Emulsifying Drug Delivery System Research Articles

Antioxidants Activity of Self-Nanoemulsifying Drug Delivery System on Dayak Onions Extract (Eleutherine palmifolia) using DPPH (2,2 difenil-1- picrylhydrazyl) Method

Dayak onions (Eleutherine palmifolia L. Merr) is one plant that has been proven to have benefits as an antioxidant. The Dayak extract is formulated in the self nano emulsifying drug delivery system (SNEDDS) because the extract has low water solubility. The aims this study to develop the SNEDDS formulation system by testing its antioxidant activity. We determined whether there was an increase in antioxidant activity when formulated in the form of SNEDDS or not. The results were then compared with a solution of Dayak onions extract without using SNEDDS. The obtained formula was the optimal result that has been done before using the D-optimal mixture design method. The results of the components consisted of 50 mg of Dayak extract, 10 % caprylic triglyceride as oil, 1% tween 80, and 6,60 % transcutol as a combination surfactant and 12,40 % propylene glycol as co-surfactant. Antioxidant activity testing was carried out using the DPPH (1,1-Diphenyl-2-picrylhydrazyl) method. The antioxidant test using the DPPH method was done with two samples, namely the extract solution and Dayak onion extract SNEDDS. We elaborated the research by using UV-VIS spectrophotometer. Each sample was made into five concentrations, namely 30 ppm, 60 ppm, 90 ppm, 120 ppm, and 150 ppm, and carried out three times replications. The results showed that the IC50 value in the Dayak onion extract solution was 227,19 ppm (very low), while for the SNEDDS solution for the Dayak onion extract the IC50 value obtained was 38,97 ppm (very strong). The analysis was carried out next using an independent T-Test to obtain the results. There was no significant difference between the extract solution and the SNEDDS solution of Dayak onion extract.

Herbal nanomedicines: Recent advancements, challenges, opportunities and regulatory overview

BackgroundHerbal Nano Medicines (HNMs) are nano-sized medicine containing herbal drugs as extracts, enriched fractions or biomarker constituents. HNMs have certain advantages because of their increased bioavailability and reduced toxicities. There are very few literature reports that address the common challenges of herbal nanoformulations, such as selecting the type/class of nanoformulation for an extract or a phytochemical, selection and optimisation of preparation method and physicochemical parameters. Although researchers have shown more interest in this field in the last decade, there is still an urgent need for systematic analysis of HNMs. PurposeThis review aims to provide the recent advancement in various herbal nanomedicines like polymeric herbal nanoparticles, solid lipid nanoparticles, phytosomes, nano-micelles, self-nano emulsifying drug delivery system, nanofibers, liposomes, dendrimers, ethosomes, nanoemulsion, nanosuspension, and carbon nanotube; their evaluation parameters, challenges, and opportunities. Additionally, regulatory aspects and future perspectives of herbal nanomedicines are also being covered to some extent. MethodsThe scientific data provided in this review article are retrieved by a thorough analysis of numerous research and review articles, textbooks, and patents searched using the electronic search tools like Sci-Finder, ScienceDirect, PubMed, Elsevier, Google Scholar, ACS, Medline Plus and Web of Science. ResultsIn this review, the authors suggested the suitability of nanoformulation for a particular type of extracts or enriched fraction of phytoconstituents based on their solubility and permeability profile (similar to the BCS class of drugs). This review focuses on different strategies for optimising preparation methods for various HNMs to ensure reproducibility in context with all the physicochemical parameters like particle size, surface area, zeta potential, polydispersity index, entrapment efficiency, drug loading, and drug release, along with the consistent therapeutic index. ConclusionA combination of herbal medicine with nanotechnology can be an essential tool for the advancement of herbal medicine research with enhanced bioavailability and fewer toxicities. Despite the challenges related to traditional medicine's safe and effective use, there is huge scope for nanotechnology-based herbal medicines. Overall, it is well stabilized that herbal nanomedicines are safer, have higher bioavailability, and have enhanced therapeutic value than conventional herbal and synthetic drugs.

