Efficient dermal delivery of retinyl palmitate: Progressive polarimetry and Raman spectroscopy to evaluate the structure and efficacy

Lee, Jun Bae; Lee, Dong Ryeol; Choi, Nak Cho; Jang, Jihui; Park, Chun Ho; Yoon, Moung Seok; Lee, Mi-Young; Won, Kyu Yeoun; Hwang, Jae Sung; Kim, Byeong Moon

doi:10.1016/j.ejps.2015.07.009

Cited by 9 publications

(4 citation statements)

References 44 publications

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“…This was attributed to the similarity of the structures of LCs and SC leading to easy distribution as well as to the efficient hydration effects of LCs, as compared with the emulsion. 80 , 81 The NSAIDs, including diclofenac diethylamine or ibuprofen lysinate, are organic acids with amphiphilic properties and, at room or body temperature, form LLC mesophases in aqueous solution. 82…”

Section: Llcs In Formulationsmentioning

confidence: 99%

Oral and transdermal drug delivery systems: role of lipid-based lyotropic liquid crystals

Rajabalaya

Musa

Kifli

et al. 2017

DDDT

105

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Liquid crystal (LC) dosage forms, particularly those using lipid-based lyotropic LCs (LLCs), have generated considerable interest as potential drug delivery systems. LCs have the physical properties of liquids but retain some of the structural characteristics of crystalline solids. They are compatible with hydrophobic and hydrophilic compounds of many different classes and can protect even biologicals and nucleic acids from degradation. This review, focused on research conducted over the past 5 years, discusses the structural evaluation of LCs and their effects in drug formulations. The structural classification of LLCs into lamellar, hexagonal and micellar cubic phases is described. The structures of these phases are influenced by the addition of surfactants, which include a variety of nontoxic, biodegradable lipids; these also enhance drug solubility. LLC structure influences drug localization, particle size and viscosity, which, in turn, determine drug delivery properties. Through several specific examples, we describe the applications of LLCs in oral and topical drug formulations, the latter including transdermal and ocular delivery. In oral LLC formulations, micelle compositions and the resulting LLC structures can determine drug solubilization and stability as well as intestinal transport and absorption. Similarly, in topical LLC formulations, composition can influence whether the drug is retained in the skin or delivered transdermally. Owing to their enhancement of drug stability and promotion of controlled drug delivery, LLCs are becoming increasingly popular in pharmaceutical formulations.

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Section: Llcs In Formulationsmentioning

confidence: 99%

Oral and transdermal drug delivery systems: role of lipid-based lyotropic liquid crystals

Rajabalaya

Musa

Kifli

et al. 2017

DDDT

105

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“…These techniques probe only at the macroscopic level, however, and the nature and composition of the cream's internal interfaces and the nature of the ordered systems that gives rise to the birefringence can only be inferred and not proven. In like manner, researchers use wide-angle X-ray scattering 12 and differential scanning calorimetry 10,[13][14][15][16] to provide details of the phase state and lateral organisation of a cream's excipients but neither of these techniques can inform as to the nature of the aggregates formed by the excipients and they cannot be used to pinpoint their microstructural loci.…”

mentioning

confidence: 99%

Revealing the Hidden Details of Nanostructure in a Pharmaceutical Cream

Ahmadi

Mahmoudi

et al. 2020

Sci Rep

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Creams are multi-component semi-solid emulsions that find widespread utility across a wide range of pharmaceutical, cosmetic, and personal care products, and they also feature prominently in veterinary preparations and processed foodstuffs. The internal architectures of these systems, however, have to date been inferred largely through macroscopic and/or indirect experimental observations and so they are not well-characterized at the molecular level. Moreover, while their long-term stability and shelflife, and their aesthetics and functional utility are critically dependent upon their molecular structure, there is no real understanding yet of the structural mechanisms that underlie the potential destabilizing effects of additives like drugs, anti-oxidants or preservatives, and no structure-based rationale to guide product formulation. In the research reported here we sought to address these deficiencies, making particular use of small-angle neutron scattering and exploiting the device of H/D contrast variation, with complementary studies also performed using bright-field and polarised light microscopy, smallangle and wide-angle X-ray scattering, and steady-state shear rheology measurements. through the convolved findings from these studies we have secured a finely detailed picture of the molecular structure of creams based on Aqueous Cream BP, and our findings reveal that the structure is quite different from the generic picture of cream structure that is widely accepted and reproduced in textbooks. Oil-in-water creams are widely used in pharmaceutical products formulated to treat conditions like atopic dermatitis, rosacea and psoriasis 1. They also form the basis of veterinary medications used to assist wound-healing and treat skin infections 2 , and they are the basis too of a great many personal care products, spanning make-up foundations, anti-perspirants, sun lotions and deodorants 3. All such products are complex, multi-component colloids in which the constituent oil and water phases are stabilised through the addition of one or more ionic, non-ionic or zwitterionic surfactants, in combination with one or more co-surfactants (sometimes referred to as consistency enhancers) which might be long chain fatty acids, fatty alcohols or monoglycerides 4,5. Other components which might be added include humectants such as propylene glycol, anti-oxidants like α-tocopherol acetate, and preservatives like phenoxyethanol 6. The molecular architecture of any given cream formulation will clearly vary according to its chemical composition, and this in turn will determine its chemical and physical stability, and also impact the cream's sensory aesthetics and efficacy as a cosmetic, pharmaceutical, or veterinary product. Despite much research into the properties of creams and their many years of use, however, our understanding of their internal molecular structure is still far from complete, with the unavoidable consequence, therefore, that they are still formulated only in a semi-empirical manner. Junginger and co-workers 7 ...

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“…To investigate the origin of this dramatic enhancement in skin efficacy through the usage of the DC formulation, we acquired the Raman fingerprint spectra from the top of the skin to a depth of 24 μm using a confocal Raman spectrometer to determine the penetration depth and rate. 3,12,27–29 Acquisition of the spectra at three different time intervals, before application ( T 0 ), immediately after application ( T 20 , 20 min after application), and after absorption ( T 60 , 60 min after application), for the NC and DC formulations shows that the DC formulation more deeply and rapidly permeates through the skin's outermost SC layer, as evidenced by the permeation depth immediately after application ( T 20 ) which is 18 and 20 μm for NC and DC, respectively (Fig. 6b and c).…”

Section: Resultsmentioning

confidence: 97%

Microencapsulation of alcohol solvents and high-content actives for efficient transdermal delivery

Lee,

Hwang,

Noh

et al. 2023

Biomater. Sci.

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Efficient dermal delivery of retinyl palmitate: Progressive polarimetry and Raman spectroscopy to evaluate the structure and efficacy

Cited by 9 publications

References 44 publications

Oral and transdermal drug delivery systems: role of lipid-based lyotropic liquid crystals

Oral and transdermal drug delivery systems: role of lipid-based lyotropic liquid crystals

Revealing the Hidden Details of Nanostructure in a Pharmaceutical Cream

Microencapsulation of alcohol solvents and high-content actives for efficient transdermal delivery

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