Pharmacokinetic aspects and in vitro–in vivo correlation potential for lipid-based formulations

Kollipara, Sivacharan; Gandhi, Rajesh

doi:10.1016/j.apsb.2014.09.001

Cited by 93 publications

(59 citation statements)

References 100 publications

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“…The formation of lipoprotein induces lymphatic transport for the highly lipophilic drug. The compounds processed by intestinal lymph are transported to the systemic circulation in association with the lipid core of lipoprotein (Kollipara & Gandhi, 2014). Among the lipids used in SEDDS, long-chain fatty acids are converted to triglyceride by re-esterification in the small intestine and incorporated into chylomicron, a large lipoprotein, followed by secretion into the lymph vessel by exocytosis.…”

Section: Lipidsmentioning

confidence: 99%

Controversies with self-emulsifying drug delivery system from pharmacokinetic point of view

et al. 2016

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Self-emulsifying drug delivery system (SEDDS) is an isotropic mixture of lipid, surfactant and co-surfactant, which forms a fine emulsion when comes in contact of an aqueous medium with mild agitation. SEDDS is considered as a potential platform for oral delivery of hydrophobic drug in order to overcome their poor and irregular bioavailability challenges. In spite of fewer advantages like improved solubility of drug, bypassing lymphatic transport etc., SEDDS faces different controversial issues such as the use of appropriate terminology (self-microemulsifying drug delivery system; SMEDDS or self-nanoemulsifying drug delivery system; SNEDDS), presence of high amount of surfactant, correlation of in vitro model to in vivo studies, lack of human volunteer study and effect of conversion of SEDDS to final administrable dosage form on pharmacokinetic behavior of the drug. In this review, potential issues or questions on SEDDS are identified and summarized from the pharmacokinetic point of view. Primarily this review includes the conflict between the influences of droplet size, variation in correlation between in vitro lipolysis or ex-vivo intestinal permeation and pharmacokinetic parameters, variation in in vivo results of solid and liquid SEDDS, and potential challenges or limitation of pharmacokinetic studies on human volunteers with orally administered SEDDS. In the past decades, hundreds of in vivo studies on SEDDS have been published. In the present study, only the relevant article on in vivo pharmacokinetic studies with orally administered SEDDS published in past 5-6 years are analyzed for an up to date compilation. KeywordsPoor bioavailability, self-nanoemulsifying delivery system, self-microemulsifying delivery system, in vitro lipolysis, pharmacokinetic of SEDDS History

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Section: Lipidsmentioning

confidence: 99%

Controversies with self-emulsifying drug delivery system from pharmacokinetic point of view

et al. 2016

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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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“…With the advent of several emerging novel chemical entities, delivery of high molecular weight and poorly soluble bioactive molecules remains a challenging task. Therapeutic efficacy of low soluble molecules (BCS Class II and IV) is generally high and hence the design of oral delivery systems with improved dissolution and permeability characteristics cannot be ignored [ 1 ] However, poor solubility characters pose greater inter/intra subject variabilities and dose disproportionalities. Yet, most of the novel strategies still remain open for developing versatile oral drug delivery systems since the route of administration is salient [ 2 , 3 ].…”

Section: Introductionmentioning

confidence: 99%

Biopharmaceutical insights of particulate emulsified systems - a prospective overview

Katamreddy

Yalavarthi

et al. 2018

Lipids Health Dis

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During the twenty-first century, drug discovery is expanding rapidly and a large number of chemical moieties are recognized. Many of them are poorly soluble and hence related biopharmaceutical constraints are to be addressed systematically. Among novel approaches to resolving biopharmaceutical issues, micro- and nano-emulsified systems serve as the best strategy for delivering both hydrophobic and hydrophilic drugs owing to their greater solubilization and transportation capabilities. Of late, the unique physical and biopharmaceutical properties of these liquid isotropic homogenous systems have gained substantive research importance. In addition nano/micro lipid systems share structural and functional similarity with that of the physiological lipids which offer better tolerance ability in the body. In this context, this article provides information on the historical emergence of particulate emulsified systems, importance and rationale of selection of carriers. It also encompasses the physicochemical principles that are responsible for the elevation of therapeutic outcomes of delivery systems. Detailed and schematic absorption of these drug delivery systems is explained here. Gastro-intestinal biochemistry necessary in the understanding of digestion process, lipolytic products formed, micellar structures, enzymes, transporters, mechanism of cell uptake involved after subsequent oral absorption are also emphasized. In addition, this article also explains disposition and pharmacokinetic properties of emulsified systems with real-time therapeutic research outcomes. The influence of biochemical compositions and biopharmaceutical principles on absorption and disposition patterns of ME/NEs was described in the article for the interest of readers and young researchers.

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Pharmacokinetic aspects and in vitro–in vivo correlation potential for lipid-based formulations

Cited by 93 publications

References 100 publications

Controversies with self-emulsifying drug delivery system from pharmacokinetic point of view

Controversies with self-emulsifying drug delivery system from pharmacokinetic point of view

Oral Gentamicin Preparation Using Solidified Lipid Particulate Delivery System

Biopharmaceutical insights of particulate emulsified systems - a prospective overview

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