t1/2) and mean residence time (MRT) of DX compared to DX solution. Thus, the DXBT composite could be an oral drug delivery platform with pH-dependent controlled-release profiles based on the unique ion-exchange property of BT.

Epinephrine evokes shortening of human airway smooth muscle cells following β2 adrenergic receptor desensitization.

Epinephrine (EPI), an endogenous catecholamine involved in the body’s fight-or-flight responses to stress, activates α1-adrenergic receptors (α1ARs) expressed on various organs to evoke a wide range of physiological functions, including vasoconstriction. In the smooth muscle of human bronchi, however, the functional role of EPI on α1ARs remains controversial. Classically, evidence suggests that EPI promotes bronchodilation by stimulating β2-adrenergic receptors (β2ARs). Conventionally, the selective β2AR agonism of EPI was thought to be, in part, due to a predominance of β2ARs and/or a sparse, or lack of α1AR activity in human airway smooth muscle (HASM) cells. Surprisingly, we find that HASM cells express a high abundance of ADRA1B (the α1AR subtype B) and identify a spontaneous “switch-like” activation of α1ARs that evokes intracellular calcium, myosin light chain phosphorylation, and HASM cell shortening. The switch-like responses, and related EPI-induced biochemical and mechanical signals, emerged upon pharmacological inhibition of β2ARs and/or under experimental conditions that induce β2AR tachyphylaxis. EPI-induced procontractile effects were abrogated by an α1AR antagonist, doxazosin mesylate (DM). These data collectively uncover a previously unrecognized feed-forward mechanism driving bronchospasm via two distinct classes of G protein-coupled receptors (GPCRs) and provide a basis for reexamining α1AR inhibition for the management of stress/exercise-induced asthma and/or β2-agonist insensitivity in patients with difficult-to-control, disease subtypes.

Development and Validation of UV Spectrophotometric Method for Doxazosin Mesylate in Bulk and Tablets

Doxazosin mesylate (DX) is an antihypertensive agent belonging to BCS class II. There is no reported literature available on development of spectrophotometric method for its analysis in bulk and pharmaceutical dosage forms using 0.1N HCl. Thus, attempt was made to develop and validate a new UV spectrophotometric method using 0.1N HCl as the solvent for its quantitative estimation in tablets that would be fast, simple, accurate, and sensitive. DX had a maximum absorbance wavelength of 245 nm and was linear with a correlation coefficient (R2) of 0.9981 across the concentration range of 2-14 μg/mL. The present method was utilized to determine the drug content of two commercial brands namely; brand I and brand II. The estimated amount of DX was 99.13% and 99.02% in these brands, respectively. The proposed method generated results that confirm the label claim and was accurate, precise, sensitive, and rugged during its validation study. The accuracy of the technique was tested using recovery research at three different levels, namely 80%, 100%, 120%, and the percent recovery rate was determined between 98% and 102% suggesting that the proposed approach is accurate. Precision and robustness were within the acceptable limits, complying with ICH standards. The proposed method could be used to quantify DX in API and dosage forms.

Thoracoscopic resection of posterior mediastinal paraganglioma: perioperative management and surgical tips

Posterior mediastinal paraganglioma (PM-PGL) is a rare disease that is difficult to diagnose. If PM-PGL is misdiagnosed preoperatively, surgeons may encounter severe tachycardia and hypertension and easy bleeding from the tumor during the operation. Therefore, it is essential to include PGL as a differential diagnosis for mediastinal tumors. We herein describe a 73-year-old Japanese man with a PM-PGL that was diagnosed preoperatively and resected safely by video-assisted thoracic surgery. Preoperative management of hypertension with doxazosin mesylate, soft coagulation of the peritumor area, and careful clipping of feeding arteries were effective for hemostasis. The patient’s vital signs were stable during and after the operation.

Elucidating a Complicated Enantioselective Metabolic Profile: A Study From Rats to Humans Using Optically Pure Doxazosin.

