Interaction of drug molecules with carrier systems as studied by parelectric spectroscopy and electron spin resonance

Braem, C.; Blaschke, Tobias; Panek-Minkin, G.; Herrmann, W. M.; Schlupp, Peggy; Paepenmüller, T.; Müller-Goyman, C.; Mehnert, W.; Bittl, Robert; Schäfer‐Korting, Monika; Kramer, K.D.

doi:10.1016/j.jconrel.2007.01.017

Cited by 39 publications

(22 citation statements)

References 25 publications

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“…ESR requires a paramagnetic spin probes to investigate SLN dispersions. Direct, repeatable, and noninvasive characterization of the distribution of the spin probe between the aqueous and the lipid phase can be performed by ESR (78,80). However, despite the great potential, NMR and ESR have been rarely applied to characterize SLNs and NLCs.…”

Section: Assessment Of Alternative Colloidal Structuresmentioning

confidence: 99%

Recent Advances in Lipid Nanoparticle Formulations with Solid Matrix for Oral Drug Delivery

2010

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Abstract. Lipid nanoparticles based on solid matrix have emerged as potential drug carriers to improve gastrointestinal (GI) absorption and oral bioavailability of several drugs, especially lipophilic compounds. These formulations may also be used for sustained drug release. Solid lipid nanoparticle (SLN) and the newer generation lipid nanoparticle, nanostructured lipid carrier (NLC), have been studied for their capability as oral drug carriers. Biodegradable, biocompatible, and physiological lipids are generally used to prepare these nanoparticles. Hence, toxicity problems related with the polymeric nanoparticles can be minimized. Furthermore, stability of the formulations might increase than other liquid nano-carriers due to the solid matrix of these lipid nanoparticles. These nanoparticles can be produced by different formulation techniques. Scaling up of the production process from lab scale to industrial scale can be easily achieved. Reasonably high drug encapsulation efficiency of the nanoparticles was documented. Oral absorption and bioavailability of several drugs were improved after oral administration of the drugloaded SLNs or NLCs. In this review, pros and cons, different formulation and characterization techniques, drug incorporation models, GI absorption and oral bioavailability enhancement mechanisms, stability and storage condition of the formulations, and recent advances in oral delivery of the lipid nanoparticles based on solid matrix will be discussed.

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Section: Assessment Of Alternative Colloidal Structuresmentioning

confidence: 99%

Recent Advances in Lipid Nanoparticle Formulations with Solid Matrix for Oral Drug Delivery

2010

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“…Interestingly, uptake from SLNs is clearly superior to uptake from particles built up from both solid lipids and oils (nanostructured lipid carriers) [14,15] . Active pharmaceutical ingredients or marker agents (dyes or spin probes) can be incorporated into the lipid matrix of SLNs [14] or attached to the particle surface [15][16][17][18] . In fact, even subcompartments of spin probe localization have been observed [16] .…”

Section: Introductionmentioning

confidence: 99%

Drug Release and Skin Penetration from Solid Lipid Nanoparticles and a Base Cream: A Systematic Approach from a Comparison of Three Glucocorticoids

Schlupp

Blaschke²,

Kramer³

et al. 2011

Skin Pharmacol Physiol

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Solid lipid nanoparticles (SLNs) can enhance drug penetration into the skin, yet the mechanism of the improved transport is not known in full. To unravel the influence of the drug-particle interaction on penetration enhancement, 3 glucocorticoids (GCs), prednisolone (PD), the diester prednicarbate (PC) and the monoester betamethasone 17-valerate (BMV), varying in structure and lipophilicity, were loaded onto SLNs. Theoretical permeability coefficients (cm/s) of the agents rank BMV (–6.38) ≧ PC (–6.57) > PD (–7.30). GC-particle interaction, drug release and skin penetration were investigated including a conventional oil-in-water cream for reference. Both with SLN and cream, PD release was clearly superior to PC release which exceeded BMV release. With the cream, the rank order did not change when studying skin penetration, and skin penetration is thus predominantly influenced by drug release. Yet, the penetration profile for the GCs loaded onto SLNs completely changed, and differences between the steroids were almost lost. Thus, SLNs influence skin penetration by an intrinsic mechanism linked to a specific interaction of the drug-carrier complex and the skin surface, which becomes possible by the lipid nature and nanosize of the carrier and appears not to be derived by testing drug release. Interestingly, PC and PD uptake from SLN even resulted in epidermal targeting. Thus, SLNs are not only able to improve skin penetration of topically applied drugs, but may also be of particular interest when specifically aiming to influence epidermal dysfunction.

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“…OxBu SLN were prepared using the hot homogenization method [17,23,24] with the modification of drug dissolution in DMSO. In short, OxBu dissolved in DMSO was mixed with melted glyceryl behenate.…”

Section: Methodsmentioning

confidence: 99%

“…In addition, scanning electron microscopy (Zeiss DSM 950 microscope; Zeiss, Jena, Germany) images were generated to study size and shape of the nanocarriers. Parelectric spectroscopy was employed to check for free drug molecules in the aqueous phase and to unravel the mode of OxBu interaction with the lipid matrix [23,25]. The amount of OxBu loaded to SLN (drug entrapment efficiency [17]) was quantified from the supernatant of centrifuged nanocarriers (70,000 g , 90 min) by high-performance liquid chromatography (HPLC).…”

Section: Methodsmentioning

confidence: 99%

Improving Topical Non-Melanoma Skin Cancer Treatment: In vitro Efficacy of a Novel Guanosine-Analog Phosphonate

Laue

Zoschke²,

Do³

et al. 2014

Skin Pharmacol Physiol

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Actinic keratosis, a frequent carcinoma in situ of non-melanoma skin cancer (NMSC), can transform into life-threatening cutaneous squamous cell carcinoma. Current treatment is limited due to low complete clearance rates and asks for novel therapeutic concepts; the novel purine nucleotide analogue OxBu may be an option. In order to enhance skin penetration, solid lipid nanoparticles (SLN, 136-156 nm) were produced with an OxBu entrapment efficiency of 96.5 ± 0.1%. For improved preclinical evaluation, we combined tissue engineering with clinically used keratin-18 quantification. Three doses of 10^-3 mol/l OxBu, dissolved in phosphate-buffered saline as well as loaded to SLN, were effective on reconstructed NMSC. Tumour response and apoptosis induction were evaluated by an increase in caspase-cleaved fragment of keratin-18, caspase-7 activation as well as by reduced expression of matrix metallopeptidase-2 and Ki-67. OxBu efficacy was superior to equimolar 5-fluorouracil solution, and thus the drug should be subjected to the next step in preclinical evaluation.

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Interaction of drug molecules with carrier systems as studied by parelectric spectroscopy and electron spin resonance

Cited by 39 publications

References 25 publications

Recent Advances in Lipid Nanoparticle Formulations with Solid Matrix for Oral Drug Delivery

Recent Advances in Lipid Nanoparticle Formulations with Solid Matrix for Oral Drug Delivery

Drug Release and Skin Penetration from Solid Lipid Nanoparticles and a Base Cream: A Systematic Approach from a Comparison of Three Glucocorticoids

Improving Topical Non-Melanoma Skin Cancer Treatment: In vitro Efficacy of a Novel Guanosine-Analog Phosphonate

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