Optimization and Characterization of Self Nano Emulsifying Drug Delivery System loaded with 18- β Glycerrhetinic acid

The purpose of this study was to prepare, optimize and evaluate self nano emulsifying drug delivery system (SNEDDS) containing 18- β glycerrhetinic acid which enhances the dissolution profile or bioavailability of the drug in comparison to pure suspension of 18- β glycerrhetinic acid.18- β glycerrhetinic acid loaded SNEDDS having geranium oil as oil phase, tween 80 as a surfactant, and dimethyl sulfoxide (DMSO) as co-surfactant were prepared using pseudo ternary phase diagram and Box-Behnken experimental design was used to optimize the different formulations. Optimized formulations were characterized for self-emulsifying time, globule size, zeta potential, and drug release. The mean droplet size and PDI of the optimized formulation were found to be in a variation of 93.42 nm and 0.401 respectively. FTIR data showed no physicochemical interaction between excipients and drug. The encapsulation efficiency of optimised 18- β glycerrhetinic acid SNEDDS was found 80.12±1.52% , % transmittance was found 99.34±0.134% and the viscosity of all the formulations was found 0.8872 cp. Three-dimensional response surface plots and two-dimensional contour plots of the responses across the selected factors were constructed that explained the relationship between the independent and dependent variables. Release kinetics was calculated by using KinetDS3.0. It was concluded that prepared formulations were formulated with approximately desired mean droplet size confirmed by Box- Behnken experimental design as well as properly optimized and characterized.

Novel Self-micro Emulsifying Drug Delivery System for Safe Intramuscular Delivery with Improved Pharmacodynamics and Pharmacokinetics.

Diclofenac Sodium (DS) injection is widely used in the management of acute or chronic pain and inflammatory diseases. It incorporates 20% w/v Transcutol-P as a solubilizer to make the stable injectable formulation. However, the use of Transcutol-P in high concentration leads to adverse effects such as severe nephrotoxicity, etc. Some advancements have resulted in the formulation of an aqueous-based injectable but that too used benzyl alcohol which is reported to be toxic for human use. This study aimed to develop an injectable Self-Micro Emulsifying Drug Delivery System (SMEDDS) as a novel carrier of DS for prompt release with better safety and efficacy. A solubility study was performed with different surfactants and co-surfactants. The conventional stirring method was employed for the formulation of SMEDDS. Detailed in vitro characterization was done for different quality control parameters. In vivo studies were performed using Wistar rats for pharmacokinetic evaluation, toxicological analysis, and analgesic activity. The optimized formulation exhibited good physical stability, ideal globule size (156±0.4 nm), quick release, better therapeutics, and safety, increase in LD50 (221.9 mg/kg) to that of the commercial counterpart (109.9 mg/kg). Furthermore, pre-treatment with optimized formulation reduced the carrageenan-induced rat paw oedema by 88±1.2% after 4 h, compared to 77±1.6% inhibition with commercial DS formulation. Moreover, optimized formulation significantly (p<0.05) inhibited the pain sensation in the acetic-acid induced writhing test in mice compared to its commercial equivalent with a better pharmacokinetic profile. The above findings confirmed that liquid SMEDDS can be a successful carrier for the safe and effective delivery of DS.

Formulation and Optimization of Self Emulsifying Drug Delivery System For Effective Anthelmintic Therapy

The present study aims to develop and optimize a self-emulsifying drug delivery system for paediatric patients to improve the oral bioavailability of the anthelmintic drug, Praziquantel (PZQ) and to perform it’s in-vitro dissolution study. The solubility of PZQ was estimated in various vehicles to select proper component combination. Capmul MCM (oil), Cremophore RH40 (surfactant) and PEG400 (co-surfactant) were employed to construct pseudo-ternary phase diagrams. Eight formulations composed of Capmul MCM, at Smix ratios (1:1, 2:1 &amp; 3:1) were selected. The optimized formulation F7 has a mean globule size 14.73 nm with a negative zeta potential -44.43 mV. The results indicated that PZQ loaded SEDDS, showed enhanced solubilization and nanosizing potential to improve the absorption of the drug.

