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Recchia, Joanne; Lurantos, Maria H. A.; Amsden, Jennifer A.; Storey, James R.; Kensil, Charlotte R.

doi:10.1023/a:1016235705448

Cited by 29 publications

(7 citation statements)

References 19 publications

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“…The plot showed a change of slope about the cmc, the value of which was calculated by selecting data well below and above the cmc, fitting these to a pair of straight lines by linear regression, and taking their point of intersection as the cmc. Using this process the cmc was estimated to be 2.09 ± 0.01 mM, a value similar to the excipients taurodeoxycholate (cmc = 1−2 mM), a glycosylated cholic acid derivative (cmc = 1−2 mM), and the semisynthetic saponin DS-1 (cmc = 1.09 mM) 1 Molar reaction enthalpy as a function of the total concentration of 11 in the sample cell as observed during the titration of a micellar PBS solution of 11 (40 mM, 3 μL steps) into 1.4 mL of PBS at 37 °C.…”

Section: Resultsmentioning

confidence: 92%

“…dose, drug/liposaccharide ratio) and in the design of the liposaccharide excipient itself. The potential to modulate the physicochemical properties of the system by altering the length of the Laa alkyl chain and the nature of the sugar moiety 23-25 makes this a highly adaptable synthetic drug delivery system in comparison to methods utilizing natural or semisynthetic agents. ,,,, …”

Section: Resultsmentioning

confidence: 99%

“…Efforts have been made to develop aminoglycosides as oral pharmaceutical products. For instance, Recchia and co-workers concluded that a semisynthetic saponin had potential as a transmucosal delivery agent for the aminoglycosides . The saponin was more effective at drug transport than the structurally similar penetration enhancers sodium glycocholate and glycyrrhizic acid.…”

Section: Introductionmentioning

confidence: 99%

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Design, Synthesis, and Evaluation of a Liposaccharide Drug Delivery Agent: Application to the Gastrointestinal Absorption of Gentamicin

et al. 2004

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The design, synthesis, and evaluation of a liposaccharide (11) for use as an agent to enhance the gastrointestinal absorption of charged, hydrophilic drugs with poor membrane permeability is reported. 11 was designed to possess both surfactant and ion-pairing properties and was conveniently synthesized from d-glucuronic acid (2) and N-Boc-lipoamino acid (5) precursors in eight steps in good yield. Isothermal titration microcalorimetry was used to determine the critical micelle concentration of 11 (in PBS) to be 2.09 +/- 0.01 mM with an enthalpy of demicellization of 4.91 +/- 0.11 kJ/mol. The ability of 11 to enhance the gastrointestinal absorption of the aminoglycoside antibiotic gentamicin (1), a hydrophilic polycation with negligible oral bioavailability, was assessed in vivo using rats. Rats dosed orally with a mixture of 11 (100 mg/kg) and 1 (60 mg/kg) had a statistically significant (P < or = 0.034) increase in Cmax, AUC120, and percent absolute bioavailability (F) compared to control 1 (60 mg/kg) alone. The highest bioavailability (F = 9.1 +/- 2.0%) was achieved by dosing with the mixture 11 (100 mg/kg) and 1 (15 mg/kg). This represents a 6-fold increase in bioavailability compared to the control (F = 1.4 +/- 0.3%). These results suggest that the molar ratio of 1:11 may be critical in optimizing the delivery system, a finding ascribed in part to the ion-pairing properties of 11. The effect of 11 on the gastrointestinal mucosa was assessed using light microscopy to examine tissue samples from rats used in the pharmacokinetic study. No morphological changes were found in either the esophagi or duodena of the rats examined. One rat dosed with 11 (100 mg/kg) and 1 (60 mg/kg) exhibited slight gastric erosion, which could be attributed to 11.

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Section: Resultsmentioning

confidence: 92%

Section: Resultsmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

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Design, Synthesis, and Evaluation of a Liposaccharide Drug Delivery Agent: Application to the Gastrointestinal Absorption of Gentamicin

et al. 2004

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“…Purified Quillaja extract are also used to prepare nucleic acid from WBC (white blood cell) [ 155 ]. Saponin DS-1 which is produced from saponin QS-21 are extensively used for increase ocular and nasal delivery of insulin [ 156 ]. Saponin DS-1 also enhance the mucosal delivery of antibacterial agent aminoglycosides which are used to treat peritonitis and pneumonia caused by gram-negative bacteria [ 157 ].…”

