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Production of single cell oil by Lipomyces starkeyi from waste plant oil generated by the palm oil mill industry

Zain NA, Kahar P, Sudesh K, Ogino C, Kondo A

J Biosci Bioeng, 2024 Aug;138(2):153-162.
PMID: 38777650 DOI: 10.1016/j.jbiosc.2024.04.005

Only a few reports available about the assimilation of hydrophobic or oil-based feedstock as carbon sources by Lipomyces starkeyi. In this study, the ability of L. starkeyi to efficiently utilize free fatty acids (FFAs) and real biomass like palm acid oil (PAO) as well as crude palm kernel oil (CPKO) for growth and lipid production was investigated. PAO, CPKO, and FFAs were evaluated as sole carbon sources or in the mixed medium containing glucose. L. starkeyi was able to grow on the medium supplemented with PAO and FFAs, which contained long-chain length FAs and accumulated lipids up to 35% (w/w) of its dry cell weight. The highest lipid content and lipid concentration were achieved at 50% (w/w) and 10.1 g/L, respectively, when L. starkeyi was cultured in nitrogen-limited mineral medium (-NMM) supplemented with PAO emulsion. Hydrophobic substrate like PAO could be served as promising carbon source for L. starkeyi.

Matched MeSH terms: Lipids/chemistry
Correlating gastric emptying of amphotericin B and paracetamol solid lipid nanoparticles with changes in particle surface chemistry

Amekyeh H, Billa N, Roberts C

Int J Pharm, 2017 Jan 30;517(1-2):42-49.
PMID: 27923696 DOI: 10.1016/j.ijpharm.2016.12.001

Oral delivery of pharmaceuticals requires that they retain their physical and chemical attributes during transit within the gastrointestinal (GI) tract, for the manifestation of desired therapeutic profiles. Solid lipid nanoparticles (SLNs) are used as carriers to improve the absorption of hydrophobic drugs. In this study, we examine the stability of amphotericin B (AmB) and paracetamol (PAR) SLNs in simulated GI fluids during gastric emptying. On contact with the simulated fluids, the particles increased in size due to ingress of the dissolution media into the particles. Simulated gastric emptying revealed that the formulations had mean sizes <350nm and neutral surface charges, both of which are optimal for intestinal absorption of SLNs. There was ingress of the fluids into the SLNs, followed by diffusion of the dissolved drug, whose rate depended on the solubility of the loaded-drug in the particular medium. Time-of-flight secondary ion mass spectrometry analyses indicated that drug loading followed the core-shell model and that the AmB SLNs have a more drug-enriched core than the PAR SLNs do. The AmB SLNs are therefore a very suitable carrier of AmB for oral delivery. The stability of the SLNs in the simulated GI media indicates their suitability for oral delivery.

Matched MeSH terms: Lipids/chemistry*
Novel drug delivery approaches in treating pulmonary fibrosis

Dua K, Awasthi R, Madan JR, Chellappan DK, Nalluri BN, Gupta G, et al.

Panminerva Med, 2018 Dec;60(4):238-240.
PMID: 29480673 DOI: 10.23736/S0031-0808.18.03428-6
Matched MeSH terms: Lipids/chemistry
Lipid-based pulmonary delivery system: a review and future considerations of formulation strategies and limitations

Ngan CL, Asmawi AA

Drug Deliv Transl Res, 2018 10;8(5):1527-1544.
PMID: 29881970 DOI: 10.1007/s13346-018-0550-4