Chemometric Approach to Assess Response Correlation and its Classification in simplex centroid design for Pre-Optimization stage of Catechin-SNEDDS

Catechins are isolated from tea leaves and shown to have pharmacological activities. However, the permeability and absorption capacity of the digestive tract is low, thus affecting the value of bioavailability. Self-nano emulsifying drug delivery system (SNEDDS) is formulated as a breakthrough in nano delivery to increase the value of bioavailability and stability in a model of natural compounds, namely catechins. This study applies chemometrics to the simplex centroid design (SCD) to analyze the catechin-SNEDDS pre-optimization design. The factors defined include oleic acid, croduret 50-SS, and propylene glycol. Evaluation parameters include emulsification time, percent transmittance (%T), freeze-thaw, and endurance test. The results showed a formula that met the requirements at the time of emulsification, stability, and %T. There were four clusters of results from the principal component analysis - cluster analysis (PCA-CA) in the SCD formula. The evaluation between responses in the SCD optimization design is indicated to have a positive correlation. Analysis using multivariate chemometric can describe the characteristics of each formula and the response based on the parameters used, which refers to the similarity, grouping, and correlation of each formula and response. The PCA-CA technique can group formulas from SCD in similar clusters and provide important information regarding response patterns or correlations.

Formulation and Evaluation of Solid Self Nano Emulsifying drug delivery System of Olanzapine to Enhance Aqueous Solubility and Dissolution Rate

Present research work was aimed to enhance aqueous solubility and dissolution rate of olanzapine by solid self nano emulsifying drug delivery system(S-SNEDDS). Olanzapine is a BCS class II drug having 65% oral bioavailability; it is used in the treatment of psychosis, depression and mania conditions. Oils, Surfactants, Co surfactants were selected depending upon the saturated solubility of olanzapine in those components; excipients were screened depending on olanzapine solubility in various oils, surfactants and co surfactants. Surfactant: co surfactant {Smix} ratios i.e., 3:1 and 4:1 were prepared to determine nano emulsion regions and also to formulate liquid self nano emulsifying drug delivery system (L-SNEDDS). Pseudo ternary phase diagram were plotted by using Triplot version 4.1.2 software, nano emulsion region was determined and evaluated. Formulations were designed based on saturated solubility of olanzapine and Pseudo ternary phase diagram using various ratios of oils [Capryol 90], surfactants [Kolliphor EL], co surfactants [Lauroglycol 90] depending on its solubility and nano emulsion formation four formulations were developed which are further selected for characterisation of L-SNEDDS like robustness to dilution, self emulsification, determination of droplet size, PDI, Drug loading efficacy, zeta potential and also Invitro drug release. Among those four formulations, F1 (SB184J 4:6) was optimum because compared to other three formulations F3 gave best results in terms of droplet size (66nm) with PDI (0.24), Invitro drug release, dissolution rate of F1 SNEDDS having (88.201± 0.25%). Invitro drug release of F1 formulation was compared with that of Olanzapine [API] (45.281± 0.52%) the results indicating that there is a increase in solubility and dissolution rate of olanzapine by 2.2 times more compared to pure olanzapine (API). F1 (SB184J 4:6) were converted into S-SNEDDS by adsorption process by addition porous carriers (Aerosil 200). Formulated S-SNEDDS were undergone various evaluation parameters and also reconstitution parameters to determine Droplet size and Invitro drug release of solid F1 (SB184J4:6) formulation. The results of present study demonstrates that olanzapine SNEDDS has an ability and potential to enhance solubility and dissolution rate.

Stability Study of Super Saturable Catechin-Self Nano Emulsifying Drug Delivery System as Antidiabetic Therapy

Diabetes mellitus is a metabolic syndrome characterized by hyperglycemic and increased ROS production, which causes oxidative stress. Catechin isolated from the tea plant has oxidative stress inhibitor activity and anti-diabetic activity with low absorption in circulation systemic. Therefore, it is formulated in a super saturable catechin-self nano emulsifying drug delivery system (SSC-SNEDDS). Stability is one of the factors that affect the safety, quality, and efficacy of SSC-SNEDDS. This study aims to evaluate the stability of the formulated oil phase using oleic acid, croduret as a surfactant, and propylene glycol as a co-surfactant. Stability studies were carried out by several tests, namely heating-cooling cycle assay, freeze-thaw cycle assay, centrifugation, and endurance assay. Droplet characterization in the form of changes in diameter, zeta potential, and mobility in evaluating stability tests using dynamic light scattering-particle size analyzer (DLS-PSA). Real-time stability was also evaluated by observing changes in the infrared spectrum pattern using FTIR-ATR. After the stability test, the emulsion droplet size of SSC-SNEDDS was still below 100 nm and showed good stability. It can be concluded that the formula has a good stability profile.

