Development and characterization of nanosuspensions of olmesartan medoxomil for bioavailability enhancement

Thakkar, Hetal; Patel, Bindesh Vishnubhai; Thakkar, Sneha Piyush

doi:10.4103/0975-7406.84459

Cited by 77 publications

(40 citation statements)

References 19 publications

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“…The obtained image indicates that the prepared drug nanosuspension particles were homogenous, almost spherical in shape, and no aggregation was noticed. This finding is in good agreement with the work done by Thakkar et al 29 for Olmesartan medoxomil nanosuspension. The size of the particles obtained by the TEM image seems to be smaller than that of the dynamic light scattering due to dilution of the sample and proper dispersion of the particles before the sample has been mounted on a carbon-coated grid, the effect that prevents NP aggregation.…”

Section: Optimum Desirabilitysupporting

confidence: 93%

Preparation of finasteride capsules-loaded drug nanoparticles: formulation, optimization, in vitro, and pharmacokinetic evaluation

Ahmed¹

2016

IJN

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In this study, optimized freeze-dried finasteride nanoparticles (NPs) were prepared from drug nanosuspension formulation that was developed using the bottom–up technique. The effects of four formulation and processing variables that affect the particle size and solubility enhancement of the NPs were explored using the response surface optimization design. The optimized formulation was morphologically characterized using transmission electron microscopy (TEM). Physicochemical interaction among the studied components was investigated. Crystalline change was investigated using X-ray powder diffraction (XRPD). Crystal growth of the freeze-dried NPs was compared to the corresponding aqueous drug nanosuspension. Freeze-dried NPs formulation was subsequently loaded into hard gelatin capsules that were examined for in vitro dissolution and pharmacokinetic behavior. Results revealed that in most of the studied variables, some of the quadratic and interaction effects had a significant effect on the studied responses. TEM image illustrated homogeneity and shape of the prepared NPs. No interaction among components was noticed. XRPD confirmed crystalline state change in the optimized NPs. An enhancement in the dissolution rate of more than 2.5 times from capsules filled with optimum drug NPs, when compared to capsules filled with pure drug, was obtained. Crystal growth, due to Ostwald ripening phenomenon and positive Gibbs free energy, was reduced following lyophilization of the nanosuspension formulation. Pharmacokinetic parameters from drug NPs were superior to that of pure drug and drug microparticles. In conclusion, freeze-dried NPs based on drug nanosuspension formulation is a successful technique in enhancing stability, solubility, and in vitro dissolution of poorly water-soluble drugs with possible impact on the drug bioavailability.

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Section: Optimum Desirabilitysupporting

confidence: 93%

Preparation of finasteride capsules-loaded drug nanoparticles: formulation, optimization, in vitro, and pharmacokinetic evaluation

Ahmed¹

2016

IJN

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“…[9,10] The unabsorbed drug may cause gastrointestinal side effects such as abdominal pain, dyspepsia, gastroenteritis, and nausea. [11] In the literature nanoparticles, [12] nanosuspension [10] and complexation with cyclodextrin [11] have been reported to improve solubility of OLM. Therefore, formulation approaches are being explored to enhance dissolution of OLM using poloxamer 407.…”