Inhalation therapy of lipid-based carriers has great potential in direct target towards the root of respiratory diseases, which make them superior over other drug deliveries. With the successful entry of lipid carriers into the target cells, drugs can be absorbed in a sustained release manner and yield extended medicinal effects. Nevertheless, translation of inhalation therapy from laboratory to clinic especially in drug delivery remains a key challenge to the formulators. An ideal drug vehicle should safeguard the drugs from any premature elimination, facilitate cellular uptake, and promote maximum drug absorption with negligible toxicity. Despite knowing that lung treatment can be done via systemic delivery, pulmonary administration is capable of enhancing drug retention within the lungs, while minimizing systemic toxicity with local targeting. Current inhalation therapy of lipid-based carriers can be administered either intratracheally or intranasally to reach deep lung. However, the complex dimensions of lung architectural and natural defense mechanism poise major barriers towards targeted pulmonary delivery. Delivery systems have to be engineered in a way to tackle various diseases according to their biological conditions. This review highlights on the developmental considerations of lipid-based delivery systems cater for the pulmonary intervention of different lung illnesses.

Matched MeSH terms: Lipids/chemistry
Fulltext Peroxisome proliferator-activated receptor gamma: promising target in glioblastoma

Gupta G, Singhvi G, Chellappan DK, Sharma S, Mishra A, Dahiya R, et al.

Panminerva Med, 2018 Sep;60(3):109-116.
PMID: 30176701 DOI: 10.23736/S0031-0808.18.03462-6

Glioblastoma, also known as glioblastoma multiforme, is the most common and worldwide-spread cancer that begins within the brain. Glioblastomas represent 15% of brain tumors. The most common length of survival following diagnosis is 12 to 14 months with less than 3% to 5% of people surviving longer than five years. Without treatment, survival is typically 3 months. Among all receptors, special attention has been focused on the role of peroxisome proliferator-activated receptors (PPARs) in glioblastoma. PPARs are ligand-activated intracellular transcription factors. The PPAR subfamily consists of three subtypes encoded by distinct genes named PPARα, PPARβ/δ, and PPARγ. PPARγ is the most extensively studied subtype of PPAR. There has been interesting preliminary evidence suggesting that diabetic patients receiving PPARγ agonists, a group of anti-diabetics, thiazolidinedione drugs, have an increased median survival for glioblastoma. In this paper, the recent progresses in understanding the potential mechanism of PPARγ in glioblastoma are summarized.

Matched MeSH terms: Lipids/chemistry
Pharmacokinetics and tissue distribution of an orally administered mucoadhesive chitosan-coated amphotericin B-Loaded nanostructured lipid carrier (NLC) in rats

Tan JSL, Roberts C, Billa N

J Biomater Sci Polym Ed, 2020 02;31(2):141-154.
PMID: 31612804 DOI: 10.1080/09205063.2019.1680926

Oral delivery of amphotericin B (AmpB) is desirable because it provides a more patient-friendly mode of administration compared to the current delivery approach akin with the marketed AmpB formulations. The goal of the study was to investigate the pharmacokinetics and tissue distribution of orally administered chitosan-coated AmpB-loaded nanostructured lipid carriers (ChiAmpB NLC) administered to Sprague Dawley rats at a dose of 15 mg/kg. Orally administered ChiAmpB NLC resulted in a two-fold increase in the area under the curve (AUC0-∞) compared to the uncoated AmpB NLC and marketed Amphotret®. This enhanced bioavailability of AmpB suggests prolonged transit and retention of ChiAmpB NLC within the small intestine through mucoadhesion and subsequent absorption by the lymphatic pathway. The results show that mean absorption and residence times (MAT & MRT) were significantly higher from ChiAmpB NLC compared to the other two formulations, attesting to the mucoadhesive effect. The ChiAmpB NLC presented a lower nephrotic accumulation with preferential deposition in liver and spleen. Thus, the limitations of current marketed IV formulations of AmpB are potentially addressed with the ChiAmpB NLC in addition to utilizing this approach for targeting internal organs in visceral leishmaniasis.

