Enhanced Solubility, In-Vitro Dissolution and Lipase Inhibition of a Self-Nanoemulsifying Drug Delivery System Containing Orlistat

The aim of this work was to prepare and optimize a solid self-nanoemulsifying drug delivery system pre-concentrate (SSP) containing water-insoluble flurbiprofen (FL) using a novel pseudo-ternary phase diagram. The pseudo-ternary phase diagram, composed of FL as the drug and dispersion core, Kollisolv MCT 70 as the oil phase, and TPGS (tocopherol polyethylene glycol 1000 succinate) as the surfactant, was constructed for the determination of the SSP region. SSP was investigated in terms of particle size, physical state by differential scanning calorimetry (DSC) and powder X-ray diffraction (PXRD), in vitro dissolution and oral pharmacokinetics in rats. The determined SSP (FL/Kollisolv MCT 70/TPGS = 10/10/80, weight %) in the pseudo-ternary phase diagram had the melting point of 32.37 °C and uniform mean particle size of below 30 nm without any precipitation of FL in the dispersion. In the dissolution test, the SSP exhibited 95.70 ± 3.40% of release at 15 min, whereas the raw FL showed poor dissolution (i.e., 6.75 ± 1.30%) at that time point. In addition, the SSP showed the enhanced oral absorption (i.e., 1.93-fold increase in AUCinfinite) as compared to the suspension group of raw FL. Therefore, the developed SSP would be a promising drug delivery system with excellent solubilization, dissolution, and bioavailability for FL.

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Applicability of Gum Karaya in the Preparation and in Vitro Evaluation of Losartan Potassium as Chronotherapeutic Drug Delivery System

Journal of Scientific Research ◽

10.3329/jsr.v7i1-2.21182 ◽

2015 ◽

Vol 7 (1-2) ◽

pp. 65-74

Author(s):

K. Latha ◽

V. V. Srikanth ◽

S. A. Sunil ◽

N. R. Srinivasa ◽

M. U. Uhumwangho ◽

...

Keyword(s):

Drug Delivery ◽

Tensile Strength ◽

Drug Delivery System ◽

Delivery System ◽

Lag Time ◽

Losartan Potassium ◽

In Vitro Dissolution ◽

Burst Release ◽

Gum Karaya

The objective of this investigation is to study the applicability of gum karaya, the natural gum for the preparation and in vitro evaluation of losartan potassium, as Chronotherapeutic Drug Delivery System (ChDDS). The compression-coated timed-release tablets (CCT) containing losartan potassium in the core tablet were prepared by dry coating technique with different ratios of gum karaya as the outer coat. The parameters investigated were tensile strength, friability, in vitro dissolution studies and drug concentration. The optimized formulation was further characterized by powder XRD and FTIR to investigate interactions and no interactions observed. The tensile strength and friability of all the CCT were between 1.06-1.23 MN/m2 and < 0.3% respectively. All the CCT showed a clear lag time before a burst release of drug. However, the lag time of drug release increased as the amount of gum karaya in the outer layer increased. For instance, the lag time of LGK1, LGK2, LGK3, LGK4, LGK5, LGK6 and LGK7 were 16, 10.5, 5.5, 3, 2, 1.5 and 0.5 hrs respectively. The drug content of all the CCT was >98%. Formulation LGK3 was taken as an optimized formulation which can be exploited to achieve ChDDS of losartan potassium for the treatment of hypertension.

