Improved intestinal delivery of salmon calcitonin by water-in-oil microemulsions

Fan, Yixuan; Li, Xinru; Zhou, Yanxia; Fan, Chao; Wang, Xiaoning; Huang, Yanqing; Liu, Yan

doi:10.1016/j.ijpharm.2011.06.029

Cited by 32 publications

(19 citation statements)

References 38 publications

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“…10 It has also been reported that W/O-MEs can protect salmon calcitonin from proteolysis and acidic degradation, thus enhancing its absorption in the gastrointestinal tract. 11 Therefore, MEs have been suggested to positively influence drug absorption in a number of ways, such as protecting the incorporated drugs from oxidation and enzymatic degradation 12 and enhancing membrane permeability and lymphatic transport. 2 Lymphatic transport is thought to make a significant contribution to absorption from the intestine as it circumvents the hepatic first-pass effect.…”

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confidence: 99%

Mechanisms of microemulsion enhancing the oral bioavailability of puerarin: comparison between oil-in-water and water-in-oil microemulsions using the single-pass intestinal perfusion method and a chylomicron flow blocking approach

Tang¹,

Hu²,

Liao³

et al. 2013

IJN

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The purpose of the present work was to determine the mechanisms by which microemulsions (MEs) enhance the oral bioavailability of puerarin. The in situ perfusion method was used in rats to study the absorption mechanisms of an oil-in-water (O/W) microemulsion (O/W-ME) and a water-in-oil (W/O) microemulsion (W/O-ME). The possibility of lymphatic transport of the MEs was investigated using a chylomicron flow blocking approach. The results for the absorption mechanisms in the stomach and intestines indicated that the absorption characteristics of the O/W-ME and W/O-ME depend on the segment. The W/O-ME had higher internal membrane permeability than the O/W-ME. The results of the lymphatic transport analyses showed that both the O/W-ME and W/O-ME underwent lymphatic transport and that this pathway was a major contributor to the oral bioavailability of MEs. Furthermore, the type of ME can significantly affect the absorption of puerarin through the lymphatic system due to the oil content and the form of the microemulsion after oral administration. In conclusion, these data indicate that microemulsions are an effective and promising delivery system to enhance the oral bioavailability of poorly water-soluble drugs.

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mentioning

confidence: 99%

Mechanisms of microemulsion enhancing the oral bioavailability of puerarin: comparison between oil-in-water and water-in-oil microemulsions using the single-pass intestinal perfusion method and a chylomicron flow blocking approach

Tang¹,

Hu²,

Liao³

et al. 2013

IJN

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“…The process is thermodynamically driven by the requirement of surfactant to maintain an aqueous phase concentration equivalent to its critical micelle concentration (CMC). In the present investigation (dispersibility test), distilled water was used as a dispersion medium because it is widely reported that there is no significant difference in the formulation prepared using nonionic surfactants, dispersed in either water, SGF or SIF [33][34][35].…”

