Assessment of solubilization characteristics of different surfactants for carvedilol phosphate as a function of pH

Chakraborty, Sayantani; Shukla, D. N.; Jain, Avinash; Mishra, Brahmeshwar; Singh, Sanjay

doi:10.1016/j.jcis.2009.03.047

Cited by 90 publications

(68 citation statements)

References 22 publications

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“…Apparent solubility (S a ), solubility factor ( f S ) of ETOX in micellar systems, binding constant to aggregation number ratio (K/N) for drug-saturated 10% poloxamine solutions in 0.9% NaCl, after 72 h at 258C, and ETOX remaining solubilized (expressed as percentage referred to the initial S a value) after 28 days of storage. (from the CMC to about 100 times greater) [42]. Using the values of N for poloxamine micelles in HCl 10 mM previously reported [21], the binding constant K would be much larger for T904 (49 260) compared with that of T908 (21 001), T1107 (16 439) and T1307 (25 482), owing to the fact that each micelle of T904 is formed by a greater number of unimers (14) than those of T908 (7), T1107 (4) and T1307 (5).…”

Section: Ethoxzolamide Solubilizationmentioning

confidence: 93%

Single and mixed poloxamine micelles as nanocarriers for solubilization and sustained release of ethoxzolamide for topical glaucoma therapy

Ribeiro

Sosnik

Chiappetta

et al. 2012

J. R. Soc. Interface.

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Polymeric micelles of single and mixed poloxamines (Tetronic) were evaluated regarding their ability to host the antiglaucoma agent ethoxzolamide (ETOX) for topical ocular application. Three highly hydrophilic varieties of poloxamine (T908, T1107 and T1307) and a medium hydrophilic variety (T904), possessing a similar number of propylene oxide units but different contents in ethylene oxide, were chosen for the study. The critical micellar concentration and the cloud point of mixed micelles in 0.9 per cent NaCl were slightly greater than the values predicted from the additive rule, suggesting that the co-micellization is hindered. Micellar size ranged between 17 and 120 nm and it was not altered after the loading of ETOX (2.7-11.5 mg drug g -1 poloxamine). Drug solubilization ability ranked in the order: T904 (50-fold increase in the apparent solubility) . T1107 ffi T1307 . T908. Mixed micelles showed an intermediate capability to host ETOX but a greater physical stability, maintaining almost 100 per cent drug solubilized after 28 days. Furthermore, the different structural features of poloxamines and their combination in mixed micelles enabled the tuning of drug release profiles, sustaining the release in the 1-5 days range. These findings together with promising hen's egg test-chorioallantoic membrane biocompatibility tests make poloxamine micelles promising nanocarriers for carbonic anhydrase inhibitors in the treatment of glaucoma.

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Section: Ethoxzolamide Solubilizationmentioning

confidence: 93%

Single and mixed poloxamine micelles as nanocarriers for solubilization and sustained release of ethoxzolamide for topical glaucoma therapy

Ribeiro

Sosnik

Chiappetta

et al. 2012

J. R. Soc. Interface.

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“…Carvedilol, ((±)-1-(carbazol-4-yloxy)-3-[[2-(omethoxyphenoxy) ethyl] amino]-2-propanol) (Chakraborty et al, 2009), is a drug showing antioxidant properties used in clinical practice for the treatment of cardiovascular diseases (hypertension, congestive heart failure, or myocardial infarction; Wen et al, 2004). The oral bioavailability remains low (e.g.…”

Section: Introductionmentioning

confidence: 99%

Carvedilol nano lipid carriers: formulation, characterization and in-vivo evaluation

et al. 2016

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The purpose of this study was to develop Carvedilol nanostructured lipid carriers (CAR-NLCs) using stearic acid and oleic acid as lipid, and to estimate the potential as oral delivery system for poorly water soluble drug. The particle-size analysis revealed that all the developed formulations were within the nanometer range. The EE and loading were found to be between 69.45-88.56% and 9.58-12.56%, respectively. The CAR-NLCopt showed spherical morphology with smooth surface under transmission electron microscope (TEM). The crystallization of the drug in NLC was investigated by powder X-ray diffraction and differential scanning calorimetry (DSC) and revealed that the drug was in an amorphous state in the NLC matrix. The ex vivo gut permeation study showed many folds increment in the permeation of CAR-NLCs compared to Carvedilol suspension (CAR-S). The oral bioavailability study of CAR was carried out using Wistar rats and relative bioavailability of CAR-NLCopt was found to be 3.95 fold increased in comparison with CAR-S. In vivo antihypertensive study in Wistar rats showed significant reduction in mean systolic BP by CAR-NLCopt vis-à-vis CAR-S (p50.05) owing to the drug absorption through lymphatic pathways. In conclusion, the NLC formulation remarkably improved the oral bioavailability of CAR and demonstrated a promising perspective for oral delivery of poorly water-soluble drugs. The promising findings in this investigation suggest the practicability of these systems for the enhancement of bioavailability of CAR.

