Oral delivery of solid lipid nanoparticles: underlining the physicochemical characteristics and physiological condition affecting the lipolysis rate

Mahmoudian, M.R.; Dizaj, Solmaz Maleki; Salatin, Sara; Löbenberg, Raimar; Saadat, Maryam; Islambulchilar, Ziba; Valizadeh, Hadi; Zakeri–Milani, Parvin

doi:10.1080/17425247.2021.1982891

Cited by 10 publications

(5 citation statements)

References 112 publications

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“…Various studies indicated that the oral bioavailability of APIs can be increased when they are formulated in lipid nanoparticles [8][9][10]. It was also reported that lipid formulations can reduce food effects [11].…”

Section: Introductionmentioning

confidence: 99%

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Orodispersible Films: A Delivery Platform for Solid Lipid Nanoparticles?

2021

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To overcome the poor bioavailability observed for many newly developed active pharmaceutical ingredients (APIs), an appropriate formulation strategy is necessary. One approach is the formulation of these substances in solid lipid nanoparticles and their further processing into solid dosage forms. A promising and innovative oral delivery platform could be orodispersible films (ODFs). ODFs were already investigated more closely, e.g., for the administration of API nanoparticles, and proved their suitability for this formulation approach. The current study was aimed at investigating if the HPMC (hydroxypropyl methyl cellulose) film matrix is also suitable to serve as an appropriate delivery platform for solid lipid nanoparticles. Dependent on the type of triglyceride nanoparticles embedded in the film matrix and the formulation of the lipid particles, lipid contents of up to 54 wt.% could be realized in the film matrix without the loss of the nanoparticulate state. Good mechanical properties were confirmed for these films by determining the tensile strength as well as the elongation before breakage. Interestingly, processing of a lipid suspension into this solid dosage form led to a significantly reduced transformation of the lipid particles from the metastable α- into the stable β-polymorph. This could prove very beneficial when the lipid particles are loaded with APIs.

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Section: Introductionmentioning

confidence: 99%

“…From these mixed micelles, the API is assumed to be directly absorbed together with the lipid. The secretion of bile salts may additionally enhance the solubilization of orally applied, poorly water-soluble APIs, and thus enable their direct absorption [9,10,12,13].…”

Section: Introductionmentioning

confidence: 99%

Orodispersible Films: A Delivery Platform for Solid Lipid Nanoparticles?

2021

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“…It should be possible to access both the affordability and the viability of the production method. [2][3][4] SLN has been offered as an option for dispersions, liposomes, and polymeric microparticles. Figure 1 depicts the first-generation (SLN) and second-generation (NLC) lipid nanocarriers.…”

Section: Introductionmentioning

confidence: 99%

Nanostructured Lipid Carriers: A Potential Era of Drug Delivery Systems

Chinthaginjala,

Bogavalli,

Hindustan

et al. 2023

Ind. J. Pharm. Edu. Res

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Nanotechnology is rapidly evolving in the development of new drug delivery systems. Nanostructured lipid carriers are the second era of Solid Lipid Nanoparticles (SLN). These are the alternative carrier system over the solid lipid nanoparticles. Nanostructured lipid carriers are composed of a mixture of solid and liquid lipids, resulting in a solely crystallized lipid system with various advantages over solid lipid nanoparticles, such as higher drug entrapment efficiency, drug release modification versatility, and improved stability. Lipid biocompatibility is responsible for their evolution as a viable drug delivery technology. It was observed that it had superior qualities to other lipid compositions. Various drug-distribution technologies have arisen in the last few decades, with the improvement of nanoscale drug-delivery devices being a fascinating component of this. This review explains the nanostructured lipid carriers in terms of structure, fabrication methods, characterization, future developments, wide applications, patents, and benefits over first-generation lipid nanoparticles. The review is primarily concerned with the forthcoming view of nanostructured lipid carriers and their specificity for various physiological affinities. Several polymers have been used in the development of nanoparticles for drug delivery research to maximize medicinal effectiveness while limiting negative effects. Because of their biological non-toxicity, non-immunogenicity, and compatibility, nanostructured lipid carriers will be the most intensively studied lipid nanocarrier systems.

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“…Recent studies have investigated the approach of formulating poorly water-soluble APIs in lipid dispersions and embedding those in the film matrix. This could be more beneficial, because it is assumed that a formulation in lipids could positively affect the bioavailability and adsorption of the poorly water-soluble drugs in the gastro intestinal tract [ 18 , 19 ] and reduce food effects [ 20 ]. So far, only melatonin particles have been dispersed in tristearin microparticles or hydrogenated castor oil and further processed into ODFs with maltodextrin used as the film-forming matrix [ 21 ].…”

Section: Introductionmentioning

confidence: 99%

Embedding of Poorly Water-Soluble Drugs in Orodispersible Films—Comparison of Five Formulation Strategies

2022

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The poor bioavailability of many newly developed active pharmaceutical ingredients (APIs) poses a major challenge in formulation development. To overcome this issue, strategies such as the preparation of amorphous solid dispersions (ASDs), and the application of the APIs in lipid nanocarriers or the wet-milling of the substances into nanoparticles have been introduced. In addition to an efficient formulation strategy, a dosage form that is accepted by all patients is also of great importance. To enable a simple application of the oral dosage form for all patients, orodispersible films (ODFs) are a very promising delivery platform for the APIs because the films directly disintegrate in the mouth. In this study, two poorly water-soluble APIs, fenofibrate and naproxen, were formulated using five different formulation strategies and then embedded in ODFs. It was found that the deliverable amount of API with one ODF highly depends on the formulation strategy as well as the physicochemical properties of the formulated API. The most promising film formulations were ASD-ODFs as well as films with API-loaded lipid nanoemulsions. Both showed a reduction of the dissolution time of the APIs from the ODF compared to an ODF with unformulated API micro particles. In addition, short disintegration times were achieved, although the mechanical film properties were slightly worse compared to the API-free film formulation.

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Oral delivery of solid lipid nanoparticles: underlining the physicochemical characteristics and physiological condition affecting the lipolysis rate

Cited by 10 publications

References 112 publications

Orodispersible Films: A Delivery Platform for Solid Lipid Nanoparticles?

Orodispersible Films: A Delivery Platform for Solid Lipid Nanoparticles?

Nanostructured Lipid Carriers: A Potential Era of Drug Delivery Systems

Embedding of Poorly Water-Soluble Drugs in Orodispersible Films—Comparison of Five Formulation Strategies

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