Enhanced bioavailability of piroxicam using Gelucire 44/14 and Labrasol: in vitro and in vivo evaluation

Yüksel, Nilüfer; Karataş, Ayşegül; Özkan, Yalçın; Savaşer, Ayhan; Özkan, Síbel A.; Baykara, Tamer

doi:10.1016/s0939-6411(03)00142-5

Cited by 118 publications

(47 citation statements)

References 18 publications

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“…This may ostensibly be owing to the synergistic contribution of lipid, surfactant and co-surfactant in the S-SNEDDS formulations through micellar solubilization of the drug via reduction of interfacial tension to produce the oil-in-water nanoemulsion (Pouton, 2000;Shafiq et al, 2007). The characteristic ''dip'' observed for the OPT S-SNEDDS during in vitro drug release, in all respect may be attributed to the lag-time required for liquefaction of the solid nanoemulsified system into the corresponding liquid form (Attama et al, 2003;Yuksel et al, 2003;Singh et al, 2012). In contrast, there was no such event observed for the inclusion complex and MKT during in vitro drug release studies (Figure 7).…”

Section: Discussionmentioning

confidence: 99%

QbD-based systematic development of novel optimized solid self-nanoemulsifying drug delivery systems (SNEDDS) of lovastatin with enhanced biopharmaceutical performance

et al. 2014

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(2015) QbD-based systematic development of novel optimized solid self-nanoemulsifying drug delivery systems (SNEDDS) of lovastatin with enhanced biopharmaceutical performance, Drug Delivery, 22:6, 765-784, DOI: 10.3109/10717544.2014 AbstractOf late, solid self-nanoemulsifying drug delivery systems (S-SNEDDS) have been extensively sought-after owing to their superior portability, drug loading, stability and patient compliance. The current studies, therefore, entail systematic development, optimization and evaluation (in vitro, in situ and in vivo) of the solid formulations of (SNEDDS) lovastatin employing rational quality by design (QbD)-based approach of formulation by design (FbD). The patient-centric quality target product profile (QTPP) and critical quality attributes (CQAs) were earmarked. Preformulation studies along with initial risk assessment facilitated the selection of lipid (i.e. Capmul MCM), surfactant (i.e. Nikkol HCO-50) and co-surfactant (i.e. Lutrol F127) as CMAs for formulation of S-SNEDDS. A face-centered cubic design (FCCD) was employed for optimization using Nikkol-HCO50 (X 1 ) and Lutrol-F127 (X 2 ), evaluating CQAs like globule size, liquefaction time, emulsification time, MDT, dissolution efficiency and permeation parameter. The design space was generated using apt mathematical models, and the optimum formulation was located, followed by validation of the FbD methodology. In situ SPIP and in vivo pharmacodynamic studies on the optimized formulation carried out in unisex Wistar rats, corroborated superior drug absorption and enhanced pharmacodynamic potential in regulating serum lipid levels. In a nutshell, the present studies report successful QbD-oriented development of novel oral S-SNEDDS of lovastatin with distinctly improved biopharmaceutical performance.

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Section: Discussionmentioning

confidence: 99%

QbD-based systematic development of novel optimized solid self-nanoemulsifying drug delivery systems (SNEDDS) of lovastatin with enhanced biopharmaceutical performance

et al. 2014

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“…Gelucire 50/13 is obtained by PEGylation of stearoyl glycerides and has considerably higher molecular volume as compared to Gelucire 44/14 which may be the reason for less solubilization potential. Gelucire 44/14 was selected as an oil phase for further investigation due to its solubilizing potential for NM and also due to its well established bioavailability enhancing properties (17,18) which would be helpful in case of NM. Amongst various surfactants that were screened, Labrasol exhibited highest solubilizing potential for NM whereas amongst various co-surfactants, Transcutol P and Plurol (Fig.…”

Section: Solubility Studiesmentioning

confidence: 99%

Design and Evaluation of Self-Emulsifying Drug Delivery Systems (SEDDS) of Nimodipine