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“…In these drugs, dissolution of the drug is the rate limiting step in the absorption process. To triumph over these obstacles, numbers of formulation approaches are reported including the use of surfactants (Allaboun et al, 2003;Balakrishnan et al, 2004;Chakraborty et al, 2009), lipids (Yeap et al, 2013), permeation enhancers (Burcin et al, 2010;Beg et al, 2011), formation of salt (Li et al, 2005;Serajuddin, 2007), co-crystallization (Shan & Zaworotko, 2008;Qiao et al, 2011;Chadha et al, 2012), solid dispersions (Serajuddin, 1999), inclusion complexes with cyclodextrins and modified cyclodextrins (Miyake et al, 2000;Veiga et al, 2000;Wang et al, 2000;Bannwart et al, 2001;Carrier et al, 2007;Gamsiz et al, 2010a,b;Gamsiz et al, 2011;Badr-Eldin et al, 2008;Kumar et al, 2013), nanosuspensions (Patravale et al, 2004), and colloidal vesicles like liposomes (Nazzal et al, 2002a;Manconi et al, 2013;Yang et al, 2013), and niosomes (Khazaeli et al, 2007;Bayindir & Yuksel, 2010;SezginBayindir et al, 2013;Jin et al, 2013) In modern years, self-nanoemulsifying drug delivery systems (SNEDDS) are the most popular and commercially feasible lipid-based formulation approach for improving oral bioavailability of poorly water soluble and lipophilic drugs (Pouton, 2006;Date, 2007;Shweta et al, 2011). SNEDDS are precisely defined as an isotropic multi-component drug delivery systems composed of a synthetic or natural oil, surfactant, and co-surfactant that have a unique ability of forming fine oil in water micro-or nano-emulsion upon mild agitation followed by dilutio...…”

Section: Introductionmentioning

confidence: 99%

Solid self-nanoemulsifying drug delivery system (S-SNEDDS) for oral delivery of glimepiride: development and antidiabetic activity in albino rabbits

Mohd¹,

Sanka²,

Bandi³

et al. 2014

Drug Delivery

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(2015) Solid self-nanoemulsifying drug delivery system (S-SNEDDS) for oral delivery of glimepiride: development and antidiabetic activity in albino rabbits, Drug Delivery, 22:4, 499-508, DOI: 10.3109/10717544.2013 Context: This study presents novel self-nanoemulsifying drug delivery system potential of oral delivering which leads poorly aqueous soluble drug glimepiride.Objective: The objective of this study was to prepare solid self-nanoemulsifying drug delivery system (S-SNEDDS) for the improved oral delivery of glimepiride and to evaluate its therapeutic efficacy in albino rabbits.Results and discussion: The droplet size analyses revealed a droplet size of less than 200 nm. The solid state characterization of S-SNEDDS by scanning electron microscopy (SEM), X-ray powder diffraction and differential scanning calorimetry (DSC) revealed the absence of crystalline glimepiride in the S-SNEDDS. The in vitro dissolution studies revealed that the significant improvement in glimepiride release characteristics. The effect of S-SNEDDS on therapeutic efficacy of glimepride was assessed in albino rabbits by monitoring blood glucose levels and compared with free drug suspension, L-SNEDDS. The S-SNEDDS showed significant (p50.05) increase in in vitro drug release and therapeutic efficacy as compared with free drug. Conclusion: This study demonstrated that S-SNEDDS is a promising novel drug delivery system of glimepride to enhance oral delivery.

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Assessment of solubilization characteristics of different surfactants for carvedilol phosphate as a function of pH

Cited by 90 publications

References 22 publications

Single and mixed poloxamine micelles as nanocarriers for solubilization and sustained release of ethoxzolamide for topical glaucoma therapy

Single and mixed poloxamine micelles as nanocarriers for solubilization and sustained release of ethoxzolamide for topical glaucoma therapy

Carvedilol nano lipid carriers: formulation, characterization and in-vivo evaluation

Solid self-nanoemulsifying drug delivery system (S-SNEDDS) for oral delivery of glimepiride: development and antidiabetic activity in albino rabbits

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