Section: Plant Based Surfactant: Saponins and Its Potential Applicati...mentioning

confidence: 99%

Comprehensive Review on Applications of Surfactants in Vaccine Formulation, Therapeutic and Cosmetic Pharmacy and Prevention of Pulmonary Failure due to COVID-19

et al. 2022

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Our world is under serious threat of environmental degradation, climate change and in association with this the out breaks of diseases as pandemics. The devastating impact of the very recent COVID-19, The sharp increase in cases of Cancer, Pulmonary failure, Heart health has triggered questions for the sustainable development of pharmaceutical and medical sciences. In the search of inclusive and effective strategies to meet today’s demand, improvised methodologies and alternative green chemical, bio-based precursors are being introduced by scientists around the globe. In this extensive review we have presented the potentiality and Realtime applications of both synthetic and bio-based surfactants in bio-medical and pharmaceutical fields. For their excellent unique amphoteric nature and ability to solubilise in both organic and inorganic drugs, surfactants are one of the most potential candidates for bio-medicinal fields such as dermatology, drug delivery, anticancer treatment, surfactant therapy, vaccine formulation, personal hygiene care and many more. The self-assembly property of surfactants is a very powerful function for drug delivery systems that increases the bio-availability of the poorly aqueous soluble pharmaceutical products by influencing their solubility. Over the decades many researchers have reported the antimicrobial, anti-adhesive, antibiofilm, anti-inflammatory, antioxidant activities of surfactants regarding its utility in medicinal purposes. In some reports surfactants are found to have spermicidal and laxative activity too. This comprehensive report is targeted to enlighten the versatile applications of Surfactants in drug delivery, vaccine formulation, Cancer Treatment, Therapeutic and cosmetic Pharmaceutical Sciences and prevention of pulmonary failure due to COVID-19.

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“…Previously, we have confirmed that aminoglycosides have a low minimum inhibitory concentration for recently isolated H. pylori , including major drug-resistant strains [ 7 ]. However, aminoglycosides are polar, water-soluble compounds with very poor intestinal membrane permeability, resulting in low oral bioavailability [ 8 , 9 ]. Therefore, we used smectite clay, comprising tetrahedral sheets of SiO 4 units and octahedral sheets of Al 3+ ions [ 10 ], as a carrier of hydrophilic drugs to synthesize a gentamicin (GM)-intercalated smectite hybrid (S-GM) as a novel therapeutic agent.…”

Section: Introductionmentioning

confidence: 99%

Efficacy and Gut Dysbiosis of Gentamicin-Intercalated Smectite as a New Therapeutic Agent against Helicobacter pylori in a Mouse Model

et al. 2020

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Helicobacter pylori eradication rate with conventional standard therapy is decreasing owing to antibiotic resistance, necessitating novel antibacterial strategies against H. pylori. We evaluated the efficacy of a gentamicin-intercalated smectite hybrid (S-GM)-based treatment and analyzed fecal microbiome composition in H. pylori-infected mice. To evaluate anti-H. pylori efficacy, mice were divided into eight groups, and H. pylori eradication was assessed by a Campylobacter-like organism (CLO) test and PCR assay of H. pylori in gastric mucosa. One week after H. pylori eradication, pro-inflammatory cytokine levels and atrophic changes in gastric mucosa were examined. Stool specimens were collected and analyzed for microbiome changes. The S-GM-based triple regimen decreased bacterial burden in vivo, compared with that in untreated mice or mice treated with other regimens. The therapeutic reactions in the CLO test from gastric mucosa were both 90% in the standard triple therapy and S-GM therapy group, respectively. Those of H. pylori PCR in mouse gastric mucosa were significantly lower in standard triple therapy and S-GM therapy groups than in the non-treatment group. Toxicity test results showed that S-GM therapy reduced IL-8 level and atrophic changes in gastric mucosa. Stool microbiome analysis revealed that compared with mice treated with the standard triple therapy, mice treated with the S-GM therapy showed microbiome diversity and abundant microorganisms at the phylum level. Our results suggested that S-GM is a promising and effective therapeutic agent against H. pylori infection.

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Abstract: DS-1 has potential as a transmucosal delivery agent for the aminoglycoside antibiotics.

Cited by 29 publications

References 19 publications

Design, Synthesis, and Evaluation of a Liposaccharide Drug Delivery Agent: Application to the Gastrointestinal Absorption of Gentamicin

Design, Synthesis, and Evaluation of a Liposaccharide Drug Delivery Agent: Application to the Gastrointestinal Absorption of Gentamicin

Comprehensive Review on Applications of Surfactants in Vaccine Formulation, Therapeutic and Cosmetic Pharmacy and Prevention of Pulmonary Failure due to COVID-19

Efficacy and Gut Dysbiosis of Gentamicin-Intercalated Smectite as a New Therapeutic Agent against Helicobacter pylori in a Mouse Model

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