Formulation and development of a self-nanoemulsifying drug delivery system of irbesartan

Patel, Jay; Patel, Anjali; Raval, Mihir; Sheth, Navin

doi:10.4103/2231-4040.79799

Cited by 171 publications

(79 citation statements)

References 13 publications

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“…The values of the coefficients X1, X2 and X3 are related to the effect of these variables on the response. A positive sign of coefficient indicates a synergistic effect while a negative term indicates an antagonistic effect upon the response [26,27]. The larger coefficient means the independent variable has a more potent influence on the response.…”

Section: Optimisation and Evaluation Of Olmesartan Sneddsmentioning

confidence: 99%

Design, Optimization and in Vitro Characterization of Self Nano Emulsifying Drug Delivery System of Olmesartan Medoxomil

Sisinthy

Nalamolu

Sarah

2016

Int J Pharm Pharm Sci

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Objective: The objective of the present study was to design, optimise and characterise self nano emulsifying drug delivery systems (SNEDDS) for a poorly water soluble drug, olmesartan medoxomil (OLM) by Formulation by Design (FbD) approach with an aim to improve its solubility and dissolution. Methods:The SNEDDS were systematically optimised using three factor Box-Behnken Results: Following optimisation, the values of formulation variables were found to be 142.276 mg (Capryol P), 399.999 mg (Cremophor EL) and 598.871 mg (Transcutol P) which produced a globule size of 12.64 nm, percentage drug release of 93.34% and a turbidity of 0.02 FNU. TEM studies demonstrated spherical droplet morphology.design. Concentration of formulation variables, namely, the oil phaseX1 (Capryol 90), the surfactant X2 (Cremophor EL), and the co-surfactant X3 (Transcutol P), was optimized for its impact on mean globule size (Y1), percentage drug release in 20 min (Y2) and turbidity (Y3) of the formulation. Ternary phase diagrams were constructed to select the areas of nanoemulsion and the amounts of oil, surfactant and cosurfactants as critical formulation variables. The prepared SNEDDS were characterised for globule size, dissolution studies, turbidity, and transmission electron microscopy (TEM). Conclusion:Thus, the present studies reveal that the SNEDDS is a promising drug delivery system approach for the enhancement of solubility and dissolution rate of OLM.

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Section: Optimisation and Evaluation Of Olmesartan Sneddsmentioning

confidence: 99%

Design, Optimization and in Vitro Characterization of Self Nano Emulsifying Drug Delivery System of Olmesartan Medoxomil

Sisinthy

Nalamolu

Sarah

2016

Int J Pharm Pharm Sci

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“…High absolute ZP values (±30 mV) should preferably be achieved in most of the emulsions prepared in order to ensure the creation of a highenergy barrier against coalescence of the dispersed droplets. 22 However, this suggested ZP cutoff point is only an experiencebased value and cannot be reliably used to predict the stability of SNEDDS, because a wide range of absolute ZP values (ie, 1.5, 12.5, 45.5 mV) have been reported for SNEDDS in previous studies, 22,26,27,37 most of which did not have any long-term stability assessment for verification purposes. In the current study, globule size, ZP, and PDI of SNEDDS diluted in distilled water (500-fold) were measured by photon correlation spectroscopy using a Malvern Zetasizer ZS, and factors included drug addition to placebo formulation, system alkalinization, and drug dose.…”

Section: 31mentioning

confidence: 99%

“…25 High emulsification efficiency is therefore judged by a small number of flask inversions (lower than ten) in addition to high-percentage transmittance (higher than 90%). 15,27,37 One flask inversion requires only 1 second. Transmittance values of different mixtures are demonstrated in Table 1.…”

Section: Preliminary Studiesmentioning

confidence: 99%

“…[35][36][37][38][39][40][41][42] In this novel method, the potential of the elaborated nanocarriers to increase RLX delivery to endocrine target organs (uterus, ovaries and fallopian tubes) was assessed in female Wistar rats weighing 190 ± 20 g. Rats were obtained from Vacsera (Cairo, Egypt). Experiments were performed in accordance with the European Community guidelines for the use of experimental animals and were approved by the institutional ethics committee.…”

Section: In Vivo Study Animals and Experimental Protocolmentioning

confidence: 99%

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Nanoemulsion liquid preconcentrates for raloxifene hydrochloride: optimization and in vivo appraisal