Formulation And Antioxidant Property Of Bitter Melon Seeds Oil Loaded Into SNEDDS Systems As A Nutraceutical

Bitter melon seeds oil is less soluble in the gastrointestinal tract and has low absorption. Therefore, a self-nanoemulsion dosage form needed to support its absorption and increase its stability. This study aimed to formulate bitter melon seeds oil into a self-nano emulsifying drug delivery system (SNEDDS) and evaluate its antioxidant activity using the Ferric Reducing Antioxidant Power (FRAP) method. The SNEDDS formulation uses bitter melon seed oil as the active ingredient and the oil phase, cremophor RH 40 as a surfactant, and glycerin as a co-surfactant. The results showed that the best SNEDDS formula obtains a ratio of oil: Smix (surfactant mixture) of 1:4. The best formula transmittance was 97.35 ± 0.04% with an emulsification time of 15.69 ± 0.06 seconds, a pH value of 6.87 ± 0.08, and a particle size of 31.8 ± 16.3 nm. Thermodynamic stability and robustness to dilution tests show the preparation is stable and resistant to various dilutions and pH. The antioxidant activity of bitter melon seed oil before and after being formulated into SNEDDS resulted in 62.73% and 50.31% reducing power. This result is not differences significantly. This study concluded that bitter melon seeds oil SNEDDS has good physical characteristics, stability, and no antioxidant activity changes.

A Literature Review on Self Nanoemulsifying Drug Delivery System (SNEDDS)

The Lipid-based drug delivery system is extensively reported within the literature for the enhancing drug solubility, permeability, and bioavailability. A considerable majority of novel pharmacologically active constituents produced in recent drug discovery programs are lipophilic and poorly soluble, posing a significant problem for pharmaceutical researchers enhancing the oral bioavailability of such drug molecules. Self-nano emulsifying drug delivery systems (SNEDDS), are the viable oil-based approaches for drugs that exhibit low dissolution rate and inadequate absorption. Ever since the progress of SNEDDS, researchers have been focusing on the challenges of BCS Class II and Class IV Drugs for enhancing water Solubility of poorly water-soluble drugs. SNEDDS is a Validate method for enhancing the solubility and bioavailability of lipophilic compounds. It’s the isotropic mixture of oil, surfactant, co-surfactant molecules and it also containing co-solvent molecule. which spontaneously form oil-in-water nano emulsion of approximately 200 nm or less in size upon dilution with water under gentle stirring. It’s Drug delivery system Which possess thermodynamically and kinetically stability. The physicochemical properties, drug solubilization capacity considerably regulates the selection of the SNEDDS components. The compositions of the SNEDDS are often optimized with the assistance of phase diagrams. Further to optimize SNEDDS can be done with the help of statistical experimental design. It’s a Novel drug delivery system which is applicable for the parenteral, Ophthalmic, intranasal and cosmetic drug delivery system. And therefore, the present review describes Preparation, components, mechanism of self-Nano emulsification, biopharmaceutical aspects, characterization methods and applications of Selfnanoemulsifying drug delivery system (SNEDDS).

Enhancement of solubility of paclitaxel by applying factorial design

Background: The poor aqueous solubility and low bioavailability of antineoplastic drugs restrict the oral route for the cancer therapy. However, specific nanotechnologies developed to address this issue. The self-micro emulsifying drug delivery system (SMEDDS) is an imperative tool in solving a lipophilic drug's low solubility and bioavailability issue. Paclitaxel (PTX) is an antineoplastic drug used to treat various kinds of cancer, especially ovarian and breast cancers. It has low aqueous solubility (0.3 μg/ml in water), resulting in poor bioavailability. This study focuses upon formulating SMEDDS incorporating PTX to increase the drug's aqueous solubility. Castor oil (Surfactant), Tween 80 (surfactant), and Transcutol (co-surfactant) were used to formulate SMEDDS. Two independent factors, concentrations of oil and surfactant, were chosen. Two dependent factors, emulsification time and in vitro drug release, were chosen. 32 factorial design analyses give a mathematical expression, which helps to study the effect of an independent factor on a dependent factor. All the nine formulations B1-B9 evaluated for globule size, zeta potential, and present drug content. Results: The globule size found is 127–217 nm range, which indicates the formation of the transparent microemulsion; zeta potential fields between −4.29 ± 1.1 and −33.05 ± 4.5 indicate suitable stable formulation. Nearly 63%–84% drug content suggests that the drug, incorporated into prepared SMEDDS. Statistical analysis shows that an increasing amount of surfactant decreases emulsification time; this may also reduce the average droplet size of the resultant microemulsion. With the increase in the concentration of tween 80, PTX release also increased. Rapid and more extent of PTX released from formulated SMEDDS indicate that the aqueous solubility of PTX has increased. B9 formulation is the optimized formulation based on higher per cent cumulative drug release 98% at the end of 60 min, 58% of pure PTX powder solubilized in the dissolution medium. Conclusion: In vitro drug release study proved that the prepared SMEDDS has acceptable properties of immediate release dosage forms. The enhanced solubility of PTX will increase its bioavailability.