Doxazosin (DOX) is prescribed as a racemic drug for the clinical treatment of benign prostatic hyperplasia and hypertension. Recent studies found that the two enantiomers of DOX exhibit differences in blood concentration and pharmacological effects. However, the stereoselective metabolic characteristics and mechanisms for DOX are not yet clear. Herein, we identified 34 metabolites of DOX in rats based on our comprehensive and effective strategy. The relationship among the metabolites and the most discriminative metabolites between (−)-DOX and (+)-DOX administration was analyzed according to the kinetic parameters using state-of-the-art multivariate statistical methods. To elucidate the enantioselective metabolic profile in vivo and in vitro, we carefully investigated the metabolic characteristics of metabolites after optically pure isomers administration in rat plasma, rat liver microsomes (RLMs) or human liver microsomes (HLMs), and recombinant human cytochrome P450 (CYP) enzymes. As a result, the differences of these metabolites were found based on their exposure and elimination rate, and the metabolic profile of (±)-DOX was more similar to that of (+)-DOX. Though the metabolites identified in RLMs and HLMs were the same, the metabolic profiles of the metabolites from (−)-DOX and (+)-DOX were greatly different. Furthermore, four human CYP enzymes could catalyze DOX to produce metabolites, but their preferences seemed different. For example, CYP3A4 highly specifically and selectively catalyzed the formation of the specific metabolite (M22) from (−)-DOX. In conclusion, we established a comprehensive metabolic system using pure optical isomers from in vivo to in vitro, and the complicated enantioselectivity of the metabolites of DOX was clearly shown. More importantly, the comprehensive metabolic system is also suitable to investigate other chiral drugs.

α-1 Adrenergic receptor antagonist doxazosin reverses hepatic stellate cells activation via induction of senescence

BackgroundActivated hepatic stellate cells (aHSCs) are the main effector cells during liver fibrogenesis. α-1 adrenergic antagonist doxazosin (DX) was shown to be anti-fibrotic in an in vivo model of liver fibrosis (LF), but the mechanism remains to be elucidated. Recent studies suggest that reversion of LF can be achieved by inducing cellular senescence characterized by irreversible cell-cycle arrest and acquisition of the senescence-associated secretory phenotype (SASP). AimTo elucidate the mechanism of the anti-fibrotic effect of DX and determine whether it induces senescence. MethodsPrimary culture-activated rat HSCs were used. mRNA and protein expression were measured by qPCR and Western blot, respectively. Cell proliferation was assessed by BrdU incorporation and xCelligence analysis. TGF-β was used for maximal HSC activation. Norepinephrine (NE), PMA and m-3M3FBS were used to activate alpha-1 adrenergic signaling. ResultsExpression of Col1α1 was significantly decreased by DX (10 μmol/L) at mRNA (−30 %) and protein level (−50 %) in TGF-β treated aHSCs. DX significantly reduced aHSCs proliferation and increased expression of senescence and SASP markers. PMA and m-3M3FBS reversed the effect of DX on senescence markers. ConclusionDoxazosin reverses the fibrogenic phenotype of aHSCs and induces the senescence phenotype.

New Approach for Administration of Doxazosin Mesylate: Comparative Study between Liquid and Solid Self-nanoemulsifying Drug Delivery Systems

Self-nanoemulsifying drug delivery systems (SNEDDS) in both liquid and solid forms were suggested to improve water solubility of Doxazosin mesylate (DOX) a poorly water- soluble antihypertensive drug. Oleic acid: Smix (1:9 w/w) and Tween 80: co-surfactant mixture (Ethanol and PEG 400) (1:1, 2:1, 3:1 and 4:1) were chosen to prepare a liquid and solid forms of SNEDDS according to their solubility. TEM images revealed change in the crystalline nature of DOX into uniform particles with smooth surface. Characterization studies revealed droplet size ranges from 79.80±14.39 to 273.10±4.17 nm, zeta potential ranges from -5.57±0.10 to -21.13±0.46 mV and dissolution enhancement of more than two folds with more favorable properties for the solid forms. FTIR demonstrated significant physical changes in DOX crystalline structure. In conclusion, the solid SNEDDS containing oleic acid: Smix (1:9 w/w) and Tween 80: co-surfactant mixture (3:1 w/w) and adsorbent mixture of Avicel 101 and Aerosil 200 (40:1 w/w) might be a promising formula for better management of hypertension with expected shelf stability.