Elsheikh¹,

Elnaggar²,

Gohar³

et al. 2012

IJN

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Raloxifene hydrochloride (RLX) is a selective estrogen-receptor modulator for treatment of osteoporosis and prevention of breast and endometrial cancer. By virtue of extensive presystemic clearance, RLX bioavailability is only 2%. The current study aimed to tailor and characterize RLX-loaded self-nanoemulsifying drug-delivery systems (SNEDDS) using bioactive excipients affecting drug metabolism. The potential of oral nanocarriers to enhance RLX delivery to endocrine target organs was assessed in fasted and fed female Wistar rats using high-performance liquid chromatography. RLX was loaded in the dissolved and dispersed status in the alkalinized (A-SNEDDS) and nonalkalinized (NA-SNEDDS) systems, respectively. Optimization and assessment relied on solubility studies, emulsification efficiency, phase diagrams, dilution robustness, cloud point, particle size, zeta potential (ZP), polydispersity index (PDI), and transmission electron microscopy. In vitro release was assessed using dialysis bag versus dissolution cup methods. NA-SNEDDS were developed with suitable globule size (38.49 ± 4.30 nm), ZP (31.70 ± 3.58 mV), PDI (0.31 ± 0.02), and cloud point (85°C). A-SNEDDS exhibited good globule size (35 ± 2.80 nm), adequate PDI (0.28 ± 0.06), and lower ZP magnitude (−21.20 ± 3.46 mV). Transmission electron microscopy revealed spherical globules and contended data of size analysis. Release studies demonstrated a nonsignificant enhancement of RLX release from NA-SNEDDS compared to drug suspension with the lowest release shown by A-SNEDDS. A conflicting result was elucidated from in vivo trial. A significant enhancement in RLX uptake by endocrine organs was observed after nanocarrier administration compared to RLX suspension. In vivo studies reflected a poor in vitro/in vivo correlation, recommended nanocarrier administration before meals, and did not reveal any advantage for drug loading in the solubilized form (A-SNEDDS). To conclude, NA-SNEDDS possessed superior in vitro characteristics to A-SNEDDS, with equal in vivo potential. NA-SNEDDS elaborated in this work could successfully double RLX delivery to endocrine target organs, with promising consequences of lower dose and side effects of the drug.

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“…The nano-sized particles would perform an effective GI lumen penetration through both active and passive absorbtion 6 . In a study by Patel et al (2011), SNEDDS system was able to induce in vivo absorption by 7.5 folds 7 . Moreover, the oil based system will escape pHrelated influence of the GI tract thus ideal as a formulation for oral adminitration 8 .…”

Section: Introductionmentioning

confidence: 99%

Acute Toxicity of Self Nano-emulsifying Formulation of Curcumin Analogue Gamavuton-0, A New Candidate for Rheumatoid Arthritis Treatment

Chabib¹,

Ikawati²,

Martien³

et al. 2017

IJPTR

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: Gamavuton-0 (GVT-0), a newly developed compound synthesized by a carbonyl group and a methylene reduction of Curcumin, has been proven to have several anti arthritic activities. The compound has been further proven to have no short-term toxicity in rat in vivo. However, GVT-0 still burdens low water solubility therefore poorly absorbed in oral administration. Currently, a self-nano-emulsifying system has been developed to formulate GVT-0 into a more effective oral anti RA candidate using various oils and surfactants (SNE GVT-0). To study whether this formulation would not alter the safety of the compound in oral administration, an in vivo acute toxicity testing was conducted. A 14 day-study was performed by using four groups of wistar strain Rattus norvegicus, three rats per group, with 300 mg/kg BW GVT-0 as preliminary dose and 2000 mg/kg BW as oral treatment dose, along with naïve GVT-0 and solvent as controls. The protocols and toxic parameters were all conducted following OECD 423. The study showed that all the treatments on both 300 and 2000 mg/kg BW of SNE GVT-0 did not compromise rats' body weight, and toxicity clinical behaviours were observed on the 2000 mg/kgBW of administration, but there is no significance observed for 300 mg/kg BW administration. Microscopic observation under haematoxylin and eosin staining confirmed the clinical findings by showing degeneration and destruction for the most of organs on the 2000 mg/kg BW of administration. The results suggest SNE GVT-0 as in category four in OECD 423 globally harmonized classification system (GHS) with estimated LD50 cut-off as 2000 mg/kg BW.

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Formulation and development of a self-nanoemulsifying drug delivery system of irbesartan

Cited by 171 publications

References 13 publications

Design, Optimization and in Vitro Characterization of Self Nano Emulsifying Drug Delivery System of Olmesartan Medoxomil

Design, Optimization and in Vitro Characterization of Self Nano Emulsifying Drug Delivery System of Olmesartan Medoxomil

Nanoemulsion liquid preconcentrates for raloxifene hydrochloride: optimization and in vivo appraisal

Acute Toxicity of Self Nano-emulsifying Formulation of Curcumin Analogue Gamavuton-0, A New Candidate for Rheumatoid Arthritis Treatment

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