Double w/o/w self-nano emulsifying drug delivery system of imatinib mesylate for colon cancer treatment

The aim of the research was to prepare & evaluate double w/o/w self-nano emulsifying drug delivery system (SNEDDS) of imatinib mesylate (IMT) and to investigates its anticancer activity against MDST8 human colon carcinoma cell lines. The self-nano emulsifying drug delivery system was prepared by the aqueous phase titration method. After the necessary screening, the optimized formulation (F-SEN-5) was characterized for surface morphology, using high-resolution transmission electron microscopy (Philips CM 120 BioTwin, U.S.A.). Furthermore, average droplet diameter (Δdm), polydispersity index (PDI), refractive index (Ri), viscosity (η), percentage transmittance (%T), percentage drug content (% DC), In-vitro drug release studies were measured for all the formulations; The optimized F-SEN-5 shows R2 = 0.9987, n (0.5 < n < 1.0) = 0.732, indicating the Korsmeyer-Peppas drug release model and anomalous transport. The higher drug release profile (99.42 ± 5.23%) at 60 min, higher transmittance (%) (98.56 ± 0.56%), low viscosity (28.67 ± 3.67cps), low PDI (0.078 ± 0.05), low average droplet diameter (47.56 ± 5.78 nm) at 2:1 Smix ratio. The in-vitro cytotoxicity (%) and IC50 value of F-SEN-5 while treating MDST8 human colon carcinoma cell lines were found to be 93.71 ± 8.11% and 15 µM. The formulation provides an additional 20% more efficiency than the free IMT drug. Overall, these findings suggested that double w/o/w nanoemulsions can be successfully used for SNEDDS of IMT for chemoprevention of colon cancer.

DESIGN AND EVALUATION OF SELF-NANO EMULSIFYING DRUG DELIVERY SYSTEMS OF ALVERINE FOR ENHANCEMENT OF SOLUBILITY

Background: The aim of this study is to develop a liquid self-nano emulsifying drug delivery system for alverine (liquid-SNEDDS).Excipients in the alverine SNEDDS include Ethyl oleate as the oil phase, Tween 80 as a surfactant, and PEG600, Propylene glycol as a cosurfactant.The prepared eleven formulations of alverine SNEDDS were performed for emulsification time, percentage transmittance, particle size, drug release, in vitro dissolution and stability studies.The optimised alverine liquid SNEDDS formulation (D1) was studied for drug-excipient compatibility using infrared spectroscopy, as well as particle size, zeta potential, transmission electron microscopy, and stability. Alverine SNEDDS have a spherical shape with uniform particle distribution, according to their morphology. D1's optimised formulation's drug release percentage (96.6). The stability data revealed no discernible changes in drug content, emulsifying properties, drug release, or appearance. As a result, a potential SNEDDS formulation of alverine with improved solubility, dissolution rate, and bioavailability was developed.

Colloidal and vesicular delivery system for herbal bioactive constituents.