Matched MeSH terms: Lipids/chemistry*
Fulltext Effects of Seasonal Variability on the Physicochemical, Biochemical, and Nutritional Composition of Western Peninsular Malaysia Gracilaria manilaensis

Aroyehun AQ, Palaniveloo K, Ghazali F, Rizman-Idid M, Abdul Razak S

Molecules, 2019 Sep 10;24(18).
PMID: 31510066 DOI: 10.3390/molecules24183298

This study evaluated the effect of seasonal variation on the physicochemical, biochemical, and nutritional composition of Gracilaria manilaensis. Sampling was designed during the main monsoon seasons in Malaysia-the Southwest monsoon (SWM) and Northeast monsoon (NEM)-to understand the intraspecific variation (p < 0.05). Carbohydrates, protein, and dietary fiber were found to be higher in NEM-G. manilaensis, whereas a higher ash content was quantified in SWM-G. manilaensis. No significant differences were found in crude lipid and moisture content (p > 0.05). Vitamin B2 was calculated as (0.29 ± 0.06 mg 100 g-1) and (0.38 ± 0.06 mg 100 g-1) for the NEM and SWM samples, respectively (p < 0.05). The fatty acid profile showed the dominance of saturated fatty acids (SFAs)-palmitic acids, stearic acid, and myristic acid-while the mineral contents were found to be good sources of calcium (1750.97-4047.74 mg 100 g-1) and iron (1512.55-1346.05 mg 100 g-1). Tryptophan and lysine were recorded as the limiting essential amino acids (EAAs) in NEM G. manilaensis, while leucine and phenylalanine were found to be the limiting EAAs in the SWM samples. None of the extracts exhibited antibacterial properties against the screened strains. The study concluded that seasonal changes have a great effect on the biochemical composition of G. manilaensis.

Matched MeSH terms: Lipids/chemistry
Fulltext Pharmacokinetics and Biodistribution of Thymoquinone-loaded Nanostructured Lipid Carrier After Oral and Intravenous Administration into Rats

Zakarial Ansar FH, Latifah SY, Wan Kamal WHB, Khong KC, Ng Y, Foong JN, et al.

Int J Nanomedicine, 2020;15:7703-7717.
PMID: 33116496 DOI: 10.2147/IJN.S262395

Background: Thymoquinone (TQ), an active compound isolated from Nigella sativa, has been proven to exhibit various biological properties such as antioxidant. Although oral delivery of TQ is valuable, it is limited by poor oral bioavailability and low solubility. Recently, TQ-loaded nanostructured lipid carrier (TQ-NLC) was formulated with the aim of overcoming the limitations. TQ-NLC was successfully synthesized by the high-pressure homogenization method with remarkable physiochemical properties whereby the particle size is less than 100 nm, improved encapsulation efficiency and is stable up to 24 months of storage. Nevertheless, the pharmacokinetics and biodistribution of TQ-NLC have not been studied. This study determined the bioavailability of oral and intravenous administration of thymoquinone-loaded nanostructured lipid carrier (TQ-NLC) in rats and its distribution to organs.
Materials and Methods: TQ-NLC was radiolabeled with technetium-99m before the administration to the rats. The biodistribution and pharmacokinetics parameters were then evaluated at various time points. The rats were imaged at time intervals and the percentage of the injected dose/gram (%ID/g) in blood and each organ was analyzed.
Results: Oral administration of TQ-NLC exhibited greater relative bioavailability compared to intravenous administration. It is postulated that the movement of TQ-NLC through the intestinal lymphatic system bypasses the first metabolism and therefore enhances the relative bioavailability. However, oral administration has a slower absorption rate compared to intravenous administration where the AUC0-∞ was 4.539 times lower than the latter.
Conclusion: TQ-NLC had better absorption when administered intravenously compared to oral administration. However, oral administration showed greater bioavailability compared to the intravenous route. This study provides the pharmacokinetics and biodistribution profile of TQ-NLC in vivo which is useful to assist researchers in clinical use.

Matched MeSH terms: Lipids/chemistry
Fulltext Redirecting Metabolic Flux towards the Mevalonate Pathway for Enhanced β-Carotene Production in M. circinelloides CBS 277.49

Naz T, Nazir Y, Nosheen S, Ullah S, Halim H, Fazili ABA, et al.