Section: Original Articlementioning

confidence: 99%

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Mali

2017

AJP

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Aim: Olmesartan medoxomil (OLM) is a poorly soluble drug and its low aqueous solubility leads to poor dissolution and bioavailability. The aim of this work was to improve the solubility of poorly aqueous soluble drug OLM by solid dispersion (SD) technique. Materials and Methods: A phase solubility study was performed to determine the effect of various polymers on aqueous solubility of drug. The binary SD of OLM was prepared by using poloxamer 407. The SDs were prepared by kneading, melting and solvent evaporation (SE) method by varying drug to carrier ratio. The optimized SD formulations were characterized by Fourier transform infrared (FTIR) spectroscopy, differential scanning calorimetry (DSC), scanning electron microscopy (SEM), and powder X-ray diffraction (XRD). Fast disintegrating tablets (FDTs) of OLM were formulated using optimized SD. The in vitro evaluation of FDTs was done including stability studies. Results: Phase solubility study indicated 5.3 fold increase in solubility of OLM by Poloxamer 407. The results of FTIR, DSC, SEM, and XRD study showed the conversion of crystalline form of OLM to amorphous form. The results revealed that SD prepared by SE method showed rapid dissolution as compared to other methods. The FDTs of optimized SD containing croscarmellose sodium showed faster and complete in vitro drug release within 20 min. Formulation M6 was found to be optimized formulation owing to its 84.09 dissolution efficiency, 4.82 min mean dissolution time and 100% drug release. Optimized formulation was found to be stable for 3-month period. Conclusion: The results conclusively confirmed successful improvement in dissolution of poorly water-soluble drug OLM.

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“…The grid was then mounted in the instrument and photographs were taken at different magnifications. 32 In addition, the surface characteristics of the optimized lyophilized nanosuspension were observed using a scanning electron microscope (JXA-840; JEOL, Tokyo, Japan). The samples were gold-coated under vacuum and then examined.…”

Section: Morphology and Surface Characteristics Of Optimized Nanosuspmentioning

confidence: 99%

Preparation, optimization, and in vitro simulated inhalation delivery of carvedilol nanoparticles loaded on a coarse carrier intended for pulmonary administration

Abdelbary¹,

Al-mahallawi²,

Abdelrahim³

et al. 2015

IJN

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Carvedilol (CAR) is a potent antihypertensive drug but has poor oral bioavailability (24%). A nanosuspension suitable for pulmonary delivery to enhance bioavailability and bypass first-pass metabolism of CAR could be advantageous. Accordingly, the aim of this work was to prepare CAR nanosuspensions and to use artificial neural networks associated with genetic algorithm to model and optimize the formulations. The optimized nanosuspension was lyophilized to obtain dry powder suitable for inhalation. However, respirable particles must have a diameter of 1–5 µm in order to deposit in the lungs. Hence, mannitol was used during lyophilization for cryoprotection and to act as a coarse carrier for nanoparticles in order to deliver them into their desired destination. The bottom-up technique was adopted for nanosuspension formulation using Pluronic stabilizers (F127, F68, and P123) combined with sodium deoxycholate at 1:1 weight ratio, at three levels with two drug loads and two aqueous to organic phase volume ratios. The drug crystallinity was studied using differential scanning calorimetry and powder X-ray diffractometry. The in vitro emitted doses of CAR were evaluated using a dry powder inhaler sampling apparatus and the aerodynamic characteristics were evaluated using an Andersen MKII cascade impactor. The artificial neural networks results showed that Pluronic F127 was the optimum stabilizer based on the desired particle size, polydispersity index, and zeta potential. Results of differential scanning calorimetry combined with powder X-ray diffractometry showed that CAR crystallinity was observed in the lyophilized nanosuspension. The aerodynamic characteristics of the optimized lyophilized nanosuspension demonstrated significantly higher percentage of total emitted dose (89.70%) and smaller mass median aerodynamic diameter (2.80 µm) compared with coarse drug powder (73.60% and 4.20 µm, respectively). In summary, the above strategy confirmed the applicability of formulating CAR in the form of nanoparticles loaded on a coarse carrier suitable for inhalation delivery.

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Development and characterization of nanosuspensions of olmesartan medoxomil for bioavailability enhancement

Cited by 77 publications

References 19 publications

Preparation of finasteride capsules-loaded drug nanoparticles: formulation, optimization, in vitro, and pharmacokinetic evaluation

Preparation of finasteride capsules-loaded drug nanoparticles: formulation, optimization, in vitro, and pharmacokinetic evaluation

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Preparation, optimization, and in vitro simulated inhalation delivery of carvedilol nanoparticles loaded on a coarse carrier intended for pulmonary administration

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