Exploring LIPIDs for their potential to improves bioavailability of lipophilic drugs candidates: A review

Preeti,; Sambhakar, Sharda; Saharan, Renu; Narwal, Sonia; Malik, Rohit; Gahlot, Vinod; Khalid, Asaad; Najmi, Asim; Zoghebi, Khalid; Halawi, Maryam A.; Albratty, Mohammed; Mohan, Syam

doi:10.1016/j.jsps.2023.101870

Cited by 15 publications

(11 citation statements)

References 128 publications

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“…The FA has been classified on its saturation level as very long chain (20 : 0–24 : 0), long chain (12 : 0–18 : 0), medium chain (8 : 0–10 : 0), and short chain (4 : 0–6 : 0). In the design and development of LBDDS, medium- and long-chain triglycerides lipids/oils with variable degree of saturation or hydrolysis have been widely used [ 126 – 130 ]. Epidemiological studies of saturated FA content have manifested a low occurrence of coronary heart diseases in the population even though they ingest a diet that is high in.…”

Section: Oral Bioavailability Enhancement Approachesmentioning

confidence: 99%

“…Long-chain PUFA acts as antihypertensive agent and decreases the possibilities for unfavorable cardiovascular disease by increasing the production of vasodilator prostaglandins. Long chain PUFA also shows their activity as inhibitor of angiotensin converting (AC) enzyme [ 129 , 130 ].…”

Section: Oral Bioavailability Enhancement Approachesmentioning

confidence: 99%

“…The melting points of oils increase with the chain length of fatty acid and decrease with the degree of unsaturation, which also increases susceptibility to oxidation. Isolation of natural oils into glycerides fraction is further used to prepare excipients that maximize desired physical and drug fascination promising properties which reduces susceptibility to oxidation [ 130 , 131 ]. Semisynthetic Lipids .…”

Section: Oral Bioavailability Enhancement Approachesmentioning

confidence: 99%

“…These lipids were finding their application as a vehicle for drug solubilization, wetting agents, surfactant, and cosurfactant in various SEDDS or SMEDDS formulation. These lipids were well-suited for both the hard and soft HPMC capsules [ 130 ]. Synthetic Lipid .…”

Section: Oral Bioavailability Enhancement Approachesmentioning

confidence: 99%

“…Many out of them are nontoxic and glycolic in nature and they are used as a vehicle for poorly aqueous soluble drugs. They can be used alone or in combination with others lipids to enhance the solubilization of formulation such as polyethylene glycol, propylene glycols, and poloxamers [ 130 ].…”

Section: Oral Bioavailability Enhancement Approachesmentioning

confidence: 99%

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Lipid Horizons: Recent Advances and Future Prospects in LBDDS for Oral Administration of Antihypertensive Agents

Preeti,

Sambhakar,

Malik

et al. 2024

International Journal of Hypertension

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The lipid-based drug delivery system (LBDDS) is a well-established technique that is anticipated to bring about comprehensive transformations in the pharmaceutical field, impacting the management and administration of drugs, as well as treatment and diagnosis. Various LBDDSs verified to be an efficacious mechanism for monitoring hypertension systems are SEDDS (self-nano emulsifying drug delivery), nanoemulsion, microemulsions, vesicular systems (transferosomes and liposomes), and solid lipid nanoparticles. LBDDSs overcome the shortcomings that are associated with antihypertensive agents because around fifty percent of the antihypertensive agents experience a few drawbacks including short half-life because of hepatic first-pass metabolism, poor aqueous solubility, low permeation rate, and undesirable side effects. This review emphasizes antihypertensive agents that were encapsulated into the lipid carrier to improve their poor oral bioavailability. Incorporating cutting-edge technologies such as nanotechnology and targeted drug delivery, LBDDS holds promise in addressing the multifactorial nature of hypertension. By fine-tuning drug release profiles and enhancing drug uptake at specific sites, LBDDS can potentially target renin-angiotensin-aldosterone system components, sympathetic nervous system pathways, and endothelial dysfunction, all of which play crucial roles in hypertension pathophysiology. The future of hypertension management using LBDDS is promising, with ongoing reviews focusing on precision medicine approaches, improved biocompatibility, and reduced toxicity. As we delve deeper into understanding the intricate mechanisms underlying hypertension, LBDDS offers a pathway to develop next-generation antihypertensive therapies that are safer, more effective, and tailored to individual patient needs.