Biomed Res Int, 2020;2020:8890269.
PMID: 33457420 DOI: 10.1155/2020/8890269

Carotenoids produced by microbial sources are of industrial and medicinal importance due to their antioxidant and anticancer properties. In the current study, optimization of β-carotene production in M. circinelloides strain 277.49 was achieved using response surface methodology (RSM). Cerulenin and ketoconazole were used to inhibit fatty acids and the sterol biosynthesis pathway, respectively, in order to enhance β-carotene production by diverting metabolic pool towards the mevalonate pathway. All three variables used in screening experiments were found to be significant for the production of β-carotene. The synergistic effect of the C/N ratio, cerulenin, and ketoconazole was further evaluated and optimized for superior β-carotene production using central composite design of RSM. Our results found that the synergistic combination of C/N ratios, cerulenin, and ketoconazole at different concentrations affected the β-carotene productions significantly. The optimal production medium (std. order 11) composed of C/N 25, 10 μg/mL cerulenin, and 150 mg/L ketoconazole, producing maximum β-carotene of 4.26 mg/L (0.43 mg/g) which was 157% greater in comparison to unoptimized medium (1.68 mg/L, 0.17 mg/g). So, it was concluded that metabolic flux had been successfully redirected towards the mevalonate pathway for enhanced β-carotene production in CBS 277.49.

Matched MeSH terms: Lipids/chemistry
Acute and subacute toxicity profiles of thymoquinone-loaded nanostructured lipid carrier in BALB/c mice

Ong YS, Saiful Yazan L, Ng WK, Noordin MM, Sapuan S, Foo JB, et al.

Int J Nanomedicine, 2016 11 09;11:5905-5915.
PMID: 27877037

BACKGROUND: Thymoquinone (TQ), the predominant active lipophilic component in Nigella sativa seed oil, has a variety of pharmacological properties such as anticancer activities. However, translation of TQ to clinical phase is still not possible due to its hydrophobic properties. This problem can be solved by encapsulating it in nanoformulations to enhance its pharmacological properties. In our previous study, TQ has been successfully encapsulated in a nanostructured lipid carrier (hereinafter referred to as TQNLC) with excellent physiochemical properties such as high encapsulation efficiency, high drug-loading capacity, particle diameter less than 100 nm, and stability up to 2 years. In vitro studies also proved that TQNLC exhibited antiproliferative activity toward breast and cervical cancer cell lines. However, no toxicity profile related to this formulation has been reported. In this study, we determine and compare the in vivo toxicity of both TQNLC and TQ.
MATERIALS AND METHODS: The in vivo toxicity (acute and subacute toxicity) study was carried out by oral administration of TQNLC and TQ to BALB/c mice. Animal survival, body weight, organ weight-to-body weight ratio, hematological profile, biochemistry profile, and histopathological changes were analyzed.
RESULTS: In acute toxicity, TQ that is loaded in nanostructured lipid carrier (NLC) was found to be less toxic than pure TQ. It can be concluded that encapsulation of TQ in lipid carrier minimizes the toxicity of the compound. In the subacute toxicity study, oral administration of 100 mg/kg of TQNLC and TQ did not cause mortality to either male or female but resulted in toxicity to the liver. It is postulated that long-term consumption of TQNLC and TQ may cause toxicity to the liver but not to the extent of altering the functions of the organ. For both treatments, the no observed adverse effect level (NOAEL) was found to be 10 mg/kg/d for mice in both sexes.
CONCLUSION: For long-term oral consumption, TQ and TQNLC at a dose of 10 mg/kg is safe in mice and does not exert any toxic effect. The results provide safety information of TQNLC, which would further help researchers in clinical use.

Matched MeSH terms: Lipids/chemistry*
Fulltext Effect of compositions in nanostructured lipid carriers (NLC) on skin hydration and occlusion

Loo Ch, Basri M, Ismail R, Lau H, Tejo B, Kanthimathi M, et al.