Kale

Patravale

2008

AAPS PharmSciTech

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Abstract. The ability of self-emulsifying drug delivery systems (SEDDS) to improve solubility, dissolution rate and bioavailability of a poorly water-soluble calcium channel blocker, nimodipine (NM) was evaluated in the present investigation. Solubility of NM in various oils, surfactants and cosurfactants was determined. The influence of the ratio of oil to surfactant + cosurfactant, pH of aqueous phase on mean globule size of resulting emulsions was studied by means of photon correlation spectroscopy. The NM loaded SEDDS selected for the in vitro and in vivo studies exhibited globule size less than 180 nm. In vitro dissolution studies indicated that NM loaded SEDDS could release complete amount of NM irrespective of the pH of the dissolution media. Pharmacokinetics of NM suspension, NM oily solution, NM micellar solution and NM SEDDS were evaluated and compared in rabbits. Relative bioavailability of NM in SEDDS was significantly higher than all the other formulations. NM loaded SEDDS were subjected to various conditions of storage as per ICH guidelines for 3 months. NM SEDDS successfully withstood the stability testing.KEY WORDS: in vitro drug release; low oral bioavailability; nimodipine; pharmacokinetics; selfemulsifying drug delivery systems (SEDDS).

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“…The nature and proportion of each component are specific to a given grade of Gelucire. Gelucires have been widely studied as controlled release matrices (Dennis et al, 1990;Galal et al, 2004) as well as for modulating the solubility of poorly soluble drugs for enhancing their dissolution rate and subsequently their bioavailability Yüksela et al, 2003). Gelucires on heating can give a molten/semisolid mass with drug in solubilized state, which can be easily filled in the hard gelatin capsule by liquid filling technique (Hauss, 2007), a technology that is more efficient and comparatively economic than powder capsule filling.…”

Section: Introductionmentioning

confidence: 99%

Modulating drug release profiles by lipid semi solid matrix formulations for BCS class II drug – anin vitroand anin vivostudy

2014

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The main objective of the study was to alter the dissolution profile of a practically insoluble Biopharmaceutics Classification System class II drug, aceclofenac, by formulating into lipid semisolid matrix (SSM) formulations using liquid filling technology in hard gelatin capsules, for both immediate and sustained release. SSM formulations of aceclofenac were prepared by melt fusion technique, using Gelucires (44/14, 50/13, 33/01 and 43/01), polyethylene glycols (4000 and 6000) and Poloxamer 188 at different levels. Role of additives like docusate sodium, Tween 80, Aerosil 200 and polyvinylpyrrolidone K-30 in enhancement of drug release was investigated. The optimized immediate and sustained SSM capsules were characterized in terms of assay, in vitro drug release, moisture uptake and differential scanning calorimetry. More than 80% of the drug was released within 15 min in various dissolution media studied, from Gelucire 44/14-based immediate release formulations. Incorporation of docusate sodium and Tween 80 provided further enhancement in drug dissolution when compared to plain drug and marketed tablet. SSM formulations based on Gelucire blends of 50/13 and 43/01 and 44/14 and 43/01 sustained the release of the drug for a period of 24 h following zero-order kinetics. The in vivo study of the optimized immediate release and sustained release formulations revealed significant enhancement in anti inflammatory activity (p50.01) in rats. From these findings, liquid fill technique in hard gelatin capsules using Gelucire and their blends might be an efficacious approach for designing immediate or sustained drug release profiles for poorly soluble drugs like aceclofenac.

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Enhanced bioavailability of piroxicam using Gelucire 44/14 and Labrasol: in vitro and in vivo evaluation

Cited by 118 publications

References 18 publications

QbD-based systematic development of novel optimized solid self-nanoemulsifying drug delivery systems (SNEDDS) of lovastatin with enhanced biopharmaceutical performance

QbD-based systematic development of novel optimized solid self-nanoemulsifying drug delivery systems (SNEDDS) of lovastatin with enhanced biopharmaceutical performance

Design and Evaluation of Self-Emulsifying Drug Delivery Systems (SEDDS) of Nimodipine

Modulating drug release profiles by lipid semi solid matrix formulations for BCS class II drug – anin vitroand anin vivostudy

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