Improved oral bioavailability of glyburide by a self-nanoemulsifying drug delivery system

Liu, Hongzhuo; Shang, Kuimao; Liu, Weina; Leng, Donglei; Li, Ran; Kong, Ying; Zhang, Tianhong

doi:10.3109/02652048.2013.843598

Cited by 21 publications

(15 citation statements)

References 26 publications

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“…GLB is a Biopharmaceutics Classification System (BCS) class II drug, with low oral bioavailability of~45% and having a high permeability and low aqueous solubility [10]. GLB has a high dose frequency due to short elimination half-life of 4 h [11]. Atenolol (ATN) is a beta-adrenergic receptor blocker with no membrane stabilization or intrinsic sympathomimetic activity, which has been used to treat hypertension.…”

Section: Introductionmentioning

confidence: 99%

Design and optimization of nano invasomal gel of Glibenclamide and Atenolol combination: in vitro and in vivo evaluation

Anitha

Satyanarayana

2021

Futur J Pharm Sci

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Background There are many circumstances where chronic disease is associated with other disorders, especially in diseases such as diabetes with noncommunicable disease risk factors, such as hypertension. The current therapies for treating such chronic comorbid diseases are limited and challenging due to the difficulties in overcoming the side effects from complex therapeutic treatment regimen. The present study is aimed to develop and optimize the combinational nano invasomal gel of Glibenclamide (GLB) and Atenolol (ATN) as a novel combination therapy for comorbid treatment of diabetic hypertensive patients. The developed formulations were characterized for various parameters, including in-vitro skin permeation, skin irritation, in-vivo antidiabetic, and antihypertensive activities. Results OCNIG showed that the % entrapment efficiency of GLB is 96.67 ± 0.65% and % entrapment efficiency of ATN is 93.76 ± 0.89%, flux of GLB (240.43 ± 1.76 μg/cm2/h), and flux of ATN (475.2 ± 1.54 μg/cm2/h) which was found to conform to the expected value. The results indicated desired release and permeation profiles. Optimized formulation showed significant pharmacokinetic properties, which shows improvement in bioavailability by 134.30% and 180.32% respectively for two drugs, when compared to marketed oral preparation. Pharmacodynamic studies showed improved and prolonged management of diabetes and hypertension in Wistar rats, compared to oral and drug-loaded nano invasomes formulations. Conclusion Overall, the results showed that nano invasomal gel was found to be a useful and promising transdermal delivery system for the treatment of concurrent diseases.

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Section: Introductionmentioning

confidence: 99%

Design and optimization of nano invasomal gel of Glibenclamide and Atenolol combination: in vitro and in vivo evaluation

Anitha

Satyanarayana

2021

Futur J Pharm Sci

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“…21,22 Due to its poor aqueous solubility and dissolution rate, GBD shows low and erratic oral bioavailability. 23 Different strategies were investigated and published to enhance the dissolution rate and bioavailability of GBD. [24][25][26][27] In spite of these efforts, overall findings were not completely satisfactory, and no GBD product which resulted from these studies have been commercialized.…”

Section: Introductionmentioning

confidence: 99%

<p>Engineering of solidified glyburide nanocrystals for tablet formulation via loading of carriers: downstream processing, characterization, and bioavailability</p>