Int J Nanomedicine, 2013;8:13-22.
PMID: 23293516 DOI: 10.2147/IJN.S35648

To study the effects of varying lipid concentrations, lipid and oil ratio, and the addition of propylene glycol and lecithin on the long-term physical stability of nanostructured lipid nanocarriers (NLC), skin hydration, and transepidermal water loss.

Matched MeSH terms: Lipids/chemistry*
Consumption of repeatedly heated soy oil increases the serum parameters related to atherosclerosis in ovariectomized rats

Adam SK, Das S, Soelaiman IN, Umar NA, Jaarin K

Tohoku J Exp Med, 2008 Jul;215(3):219-26.
PMID: 18648182

Repeated heating of soy oil may promote lipid peroxidation. Oxidized unsaturated fatty acids may contribute to the pathogenesis of atherosclerosis, especially in estrogen-deficient states. This study was performed to explore the deleterious effects of repeatedly heated soy oil on the development of atherosclerosis using ovariectomized rats, which represent an estrogen-deficient state. Twenty-four female Sprague-Dawley rats were ovariectomized and were divided equally into four groups. The control group was fed with 2% cholesterol diet without any oil. The three treatment groups each received 2% cholesterol diet fortified with fresh, once-heated or five-times-heated (repeatedly heated) soy oil, respectively. Serum thiobarbituric acid reactive substances (TBARS), lipid profile and homocysteine levels were measured prior to ovariectomy and at the end of four months. Ovariectomized rats treated with repeatedly heated soy oil showed significant increases in lipid peroxidation and low-density lipoprotein (LDL) levels. Treatment with once-heated or repeatedly heated soy oil caused a significant increase in total cholesterol, while fresh soy oil caused significant reduction in homocysteine level as compared to other groups. Repeatedly heated soy oil caused significant increases in TBARS and LDL as compared to fresh oil. The higher level of homocysteine in the ovariectomized rats fed with repeatedly heated oil, as compared to those fed with fresh oil, also suggests the repeatedly heated oil contributes to the development of atherosclerosis. Importantly, the protective effect of the soy oil may be lost once it was being repeatedly heated. In conclusion, the consumption of repeatedly heated oil may predispose to atherosclerosis in estrogen-deficient states.

Matched MeSH terms: Lipids/chemistry
The oil of Adenanthera pavonina L. seeds and its emulsions

Zarnowski R, Jaromin A, Certik M, Czabany T, Fontaine J, Jakubik T, et al.

Z Naturforsch C J Biosci, 2008 11 13;59(5-6):321-6.
PMID: 18998394

The oil of Adenanthera pavonina L. seeds was analysed by chromatographic and instrumental means. The oil was found to be rich in neutral lipids (86.2%), and low in polar lipids (13.8%). The neutral lipids consisted mainly of triacylglycerols (64.2%). Unsaturated fatty acids were found as high as 71%, while the percentage of saturated fatty acids was only 29%. GC and GC/MS analyses revealed linoleic, oleic and lignocerotic acid to be predominant among all fatty acids in the A. pavonina oil, whereas stigmasterol was the major steroid identified within this study. Subsequently, the oil was used for preparation of submicron oil-in-water (o/w) lipid emulsions. Lipid emulsions were formulated by using soybean lecithin (SL) to investigate their particle size, Zeta potential and stability at the different oil and SL ratios. The results obtained indicate possible applications of the tested oil in pharmaceutical and medical fields as drug and cosmetic active ingredient carriers.