Section: Resultsmentioning

confidence: 99%

Oral Gentamicin Preparation Using Solidified Lipid Particulate Delivery System

Adedokun

Jackson

Uchegbu

et al. 2017

Int J Pharm Pharm Sci

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Objective: Despite the broad pharmacological activity of gentamicin against a number of bacteria, it's very inadequate oral bioavailability due to poor intestinal membrane permeability has limited its formulation into oral dosage delivery system. This work was thus aimed at formulation and evaluation of gentamicin-loaded microemulsions based on preparation of lipid matrix for sustained release delivery. Methods:Oral gentamicin suspensions were prepared by emulsification method using Tween 80 as a mobile surfactant in the lipid matrix dispersion. The resultant oral suspensions were evaluated for mean particle size and morphology using a photomicrograph, encapsulation efficiency/entrapment, EE (%), dispersibility, pH and absolute drug content. Release study as a function of inhibition zone diameter (IZD) and in vitro release study was also carried out. The in vitro release study was performed in both simulated gastric fluid (pH 1.2) and simulated intestinal fluid (pH 7.2) respectively. The release data were analyzed mathematically according to zero order, first order and Higuchi equations. Results:The prepared suspensions were cream-white in colour, easily dispersed and well homogenized. Batch D, which had least amount of excipients incorporated into the lipid matrix showed clumped irregular-shaped and less free-flowing particles. The particle size was significantly influenced by lipid matrix combination ratio in the presence of a surfactant (p<0.05). The mean particle size diameters of the samples were 15.44 mm, 10.64 mm, 4.12 mm, and 2.70 mm for batches A, B, C and D respectively. The values of EE obtained varied between 47% and 59% with Batch B exhibiting the highest value. The Higuchi model gave the best release kinetics result followed by zero order kinetics. Conclusion:Oral gentamicin prepared exhibited antibacterial properties against Klebsiella spp., Escherchia coli, Bacillus subtilis, Staphylococcus aureus, and Pseudomonas aeruginosa. The results suggest that a lipid matrix system could be useful as a sustained release oral delivery system of a poorly absorbable drug such as gentamicin.

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“…Intestinal delivery of peptides and proteins has been reported (35), but most of the reports have focused on the improvement of systemic absorption. There are quite limited reports on the local intestinal delivery of peptides or proteins for the treatment of local pathologies, like IBDs.…”

Section: In Vivo Studies For Intestinal Deliverymentioning

confidence: 99%

In Vitro and In Vivo Evaluation of a Water-in-Oil Microemulsion System for Enhanced Peptide Intestinal Delivery

Liu

Russo

et al. 2012

AAPS J

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Abstract. Peptide and protein drugs have become the new generation of therapeutics, yet most of them are only available as injections, and reports on oral local intestinal delivery of peptides and proteins are quite limited. The aim of this work was to develop and evaluate a water-in-oil (w/o) microemulsion system in vitro and in vivo for local intestinal delivery of water-soluble peptides after oral administration. A fluorescent labeled peptide, 5-(and-6)-carboxytetramethylrhodamine labeled HIV transactivator protein TAT (TAMRA-TAT), was used as a model peptide. Water-in-oil microemulsions consisting of Miglyol 812, Capmul MCM, Tween 80, and water were developed and characterized in terms of appearance, viscosity, conductivity, morphology, and particle size analysis. TAMRA-TAT was loaded and its enzymatic stability was assessed in modified simulated intestinal fluid (MSIF) in vitro. In in vivo studies, TAMRA-TAT intestinal distribution was evaluated using fluorescence microscopy after TAMRA-TAT microemulsion, TAMRA-TAT solution, and placebo microemulsion were orally gavaged to mice. The half-life of TAMRA-TAT in microemulsion was enhanced nearly three-fold compared to that in the water solution when challenged by MSIF. The treatment with TAMRA-TAT microemulsion after oral administration resulted in greater fluorescence intensity in all intestine sections (duodenum, jejunum, ileum, and colon) compared to TAMRA-TAT solution or placebo microemulsion. The in vitro and in vivo studies together suggested TAMRA-TAT was better protected in the w/o microemulsion in an enzyme-containing environment, suggesting that the w/o microemulsions developed in this study may serve as a potential delivery vehicle for local intestinal delivery of peptides or proteins after oral administration.

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Improved intestinal delivery of salmon calcitonin by water-in-oil microemulsions

Cited by 32 publications

References 38 publications

Mechanisms of microemulsion enhancing the oral bioavailability of puerarin: comparison between oil-in-water and water-in-oil microemulsions using the single-pass intestinal perfusion method and a chylomicron flow blocking approach

Mechanisms of microemulsion enhancing the oral bioavailability of puerarin: comparison between oil-in-water and water-in-oil microemulsions using the single-pass intestinal perfusion method and a chylomicron flow blocking approach

Oral Gentamicin Preparation Using Solidified Lipid Particulate Delivery System

In Vitro and In Vivo Evaluation of a Water-in-Oil Microemulsion System for Enhanced Peptide Intestinal Delivery

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