Ali

Hanafy

Alqurshi

2019

IJN

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Introduction: Presenting poorly water-soluble drugs as nanoparticles has shown to be an effective technique in enhancing drug dissolution rate, intrinsic solubility, and thus oral bioavailability. Nevertheless, working with nanoparticles introduces many challenges, one of which is their physical instability. Formulating nanoparticles into a solid dosage form may overcome such challenges and thus unlock the potential benefits of nanosizing. Methods: The current work investigates the possibility of developing a novel solid dosage form, with enhanced dissolution rate, whereby nanocrystals (~400 nm) of the class II Biopharmaceutical Classification System drug, glyburide (GBD) were fabricated through combined precipitation and homogenization procedures. Using a novel, but scalable, spraying technique, GBD nanocrystals were loaded onto commonly used tablet fillers, water-soluble lactose monohydrate (LAC), and water insoluble microcrystalline cellulose (MCC). Conventional tableting processes were then used to convert the powders generated into a tablet dosage form. Results: Studies of redispersibility showed considerable preservation of size characteristics of GBD nanocrystals during downstream processing with redispersibility indices of 105 and 118 for GBD-LAC and GBD-MCC, respectively. Characterization by differential scanning calorimetry, powder X-ray diffraction, and scanning electron microscopy showed that the powders generated powders contained nanosized crystals of GBD which adhered to carrier surfaces. Powder flowability was characterized using Hausner ratio (HR) and Carr's index (CI). GBD-LAC-loaded particles exhibited poor flowability with CI and HR of 37.5% and 1.60, respectively, whilst GBD-MCC particles showed a slightly improved flowability with CI and HR of 26.47% and 1.36, respectively. The novel tablet dosage form met US Pharmacopeia specifications, including drug content, hardness, and friability. Conclusion: Higher dissolution rates were observed from the nanocrystal-based tablets compared to the microsized and commercial drug formulations. Moreover, the novel nanocrystal tablet dosage forms showed enhanced in vivo performance with area under the plasma concentrationtime curve in the first 24 hours values 1.97 and 2.24 times greater than that of marketed tablets.

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“…This dispersion helps to enhance the solubility and absorption of lipophilic drugs in aqueous system. Various forms of lipid-based delivery systems are present, namely solutions, suspensions, emulsions, microemulsions, SEDDS, or dry emulsions [20].…”

Section: Solubilitymentioning

confidence: 99%

Amelioration of lipophilic compounds in regards to bioavailability as self-emulsifying drug delivery system (SEDDS)

Baghel¹,

Roy²,

Verma

et al. 2020

Futur J Pharm Sci

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Background: High lipophilicity and poor aqueous solubility are the endemic problems of new drug molecules. Sixty to seventy percent of these drugs are unable to solubilize completely in aqueous media, or have very low permeability. This hampers their oral absorption and further leads to their poor bioavailability. Various researches are in progress to overcome these limitations. Novel technologies like nano-carrier systems have become popular for improving the solubility of drugs. Main body: Lipid-based formulations, among nano systems, are taking pace for the enhancement of solubility, oral absorption, and hence the bioavailability of drugs. Among the lipid formulations, self-emulsification systems are gaining popularity by offering various advantages to delivery systems. Self-emulsifying drug delivery systems (SEDDS) are isotropic blends of oil and surfactant/co-surfactants. These ingredients upon gentle agitation in aqueous media results in the formation of o/w emulsion. In spite of many works published in SEDDS, the major concerns of this article are to discuss the various approaches to formulate a good lipid-based carrier system for poorly aqueous soluble drugs, role of various polymers, and their categories used in the formulation along-with the modern technologies used for enhancing the stability of liquid SEDDS. This review majorly focuses upon the problems related to the poor aqueous solubility of the newer lipid molecules and the solutions to overcome their solubility and in addition bioavailability. Conclusion:As per the researches done in formulation and optimization of SEDDS for the enhancement of bioavailability of lipophilic molecules, it can be stated that the aqueous solubility as well as bioavailability can be increased by many folds compared to their marketed or other oral formulations.

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Improved oral bioavailability of glyburide by a self-nanoemulsifying drug delivery system

Abstract: These results indicated that SNEDDS is a promising drug delivery system for increasing the oral bioavailability of glyburide.

Cited by 21 publications

References 26 publications

Design and optimization of nano invasomal gel of Glibenclamide and Atenolol combination: in vitro and in vivo evaluation

Design and optimization of nano invasomal gel of Glibenclamide and Atenolol combination: in vitro and in vivo evaluation

<p>Engineering of solidified glyburide nanocrystals for tablet formulation via loading of carriers: downstream processing, characterization, and bioavailability</p>

Amelioration of lipophilic compounds in regards to bioavailability as self-emulsifying drug delivery system (SEDDS)

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