Matched MeSH terms: Lipids/chemistry*
Microbial colonization of medical devices and novel preventive strategies

Shunmugaperumal T

Recent Pat Drug Deliv Formul, 2010 Jun;4(2):153-73.
PMID: 20236065

Upon implantation or insertion into patient's body for exerting the intended purpose like salvage of normal functions of vital organs, the medical devices are unfortunately becoming the sites of competition between host cell integration and microbial adhesion. Moreover, since there is an increased use of implanted medical devices, the incidence of biofilm-and medical devices-related nosocomial infections is also increasing progressively. To control microbial colonization and subsequent biofilm formation of the medical devices, different approaches either to enhance the efficiency of certain antimicrobial agents or to disrupt the basic physiology of the pathogenic microorganisms including novel small molecules and antipathogenic drugs are being explored. In addition, the various lipid-and polymer-based drug delivery carriers are also investigated for applying antibiofilm coating of the medical devices especially over catheters. The main intention of this review is therefore to summarize the major and/breakthrough inventions disclosed in patent literature as well as in research papers related to microbial colonization of medical devices and novel preventive strategies. This review starts with an overview of the preventive strategies followed by a short description about the potential of different lipidic-and polymeric-drug delivery carriers in eradicating the biofilm-associated infections from the medical devices.

Matched MeSH terms: Lipids/chemistry
Production of lipids containing high levels of docosahexaenoic acid by a newly isolated microalga, Aurantiochytrium sp. KRS101

Hong WK, Rairakhwada D, Seo PS, Park SY, Hur BK, Kim CH, et al.

Appl Biochem Biotechnol, 2011 Aug;164(8):1468-80.
PMID: 21424706 DOI: 10.1007/s12010-011-9227-x

In the present study, a novel oleaginous Thraustochytrid containing a high content of docosahexaenoic acid (DHA) was isolated from a mangrove ecosystem in Malaysia. The strain identified as an Aurantiochytrium sp. by 18S rRNA sequencing and named KRS101 used various carbon and nitrogen sources, indicating metabolic versatility. Optimal culture conditions, thus maximizing cell growth, and high levels of lipid and DHA production, were attained using glucose (60 g l⁻¹) as carbon source, corn steep solid (10 g l⁻¹) as nitrogen source, and sea salt (15 g l⁻¹). The highest biomass, lipid, and DHA production of KRS101 upon fed-batch fermentation were 50.2 g l⁻¹ (16.7 g l⁻¹ day⁻¹), 21.8 g l⁻¹ (44% DCW), and 8.8 g l⁻¹ (40% TFA), respectively. Similar values were obtained when a cheap substrate like molasses, rather than glucose, was used as the carbon source (DCW of 52.44 g l⁻¹, lipid and DHA levels of 20.2 and 8.83 g l⁻¹, respectively), indicating that production of microbial oils containing high levels of DHA can be produced economically when the novel strain is used.

Matched MeSH terms: Lipids/chemistry
Fulltext Thymoquinone-loaded nanostructured lipid carrier exhibited cytotoxicity towards breast cancer cell lines (MDA-MB-231 and MCF-7) and cervical cancer cell lines (HeLa and SiHa)

Ng WK, Saiful Yazan L, Yap LH, Wan Nor Hafiza WA, How CW, Abdullah R

Biomed Res Int, 2015;2015:263131.
PMID: 25632388 DOI: 10.1155/2015/263131

Thymoquinone (TQ) has been shown to exhibit antitumor properties. Thymoquinone-loaded nanostructured lipid carrier (TQ-NLC) was developed to improve the bioavailability and cytotoxicity of TQ. This study was conducted to determine the cytotoxic effects of TQ-NLC on breast cancer (MDA-MB-231 and MCF-7) and cervical cancer cell lines (HeLa and SiHa). TQ-NLC was prepared by applying the hot high pressure homogenization technique. The mean particle size of TQ-NLC was 35.66 ± 0.1235 nm with a narrow polydispersity index (PDI) lower than 0.25. The zeta potential of TQ-NLC was greater than -30 mV. Polysorbate 80 helps to increase the stability of TQ-NLC. Differential scanning calorimetry showed that TQ-NLC has a melting point of 56.73°C, which is lower than that of the bulk material. The encapsulation efficiency of TQ in TQ-NLC was 97.63 ± 0.1798% as determined by HPLC analysis. TQ-NLC exhibited antiproliferative activity towards all the cell lines in a dose-dependent manner which was most cytotoxic towards MDA-MB-231 cells. Cell shrinkage was noted following treatment of MDA-MB-231 cells with TQ-NLC with an increase of apoptotic cell population (P < 0.05). TQ-NLC also induced cell cycle arrest. TQ-NLC was most cytotoxic towards MDA-MB-231 cells. It induced apoptosis and cell cycle arrest in the cells.