The main objective of the present review is to explore and examine the effectiveness of currently developed novel techniques to resolve the issues which are associated with the herbal constituents/extract. A systematic thorough search and collection of reviewed information from Science direct, PubMed and Google Scholar databases based on various sets of key phrases have been performed. All the findings from these data have been studied and briefed based on their relevant and irrelevant information. Herbal drugs are gaining more popularity in the modern world due to their applications in curing various ailments with minimum toxic effects, side effect or adverse effect. However, various challenges exist with herbal extracts/plant actives such as poor solubility (water/lipid), poor permeation, lack of targeting specificity, instability in highly acidic pH, and liver metabolism, etc. Nowadays with the expansion in the technology, novel drug delivery system provides avenues and newer opportunity towards the delivery of herbal drugs with improved physical chemical properties, pharmacokinetic and pharmacodynamic. Developing nano-strategies like Polymeric nanoparticles, Liposomes, Niosomes, Microspheres, Phytosomes, Nanoemulsion and Self Nano Emulsifying Drug Delivery System, etc. imparts benefits for delivery of phyto formulation and herbal bioactives. Nano formulation of phytoconstituents/ herbal extract could lead to enhancement of aqueous solubility, dissolution, bioavailability, stability, reduce toxicity, permeation, sustained delivery, protection from enzymatic degradation, etc. CONCLUSION: Based on the above findings, the conclusion can be drawn that the nano sized novel drug delivery systems of herbal and herbal bioactives have a potential future for upgrading the pharmacological action and defeating or overcoming the issues related with these constituents. The aims of the present review was to summarize and critically analyze the recent development of nano sized strategies for promising phytochemicals delivery systems along with their therapeutic applications supported by experimental evidence and discussing the opportunities for further aspects.

A Systemic Review on the Self Micro Emulsifying Drug Delivery System

Comfort direction and painless method made oral route the most favored. Mainstream of recent active constituents have less oral bioavailability because of dissolution rate limited absorption. While many inventive methods like complexation, cocrystals exist, solid dispersions, pH modification and, lipid-based delivery systems conclusively improved appliance with the seeming rise in drug absorption. Among lipid-based formulations, self-micro emulsifying formulations (SMEDDS) (droplet size &lt; 100 nm) are evident to enhance permeation across intestinal membrane, protection of drug against gastric effect, unit dosage is possible, increased bioavailability of drug, reduces the dose of drug etc. Numerous components are used to formulate these dosage forms like Oil, surfactants, Co-surfactant and lipids mixture contribute to the enhancement in oral bioavailability through promoting the lymphatic passage; thus, hepatic first pass metabolism can be overcoming. The present review highlights comprehensive information on the formulation design, probable mechanisms and characterization of SMEDDS

Formulation and Evaluation of Self Nano Emulsifying Drug Delivery System of Raloxifene Hydrochloride

Raloxifene hydrochloride (RLX) is a selective Estrogen-receptor modulator used to treat osteoporosis as well as breast and endometrial cancer prevention. The bioavailability of RLX is only 2% due to substantial pre-systemic clearance. The goal of this research was to customise and characterise RLX-loaded self-nanoemulsifying drug-delivery systems (SNEDDS) by using bioactive excipients that impact drug metabolism. The droplet size, zeta potential and drug content determination of optimized formulation (F-06) was found to be 147.5 nm, -28.8, 99.67% respectively. The drug release study from the nano formulation was studied in Phosphate buffer 6.8 for all the formulations F1,F2,F3,F4,F5,F6 and F7. The optimized formulation was found to be F6&#x0D; Keywords: Raloxifene hydrochloride, nanoemulsion, SNEDDS

Self microemulsifying powder using Aerosil as a carrier

This investigation highlighted the development of a solid self micro emulsifying drug delivery system (solid SMEDDS) for improved oral delivery of Valsartan. Liquid SMEDDS were formulated and then the liquid formulation was transformed into free-flowing powder by adsorption on a solid carrier. Here the formulations were prepared in various ratios of the drug to the excipients. Various evaluation studies were performed. In-vitro release profiles of all formulations were evaluated. The concentration of the diffused drug was measured using a UV-visible spectrophotometer at λmax= 250 nm. The faster dissolution was exhibited by the formulations containing Avicel. The experimental results for prepared solid-SMEDDS showed the improved dissolution of the study drug in a short time. F-3 (Assay:77%; Dissolution: 51.7% after 45 min, 63% after 60 min) and F-4 (Assay:63%; Dissolution: 49.1% after 45 min, 67% after 60 min) showed better evaluation study and this two might be formulated in future. Thus, this study revealed the formulation solid-SMEDDS using Aerosil 200 as an adsorbent with the potential of enhancing the solubility, and dissolution rate of the drug.&#x0D; Bangladesh J. Sci. Ind. Res.56(2), 141-146, 2021

Formulation and Characterization of Self-Microemulsifying Drug Delivery System of Tacrolimus