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Section: Oral Bioavailability Enhancement Approachesmentioning

confidence: 99%

Section: Oral Bioavailability Enhancement Approachesmentioning

confidence: 99%

Section: Oral Bioavailability Enhancement Approachesmentioning

confidence: 99%

Section: Oral Bioavailability Enhancement Approachesmentioning

confidence: 99%

Section: Oral Bioavailability Enhancement Approachesmentioning

confidence: 99%

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Lipid Horizons: Recent Advances and Future Prospects in LBDDS for Oral Administration of Antihypertensive Agents

Preeti,

Sambhakar,

Malik

et al. 2024

International Journal of Hypertension

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Pilot and feasibility study of dietary composition with elexacaftor‐tezacaftor‐ivacaftor concentrations in people with cystic fibrosis

Rose,

Bailey,

Anderson

et al. 2024

Pharmacotherapy

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BackgroundNutritional support for people with cystic fibrosis (PwCF) after the implementation of novel drug therapies is shifting from managing malnutrition through a high‐fat, high‐calorie diet to managing emerging incidences of obesity in this population. Additionally, dietary recommendations prescribed with elexacaftor/tezacaftor/ivacaftor (ETI) recommend taking this drug with a fat‐containing meal, which is variably interpreted by patients. This pilot and feasibility study was conducted to assess dietary fat intake and body composition on ETI plasma concentrations.MethodsTen participants were enrolled in a 1:1 crossover design by dietary recommendations. To mimic recommendations made during routine clinical care, participants were instructed to consume either a general healthful diet (no more than 30% calories from fat) or a high‐fat diet (>40% calories from fat) for a week before crossing over to the alternative diet.ResultsThis pilot study was acceptable to and feasible for study participants. Most participants increased fat intake calories when following a high‐fat diet. Body composition measurements showed a trending correlation between lean mass and fat‐free mass with ETI plasma concentrations. ETI compounds were quantified in plasma at 0 h (prior to the ETI morning dose) and 6 h after ingestion, and consuming a high‐fat diet did not significantly impact ETI concentrations.ConclusionsConsuming a higher‐fat diet did not significantly impact ETI plasma concentrations, and all participants were in range for clinical effectiveness of ETI regardless of fat intake. This work provides vital pilot data to design larger studies to clarify dietary composition for optimal ETI exposure for PwCF on this therapy.

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Therapeutic Peptides and Proteins: Stabilization Challenges and Biomedical Applications by Means of Nanodelivery Systems

Berselli,

Coccolini,

Tosi

et al. 2024

Int J Pept Res Ther

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The delivery of peptides and proteins usually faces formulation development challenges attributed to the difficulties encountered in their stabilization. Nanoparticles offer an alternative to improve the physicochemical stability of such biomacromolecules, while increasing their bioavailability by overcoming biological absorption barriers. With this review, we aim to discuss the stability problems of proteins and peptides that have driven the scientific community to find in nanotechnology a valid alternative for oral administration of biomolecules. In addition, we describe the most commonly used nanoparticles for this purpose (e.g., polymers such as polylactic acid, poly(lactic-co-glycolic acid), polycaprolactone, modified chitosan, and lipids such as oil-in-water nanoemulsions, self-emulsified drug delivery systems, solid lipid nanoparticles, nanostructured lipid carriers, liposomes, as well as hybrid systems like micelles), and we show some of the most important recent applications of these nanoparticles for the delivery of proteins and peptides, including for the treatment of diabetes, viruses (such as HIV), cancer, as well as in the development of vaccines.

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Exploring LIPIDs for their potential to improves bioavailability of lipophilic drugs candidates: A review

Cited by 15 publications

References 128 publications

Lipid Horizons: Recent Advances and Future Prospects in LBDDS for Oral Administration of Antihypertensive Agents

Lipid Horizons: Recent Advances and Future Prospects in LBDDS for Oral Administration of Antihypertensive Agents

Pilot and feasibility study of dietary composition with elexacaftor‐tezacaftor‐ivacaftor concentrations in people with cystic fibrosis

Therapeutic Peptides and Proteins: Stabilization Challenges and Biomedical Applications by Means of Nanodelivery Systems

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