Matched MeSH terms: Lipids/chemistry*
Transdermal delivery of oxybutynin chloride proniosomal gels for the treatment of overactive bladder

Rajabalaya R, David SR, Chellian J, Xin Yun G, Chakravarthi S

Drug Deliv, 2016 Jun;23(5):1578-87.
PMID: 26634274 DOI: 10.3109/10717544.2015.1116027

CONTEXT: Overactive bladder (OAB) is a common problem and anticholinergic drugs are first-line therapy, but they have side effects.
OBJECTIVE: Development of oxybutynin chloride (OC) proniosomal gels and analyses of its efficacy for OAB treatment.
MATERIALS AND METHODS: Phase separation coacervation was used to prepare proniosomal gels using various non-ionic surfactants, lipids, soy lecithin and isopropyl alcohol. Gels were characterized with regard to entrapment efficiency (EE), vesicle size, surface morphology (using environmental scanning electron microscopy [E-SEM]), stability, attenuated total reflectance Fourier transform infrared (ATR-FTIR) spectroscopy, in vitro skin permeation, in vivo animal studies and histopathology.
RESULTS AND DISCUSSION: EE was 87-92%, vesicle size was 0.38-5.0 μm, and morphology showed some loosened pores in proniosomes after hydration. ATR-FTIR spectroscopy showed no significant shifts in peaks corresponding to OC and excipients. Most formulations exhibited >50% permeation but the cholesterol-containing formulations P3 (Span 20:Span 60 [1:1]) and P4 [Tween 20:Tween 80 (1:1)] had the highest percent cumulative permeation. P3 and P4 also showed faster recovery of cholinergic effects on salivary glands than oral formulations. P3 and P4 had pronounced therapeutic effects in reduction of urinary frequency and demonstrated improvements in bladder morphology (highly regenerative surface of the transitional epithelium).
CONCLUSION: These results suggest that OC could be incorporated into proniosomal gels for transdermal delivery in the treatment of OAB.

Matched MeSH terms: Lipids/chemistry*
Inhalable solid lipid nanoparticles of levofloxacin for potential tuberculosis treatment

Paul PK, Nakpheng T, Paliwal H, Prem Ananth K, Srichana T

Int J Pharm, 2024 Jul 20;660:124309.
PMID: 38848797 DOI: 10.1016/j.ijpharm.2024.124309

Delivering novel antimycobacterial agents through the pulmonary route using nanoparticle-based systems shows promise for treating diseases like tuberculosis. However, creating dry powder inhaler (DPI) with suitable aerodynamic characteristics while preserving nanostructure integrity and maintaining bioactivity until the active ingredient travels deeply into the lungs is a difficult challenge. We developed DPI formulations containing levofloxacin-loaded solid lipid nanoparticles (SLNs) via spray-drying technique with tailored aerosolization characteristics for effective inhalation therapy. A range of biophysical techniques, including transmission electron microscopy, confocal microscopy, and scanning electron microscopy were used to measure the morphologies and sizes of the spray-dried microparticles that explored both the geometric and aerodynamic properties. Spray drying substantially reduced the particle sizes of the SLNs while preserving their nanostructural integrity and enhancing aerosol dispersion with efficient mucus penetration. Despite a slower uptake rate compared to plain SLNs, the polyethylene glycol modified formulations exhibited enhanced cellular uptake in both A549 and NR8383 cell lines. The percent viability of Mycobacterium bovis had dropped to nearly 0 % by day 5 for both types of SLNs. Interestingly, the levofloxacin-loaded SLNs demonstrated a lower minimum bactericidal concentration (0.25 µg/mL) compared with pure levofloxacin (1 µg/mL), which indicated the formulations have potential as effective treatments for tuberculosis.