Abstract&#x0D; The present investigation aimed to formulate a liquid self-microemulsifying drug delivery system (SMEDDS) of tacrolimus to enhance its oral bioavailability by improving its dispersibility and dissolution rate. Four liquid SMEDDS were prepared using maisine CC as oil phase, labrasol ALF as surfactant and transcutol HP as co-surfactant based on the solubility studies of tacrolimus in these components. The phase behavior of the components and the area of microemulsion were evaluated using pseudoternary phase diagrams. The formulations were also assessed for thermodynamic stability, robustness to dilution, self-emulsification time, drug content, globule size and polydispersity index. The prepared SMEDDS formulations exhibited improved drug release compared to the pure drug powder. From this study, it was concluded that using a composition of 10% maisine CC, 67.5% labrasol ALF and 22.5% transcutol produced a liquid SMEDDS with good thermodynamic stability and enhanced in-vitro drug release profiles compared with pure tacrolimus powder. All which supports the use of self-micro emulsifying drug delivery systems as a promising approach to improve solubility, dissolution and stability of poorly soluble drugs like tacrolimus.

A Review on Formulation and Development of Solid Self-Nano Emulsifying Drug Delivery Systems

This article describes current strategies to enhance aqueous solubility and dissolution rate of poor soluble drugs. Most drugs in the market are lipophilic with low or poor water solubility. There are various methods to enhance solubility: co-solvency, particle size reduction, salt formation and Self Nanoemulsifying drug delivery systems, SEDDS is a novel approach to enhance solubility, dissolution rate and bioavailability of drugs. The study involves formulation and evaluation of solid self-Nano emulsifying drug delivery system (S-SNEDDS) to enhance aqueous solubility and dissolution rate. Oral route is the most convenient route for non-invasive administration. S-SNEDDS has more advantages when compared to the liquid self-emulsifying drug delivery system. Excipients were selected depends upon the drug compatibility oils, surfactants and co surfactants were selected to formulate Liquid SNEDDS these formulated liquid self-nano emulsifying drug delivery system converted into solid by the help of porous carriers, Melted binder or with the help of drying process. Conversion process of liquid to solid involves various techniques; they are spray drying; freeze drying and fluid bed coating technique; extrusion, melting granulation technique. Liquid SNEDDS has a high ability to improve dissolution and solubility of drugs but it also has disadvantages like incompatibility, decreased drug loading, shorter shelf life, ease of manufacturing and ability to deliver peptides that are prone to enzymatic hydrolysis.&#x0D;

QUALITY BY DESIGN BASED DEVELOPMENT OF ETRAVIRINE SELF MICRO EMULSIFYING DRUG DELIVERY SYSTEM

Objective: The main objective of the present research work was to develop systematically the Self Micro Emulsifying Drug Delivery system of BCS Class IV drug in a Quality by Design framework.&#x0D; Methods: The quality by design-based formulation development proceeds with defining the Quality Target Product Profile and Critical Quality Attributes of dosage form with appropriate justification for the same. The statistical Mixture design was used for the development of the formulation. The independent variables selected for the design were Oleic acid, Labrasol and PEG 6000, whereas droplet size (nm), emulsification time (sec), % drug loading and % drug release at 15 min were considered as the potential quality attributes of the Self Micro Emulsifying System. The eight different batches of Etravirine-Self Micro Emulsifying systems (ETV-SMEDDS) were prepared and checked for the Critical Quality Attributes. The simultaneous optimization of the formulation was done by the global desirability approach.&#x0D; Results: The characterization report obtained for all the different batches of formulation was analyzed statistically by fitting into regression models. The statistically significant models determined for droplet size (nm) (R2= 0.96 and p-0.1022), emulsification time (sec) (R2= 0.99 and p-0.0267), % drug loading (R2= 0.93 and p-0.1667) and % drug release at 15 min (R2= 0.96 and p-0.0911) and were statistically significant. The maximal global desirability value obtained was 0.9415 and the value indicates, the selected factors and responses have a good correlation and are significant enough for optimization and prediction of best formulation.&#x0D; Conclusion: The QbD approach utilized during the development of ETV-SMEEDS facilitated the identification of Critical Material Attributes and their significant impact on the Critical Quality Attributes of SMEDDS. The concept of building quality into product through the QbD application was utilized successfully in the formulation development.