Improved Hypertension by Investigating Circadian Rhythm of Blood Pressure

Case: The case is 86-year-old male hypertensive patient with anti-hypertensive drug for 5 years. He has been provided Amlodipine besilate 5mg at 0800h and doxazosin mesylate 2mg at 2300h for long. In June 2020, he noticed unstable fluctuation of Blood Pressure (BP) during morning, afternoon and night. Results: Then, he checked the circadian rhythm of BP, which showed higher BP in early morning, decreasing BP 0800-1000h, minimum BP during 1000-1400h, increasing BP during 1400-1800h and stable BP during 1800-2400h. Due to the result, he changed to take amlodipine at 2300h. Consequently, his BP gradually became stable during 24 hours after 2 weeks. Discussion: Some factors may exist for contributing improved BP fluctuation. They include a) pathophysiological characteristics of BP circadian rhythm, b) effective time for anti-hypertensive drug, c) accuracy of the obtained BP data and d) the social and psychological reliability of the patient. Regarding d) he was engaged in research and development work as a senior researcher at a chemical company. He has been also a member of New Elderly Association (NEA), which was established by Shigeaki Hinohara. He lives on the philosophy of Hinohara-ism for long, associated with stable mind and body.

Spectrophotometric determination of buspirone HCl and doxazosin mesylate using citrate-capped silver nanoparticles

A simple and rapid spectrophotometric method was developed for determination of buspirone HCl and doxazosin mesylate in bulk and pharmaceutical formulations. In this paper silver nanoparticles (Ag-NPs) were prepared chemically using sodium citrate as reducing and stabilising agent. Silver nanoparticles showed an absorption band at 420 nm. Aggregation of citrate stabilised silver nanoparticles (Ag NPs) were used for quantitative determination of the studied drugs with formation of a new red shifted band at 545, 690 nm for buspirone HCl and doxazosin mesylate respectively. Different experimental factors were optimised and the calibration curves were linear with concentrations of (0.10-0.60 μg/mL), (5.0-14.0 μg/mL) for buspirone HCl and doxazosin mesylate respectively. Validation of the analytical performance of the method was carefully investigated, and the results were satisfactory.

Spectrophotometric determination of buspirone HCl and doxazosin mesylate using citrate-capped silver nanoparticles

Spectrophotometric determination of buspirone HCl and doxazosin mesylate using citrate-capped silver nanoparticles

Fast disintegrating tablet of Doxazosin Mesylate nanosuspension: Preparation and characterization

Doxazosin Mesylate (DOX) is an antihypertensive drug which possesses poor water solubility and hence low bioavailability. The study objective is to prepare DOX fast disintegrating tablets as a new dosage form for geriatric patients. First, 23 full factorial design using Polyvinyl pyrrolidone k 30, Poloxamer-407 and Sodium Lauryl Sulphate at low and high ratios were used for preparation of DOX nanosuspension as a trial to improve its dissolution properties. Nanosuspension formulations were characterized using Transmission electron microscopy, Differential scanning calorimetry and Fourier transform infrared spectroscopy. Then, the optimized formula was incorporated in fast disintegrating tablets using different superdisintegrants. The tablets were evaluated for hardness, thickness, friability percentage, diameter, weight variation, Wetting time, disintegration time and percentage dissolution after 10 min. A significant reduction (rapidly and efficiently) in mean arterial pressure of hypertensive rats was observed for DOX nanosuspension fast disintegrating tablet using Ac-Di-Sol as a superdisintegrant with 100% dissolution after 10 min.