Solid-Nanoemulsion Preconcentrate for Oral Delivery of Paclitaxel: Formulation Design, Biodistribution, and<i>γ</i>Scintigraphy Imaging

Ahmad, Javed; Mir, Showkat R.; Kohli, Kanchan; Chuttani, Krishna; Mishra, Anil K.; Panda, Amulya K.; Amin, Saima

doi:10.1155/2014/984756

Cited by 61 publications

(35 citation statements)

References 37 publications

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“…The existence of high negative charge on the prepared NE formulations could be due to the presence of anionic groups of fatty acids in the cinnamon oil, tween 80, glycol part of poloxamer and alcohol moiety of transcutol HP (Ahmad et al 2014).…”

Section: Zeta Potential Measurementmentioning

confidence: 99%

Oral nanoemulsions of candesartan cilexetil: formulation, characterization and in vitro drug release studies

Ali

Hussein

2017

AAPS Open

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Nanoemulsion is considered to be a new and exciting field of research that seeks to exploit the attractive properties of components to improve oral delivery of drugs like candesartan cilexetil used in the management of chronic diseases. Candesartan cilexetil is a lipophilic acidic drug with a half-life of about (5-10) hour and absolute bioavailability of (14-40%). For this reason, the study target was to formulate and characterize candesartan cilexetil nanoemulsions that could improve solubility, dissolution and stability of the lipophilic drug candesartan cilexetil. The solubility of candesartan cilexetil was checked in various vehicles in order to choose the best solubilizing components for building up an efficient nanoemulsion based on regulating hydrophilic/lipophilic balance (HLB) value above 10, and then pseudo-ternary phase diagram was used as a useful tool to evaluate the nanoemulsion domain. The nanoemulsion formulations were prepared using various concentrations of cinnamon oil, tween 80 with poloxamer mixture and transcutol HP as oil, surfactant mixture and co-surfactant respectively by aqueous titration method at surfactant/co-surfactant ratios of 3:1 and 4:1 and varying the type of poloxamer in each ratio. The prepared nanoemulsions were tested for nanodispersion stability studies, droplet size distribution, polydispersity index, zeta potential, viscosity, filter paper spreadability, dye miscibility, electroconductivity, pH, percent transmittance, surface tension, refractive index, morphology and drug dissolution. It was found that release rate and extent for all prepared nanoformulations were significantly higher (p < 0.05) than marketed tablet formulation as well as plain drug powder. The results demonstrated that, the potential use of this system is a perfect technique for improving solubility and dissolution of candesartan cilexetil.

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Section: Zeta Potential Measurementmentioning

confidence: 99%

Oral nanoemulsions of candesartan cilexetil: formulation, characterization and in vitro drug release studies

Ali

Hussein

2017

AAPS Open

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“…This could be explained by the fact that higher amount of surfactant (tween 80 with poloxamer 407 mixture) raise the numbers of the hydroxyl group of fatty acid and glycol of tween 80 and poloxamer 407, respectively which further elevate CC SNEDDSs negativity (Ahmad et al 2014). …”

Section: Measurement Of Surface Chargementioning

confidence: 99%

Oral solid self-nanoemulsifying drug delivery systems of candesartan citexetil: formulation, characterization and in vitro drug release studies

Ali

Hussein

2017

AAPS Open

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Candesartan cilexetil is an ester prodrug antagonist to angiotensin II receptor type 1 (AT1) used in management of many cardiovascular diseases. The absolute bioavailability of candesartan cilexetil is about (14-40%). Therefore, the paper aim was to prepare and evaluate solid self-nanoemulsifying drug delivery systems for candesartan cilexetil in order to improve its solubility, dissolution and stability. Solubility study was run in different vehicles to select the best excipients for dissolving candesartan cilexetil. Pseudo-ternary phase diagrams were constructed at 1:1, 2:1, 3:1 and 4:1 ratios and four formulations were prepared using various concentrations of cinnamon oil, tween 80 with poloxamer 407 mixture and transcutol HP as oil, surfactant mixture and co-surfactant, respectively. After this step about (0.2 milliliter) of each formulation was adsorbed on to two different adsorbent mixtures set which were: avicel 101 with aerosil 200 and avicel 101 with dibasic calcium phosphate anhydrous resulted in eight solid nanoformulations. All prepared formulations were evaluated for particle size distribution, polydispersity index, zeta potential, scanning probe microscopy, Fourier transform infrared spectroscopy, differential scanning calorimetry, X-ray powder diffractometry and in vitro drug dissolution. It was found that release rate and extent for all prepared formulations were significantly higher (p < 0.05) than marketed tablet as well as plain drug powder. It could be concluded from the study that self-nanoemulsifying drug delivery system is a promising approach to improve solubility, wettability, dissolution and stability of candesartan cilexetil.

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“…Our data supports that a lower concentration of PVA (1% w/v) is suitable to obtain well-controlled particle size formulations provided stability of dispersion is not compromised. Analysing the response surface of interactions of PLGA and ethyl acetate at constant PVA, we found that initially, with an increase of solvent volume, the particle size did not change much and then decreased with further increase in the volume of ethyl acetate (trial [13][14][15][16][17][18][19][20].…”

Section: Influence On Particle Sizementioning

confidence: 99%

“…The drug release is usually faster from the nanoparticles of lower drug entrapment efficiency [19]. The study is performed by using dialysis bag method [20].…”

Section: In Vitro Releasementioning

confidence: 99%

Polymeric Nanoparticles for Improved Bioavailability of Cilnidipine

Mishra

Mir

Amin

2017

Int J Pharm Pharm Sci

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Objective: In the present study, we aimed to optimize, characterize and evaluate poly lactic-glycolic acid nanoparticles of cilnidipine for improved permeation across the gastrointestinal tract.Methods: Poly lactic-glycolic acid-cilnidipine (PLGA-CIL) nanoparticles were prepared by an emulsification solvent evaporation/diffusion method using polyvinyl alcohol (PVA) as a surfactant. The prepared nanoparticles were successfully characterized for particle size, shape, drug release and pharmacological effect.Results: Polymeric nanoparticles of cilnidipine at a dose of 10 mg had a small particle size of 272 nm with smooth morphology. Nearly 81% of the drug was encapsulated in the polymeric structure and showed 18.99±0.59% of release at pH 1.2 within 3h, however, at pH 6.8 the release was 80.89±1.59%. The formulation had a better antihypertensive effect on methylprednisolone-induced hypertensive rats. The relative bioavailability of the nanoparticles was found to be 2.44 and 2.94 fold higher than the tablet and drug suspension respectively. Conclusion:The results demonstrated that the novel delivery system offers an effective strategy for treatment of hypertension.

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Solid-Nanoemulsion Preconcentrate for Oral Delivery of Paclitaxel: Formulation Design, Biodistribution, andγScintigraphy Imaging

Cited by 61 publications

References 37 publications

Oral nanoemulsions of candesartan cilexetil: formulation, characterization and in vitro drug release studies

Oral nanoemulsions of candesartan cilexetil: formulation, characterization and in vitro drug release studies

Oral solid self-nanoemulsifying drug delivery systems of candesartan citexetil: formulation, characterization and in vitro drug release studies

Polymeric Nanoparticles for Improved Bioavailability of Cilnidipine

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