Interfacial and colloidal properties of emulsified systems

Sharma, Shweta; Shukla, P.K.; Misra, Amit; Mishra, Prabhat Ranjan

doi:10.1016/b978-0-444-62614-1.00008-9

Cited by 38 publications

(24 citation statements)

References 65 publications

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“…As was reported by Roland et al ZP values should be at least 10 mV to permit estimate of distinct stability (38). In general, emulsion systems with ZP > ±30 mV is completely pharmaceutically stable (39). ZP of optimized formulation was 24.3 mV indicating a good stability when prepared as a colloidal system.…”

Section: Discussionmentioning

confidence: 55%

Targeted Nanostructured Lipid Carrier for Brain Delivery of Artemisinin: Design, Preparation, Characterization, Optimization and Cell Toxicity

2018

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In the present study, a transferrin-conjugated nanostructured lipid carrier (TF-NLCs) for brain delivery of artemisinin (ART) was developed. ART-loaded NLCs (ART-NLCs) were prepared using solvent evaporation method and the impact of various formulation or process variables on the responses were assessed using a Taguchi design. Optimized ART-NLC was then coupled with transferrin as targeting ligand and its in vitro cytotoxicity was investigated against U-87MG brain cancer cell line. As a result, the following values are suggested by the software to prepare the optimized formulation: 20 mg Compritol®, 0.25% Tween 80, 5 mg oleic acid, 2.5 mL dichloromethane and 4 min sonication. Mean particle size (PS), zeta potential (ZP), polydispersity index (PDI), entrapment efficiency (EE), mean release time (MRT) of adopted formulation were confirmed to be 145 ± 12.5 nm, 24.3 ± 1.5 mV, 0.513 ± 0.021, 82.3 ± 7.3 % and 24.0 ± 1.1 h, respectively. Following conjugation of optimized ART-NLCs with TF, PS and MRT were increased, while ZP, and EE were decreased significantly. TF-ART-NLCs showed higher cytotoxic activity compared to non-targeted NLCs and free drug. These results indicated that the TF-ART-NLCs could potentially be exploited as a delivery system for anticancer and antimalarial drug ART in brain tumors and malaria.

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Section: Discussionmentioning

confidence: 55%

Targeted Nanostructured Lipid Carrier for Brain Delivery of Artemisinin: Design, Preparation, Characterization, Optimization and Cell Toxicity

2018

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“…It is known that increasingly negative or positive zeta-potential values (i.e., >30 mV or ˂−30 mV) signify increased electrostatic repulsion between droplets, and are therefore considered favorable as coagulation is circumvented [ 68 ]. Nevertheless, a minute deviation is allowed as research recognized that emulsions stabilized by both steric and combined electrostatic forces, as enabled by Tween ® 80, with a minimum zeta-potential value of −20 mV, can be contemplated acceptable [ 69 , 70 ].…”

Section: Resultsmentioning

confidence: 99%

Development of a Self-Emulsifying Drug Delivery System for Optimized Topical Delivery of Clofazimine

2020

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A quality-by-design and characterization approach was followed to ensure development of self-emulsifying drug delivery systems (SEDDSs) destined for topical delivery of the highly lipophilic clofazimine. Solubility and water-titration experiments identified spontaneous emulsification capacity of different excipient combinations and clofazimine. After identifying self-emulsification regions, check-point formulations were selected within the self-emulsification region by considering characteristics required to achieve optimized topical drug delivery. Check-point formulations, able to withstand phase separation after 24 h at an ambient temperature, were subjected to characterization studies. Experiments involved droplet size evaluation; size distribution; zeta-potential; self-emulsification time and efficacy; viscosity and pH measurement; cloud point assessment; and thermodynamic stability studies. SEDDSs with favorable properties, i.e., topical drug delivery, were subjected to dermal diffusion studies. Successful in vitro topical clofazimine delivery was observed. Olive oil facilitated the highest topical delivery of clofazimine probably due to increased oleic acid levels that enhanced stratum corneum lipid disruption, followed by improved dermal clofazimine delivery. Finally, isothermal microcalometric experiments studied the compatibility of excipients. Potential interactions were depicted between argan oil and clofazimine as well as between Span®60 and argan-, macadamia- and olive oil, respectively. However, despite some mundane incompatibilities, successful development of topical SEDDSs achieved enhanced topical clofazimine delivery.

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“…The charge on the particle surface could be occurred due to the dissociation of some functional groups which are mainly depending on the pH of the suspension. Zeta potential value between (-20 and -30 mV) indicates stable suspensions [ 25 ]. The zeta potential of ROSCa nanosuspension not containing stabilizer was measured and was found (-6.91 mv), ( Fig 1 ).…”

Section: Resultsmentioning

confidence: 99%

Rosuvastatin calcium nanoparticles: Improving bioavailability by formulation and stabilization codesign

et al. 2018

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PurposeRosuvastatin calcium (ROSCa) is a poorly soluble drug with bioavailability not exceeding 20%. Decreasing the particle size may enhance its solubility, dissolution rate and bioavailability. Therefore, the aim of the current study is to prepare ROSCa nanoparticles by wet milling technique using planetary ball mill. The codesign between formulation and stabilization of nanoparticles was studied to achieve both high dissolution as well as bioavailability.MethodologyROSCa nanosuspensions was prepared by wet milling technique using planetary ball mill, by applying milling ball size of 0.1 mm at speed of 800 rpm for 3 cycles each cycle composed of 10 minutes. HPMC, PVP k-30, pluronic F-127, Tween 80 and PEG 6000 were used as stabilizers. The nanosuspensions were then freeze-dried, and the dried nanoparticles were evaluated for particle size, zeta potential, in-vitro dissolution test, XRPD and in-vivo study.ResultsROSCa nanoparticles stabilized with 10% PVP (P3) had a good stability with smallest particle size, which in turn enhanced the dissolution rate. The particle size of the leading formula was 461.8 ± 16.68 nm with zeta potential of -31.8 ± 7.22 mV compared to untreated drug that has a particle size of 618μm. The percent of ROSCa dissolved after 1 hour enhanced significantly which reached 72% and 58.25% for leading nanoparticle formula and untreated ROSCa, respectively (P < 0.05). The in-vivo study of ROSCa from the leading nanoparticle formula showed a significant enhancement in the Cmax after 2 h (82.35 ng/ml) compared to 9.2 ng/ml for untreated drug.ConclusionWet milling technique is a successful method to prepare ROSCa nanoparticles. From different stabilizer used, PVP (10%) was able to produce stable nanoparticle with small particle size which significantly enhance the dissolution rate and pharmacokinetics parameters of ROSCa.

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Interfacial and colloidal properties of emulsified systems

Cited by 38 publications

References 65 publications

Targeted Nanostructured Lipid Carrier for Brain Delivery of Artemisinin: Design, Preparation, Characterization, Optimization and Cell Toxicity

Targeted Nanostructured Lipid Carrier for Brain Delivery of Artemisinin: Design, Preparation, Characterization, Optimization and Cell Toxicity

Development of a Self-Emulsifying Drug Delivery System for Optimized Topical Delivery of Clofazimine

Rosuvastatin calcium nanoparticles: Improving bioavailability by formulation and stabilization codesign

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