Factors affecting microencapsulation of drugs in liposomes

Kulkarni, Shirish; Betageri, Guru V.; Singh, Mandip

doi:10.3109/02652049509010292

Cited by 233 publications

(142 citation statements)

References 53 publications

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“…For example, 25.32% and 70.84% were the resulted EEFs for batches 1 and 5, which were prepared with 5% and 15% (w/w) stearylamine, respectively (Table I). This result could be attributed to the ionization of tenofovir into its negatively charged conjugated acid that may interact with the positive stearylamine component of the lipid bilayers (27). Deleers et al…”

Section: Results and Discussion Entrapment Efficiency Particle Sizinmentioning

confidence: 99%

Near-Infrared Investigations of Novel Anti-HIV Tenofovir Liposomes

Zidan

Spinks

Fortunak

et al. 2010

AAPS J

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Abstract. Near-infrared (NIR) approaches is considered one of the most well-studied process analyzers evolving from the process analytical technology initiatives. The objective of this study was to evaluate NIR spectroscopy and imaging to assess individual components within a novel tenofovir liposomal formulation. By varying stearylamine, as a positive charge imparting agent, five batches were prepared by the thin film method. Each formulation was characterized in terms of drug entrapment efficiency, release characteristics, particle sizing, and zeta potential. Drug excipients compatibility was tested using Fourier transform infrared spectroscopy, differential scanning calorimetry, and X-ray diffraction. The obtained results showed an increase in drug entrapment and a slower drug release by increasing the incorporated percentage of stearylamine. The compatibility testing revealed a significant interaction between the drug and some of the investigated excipients. The developed NIR calibration model was able to assess drug, phospholipid, and stearylamine levels along the batches. The calibration and prediction plots were linear with correlation coefficients of more than 0.9. The root square standard errors of calibration and prediction did not attain 5% of the measured values confirming the accuracy of the model. In contrast, NIR spectral imaging was capable of clearly distinguishing the different batches, both qualitatively and quantitatively. A linear relationship was obtained correlating the actual drug entrapped and the predicted values obtained from the partial least squares images.

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Section: Results and Discussion Entrapment Efficiency Particle Sizinmentioning

confidence: 99%

Near-Infrared Investigations of Novel Anti-HIV Tenofovir Liposomes

Zidan

Spinks

Fortunak

et al. 2010

AAPS J

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“…Most of the phospholipid membranes of liposomes are not sufficiently rigid; they often leak encapsulated drugs during processing and storage (Kulkarni et al, 1995). Cholesterol, when added to lipid bilayer, fills in the gaps created by imperfect packing of other lipid bilayers and modulates the membrane fluidity, elasticity, and permeability.…”

Section: Preparation and Characterization Of Proliposomesmentioning

confidence: 99%

Controlled release application of multilamellar vesicles: a novel drug delivery approach

2010

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“…As a result, liposomes prepared by the REV and PD methods would be suitable for entrapment with high volumes of water soluble drug such as AR. However, entrapment efficiency remains dependent on other factors such as bilayer composition and the characteristics of the drug to be encapsulated (17). Furthermore, the present study demonstrated that the percentage of entrapment efficiency significantly decreased with increasing AR to lipid ratio for each method of preparation (P<0.05; ANOVA).…”

Section: Resultsmentioning

confidence: 52%

Anti-inflammatory activity of liposomes of Asparagus racemosus root extracts prepared by various methods

Plangsombat

Rungsardthong

Kongkaneramit

et al. 2016

Experimental and Therapeutic Medicine

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Abstract. Asparagus racemosus root extracts (AR) have been reported to possess a variety of pharmacological properties. The aim of the present study was to develop liposomes of AR and to assess their physicochemical characteristics and anti-inflammatory activity in the monocytic leukemia cell line THP-1. Liposomes containing various ratios of AR to lipid and a phosphatidylcholine to cholesterol molar ratio of 7:3 were prepared by thin-film hydration (TF), reverse-phase evaporation (REV) and polyol dilution (PD). The results showed that AR liposomes prepared by TF had a multilamellar structure and a large size, whereas those prepared by REV and PD were oligolamellar in structure, and of a smaller size. The particle sizes and zeta potentials of the liposomes ranged from 196.5 to 456.6 nm and from -4.34 to -18.94 mV, respectively. The AR to lipid ratio was shown to have no significant influence on particle size, while the zeta potential generally increased with increasing AR to lipid ratio. The highest entrapment efficiency values were detected in liposomes with an AR to lipid ratio of 1:5, and for liposomes prepared by TF, REV and PD methods, the entrapment efficiencies were 55.71±2.04, 56.21±3.59 and 67.68±1.37%, respectively. AR was found to exert no toxicity on THP-1 cells. The maximum anti-inflammatory activities of AR and AR liposomes, evaluated in terms of the percentage inhibition of tumor necrosis factor-α in THP-1 cells, were ~52% at a concentration of 1 µg/ml. It can be concluded from the present study that AR liposomes have the potential to be used a formulation for topical and/or transdermal drug delivery to provide anti-inflammatory activity.

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Factors affecting microencapsulation of drugs in liposomes

Cited by 233 publications

References 53 publications

Near-Infrared Investigations of Novel Anti-HIV Tenofovir Liposomes

Near-Infrared Investigations of Novel Anti-HIV Tenofovir Liposomes

Controlled release application of multilamellar vesicles: a novel drug delivery approach

Anti-inflammatory activity of liposomes of Asparagus racemosus root extracts prepared by various methods

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