Matched MeSH terms: Lipids/chemistry
Cubosome-based skin delivery: from topical to transdermal applications

Gunawan M, Efendi A, Ramadon D, Liew CV, Chutoprapat R

Expert Opin Drug Deliv, 2026 Nov;23(11):2059-2087.
PMID: 42779272 DOI: 10.1080/17425247.2026.2739504

INTRODUCTION: Skin delivery provides an alternative drug administration, although its effectiveness is limited by the stratum corneum barrier. Cubosomes, as third-generation lipid nanoparticles with bicontinuous cubic liquid crystalline structures, have emerged as promising nanocarriers that enhance skin penetration, sustain drug release, improve bioavailability, and minimize toxicity.
AREAS COVERED: This review discusses the biopharmaceutical mechanisms of cubosome-mediated skin delivery, including bioadhesion, stratum corneum lipid fluidization, controlled release, enhanced cellular uptake, and improved bioavailability. Literature from 2006-2026 was collected from Scopus, PubMed, and patent databases, covering localized applications such as dermatological disorders, wound healing, fungal infections, alopecia, inflammatory skin diseases, and oncology, as well as systemic therapies including rheumatoid arthritis, gout, diabetes mellitus, and hormone replacement therapy. Recent advances, including microneedle integration, thermosensitive hydrogels, stimuli-responsive systems, and surface-engineered cubosomes, are also highlighted.
EXPERT OPINION: Cubosomes represent a promising platform for advanced skin delivery. Optimal performance depends on the therapeutic goal, with systemic delivery requiring enhanced permeation and sustained absorption, whereas localized therapy prioritizes intradermal retention and tissue depot formation with minimal systemic exposure. Despite strong preclinical evidence, further studies on long-term safety, manufacturing standardization, and clinical validation are essential for successful clinical translation and commercialization of cubosome-based skin delivery.

Matched MeSH terms: Lipids/chemistry
Methotrexate and beta-carotene loaded-lipid polymer hybrid nanoparticles: a preclinical study for breast cancer

Jain A, Sharma G, Kushwah V, Garg NK, Kesharwani P, Ghoshal G, et al.

Nanomedicine (Lond), 2017 Aug;12(15):1851-1872.
PMID: 28703643 DOI: 10.2217/nnm-2017-0011

AIM: This work was intended to investigate the targeting potential of fructose-tethered lipid-polymeric hybrid nanoparticles (F-BC-MTX-LPHNPs) co-loaded with beta carotene (BC) and methotrexate (MTX) in breast cancer therapeutics and find out the possible protective role of BC on MTX-induced toxicity.
MATERIALS & METHODS: F-BC-MTX-LPHNPs were fabricated using self-assembled nano-precipitation technique. Fructose was conjugated on the surface of the particles. The in vitro cytotoxicity, sub-cellular localization and apoptotic activity of F-BC-MTX-LPHNPs were evaluated against MCF-7 breast cancer cells. The antitumor potential of F-BC-MTX-LPHNPs was further studied.
RESULTS & CONCLUSION: Outcomes suggested that F-BC-MTX-LPHNPs induced the highest apoptosis index (0.89) against MCF-7 cells. Following 30 days of treatment, the residual tumor progression was assessed to be approximately 32%, in animals treated with F-BC-MTX-LPHNPs. F-BC-MTX-LPHNPs are competent to selectively convey the chemotherapeutic agent to the breast cancers. Beta carotene ameliorated MTX-induced hepatic and renal toxicity.

Matched MeSH terms: Lipids/chemistry

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