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SELF-EMULSIFYING DRUG DELIVERY SYSTEM CONTAINING ACECLOFENAC: DESIGN & DEVELOPMENT USING QUALITY BY DESIGN (QBD) CONCEPT

INDIAN DRUGS ◽

10.53879/id.51.06.p0016 ◽

2014 ◽

Vol 51 (06) ◽

pp. 16-26

Author(s):

V Suthar ◽

◽

M Gokel ◽

S Butani ◽

A Solanki

Keyword(s):

Drug Delivery ◽

Drug Delivery System ◽

Delivery System ◽

Dosage Form ◽

Quality By Design ◽

Tween 80 ◽

Current Approach ◽

In Vitro Dissolution ◽

Design Development

The aim of the present study was to develop self-emulsifying drug delivery system (SEDDS) of aceclofenac for potential improvement in the in vitro dissolution. The Food and Drug Control Agency (FDCA) has put more stress on the quality, safety and efficacy of the dosage form. The use of design of experiments and quality by Design (QbD) in the development of self emulsifying drug delivery system (SEDDS) containing aceclofenac is demonstrated. The optimum formulation contained Labrafil M 1944 CS, Tween 80 and Transcutol P. The systematic approach enabled us in identifying the design space. The results revealed that while devising the control strategies during manufacturing, more attention should be focused on the ratios of oil to surfactant and surfactant to co-surfactant. The drug was released at a faster rate due to a large surface area. The current approach enabled us to develop a dosage form which is economic, patient-friendly and does not require assistance of a doctor or nurse, especially at remote places at odd hours.

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DEVELOPMENT AND EVALUATION OF ZIPRASIDONE LOADED SOLID SELF-MICRO EMULSIFYING DRUG DELIVERY SYSTEM

INDIAN DRUGS ◽

10.53879/id.57.08.12632 ◽

2020 ◽

Vol 57 (08) ◽

pp. 53-60

Author(s):

Purushottam Patil ◽

Malik Shaikh ◽

Paresh Mahaparale

Keyword(s):

Drug Delivery ◽

Drug Delivery System ◽

Delivery System ◽

Physical Adsorption ◽

Gastrointestinal Transit ◽

Water Soluble ◽

In Vitro Dissolution ◽

Scanning Calorimetry ◽

Poorly Water Soluble

Solid self-micro emulsification technique is the new approach for poorly water-soluble and poorly bioavailable drugs by allowing the drug substance to be incorporated into the oil phase and thus having the ability to permeate the GI membrane to a faster extent. Oleic acid, Tween 80, methanol and colloidal silicon dioxide were used as penetrant, surfactant, co-surfactant and adsorbent, respectively. The interaction between drug and excipients was examined by differential scanning calorimetry (DSC) and Fourier transform infrared spectroscopy (FTIR). The results of DSC and FTIR studies did not reveal any possible drug-excipient interactions. The conversion of liquid self-microemulsifying drug delivery system (SMEDDS) into the solid SMEDDS increases the stability of the emulsion formulation achieved by physical adsorption of an adsorbent material. The release of drug from SMEDDS formulation is justified by in-vitro dissolution studies. SMEDDS increases the solubility of the drug and improves the bioavailability, without disturbing gastrointestinal transit. SMEDDS has the potential to provide a useful oral solid dosage form for the poorly water-soluble drug ziprasidone.

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SELF-NANO EMULSIFYING DRUG DELIVERY SYSTEM OF EFAVIRENZ: FORMULATION, IN VITRO EVALUATION AND CHARACTERIZATION

Asian Journal of Pharmaceutical and Clinical Research ◽

10.22159/ajpcr.2019.v12i12.35227 ◽

2019 ◽

pp. 217-226

Author(s):

PAMU SANDHYA

Keyword(s):

Drug Delivery ◽

Dissolution Rate ◽

Drug Delivery System ◽

Delivery System ◽

In Vitro Release ◽

Visual Observation ◽

Stability Study ◽

In Vitro Dissolution ◽

Tween 20

Objective: The main objective of this study was to preparation and evaluation of efavirenz (EFV) to enhance its solubility and dissolution rate by self-emulsifying drug delivery system. Methods: EFV self-emulsifying drug delivery systems (SNEDDS) were formulated using different oils, surfactant, and co-surfactant. Peceol, Tween 20, and Capmul MCM were used as oil, surfactant, and co-surfactant, respectively, followed by the evaluation by the performance of different tests such as visual observation, solubility studies, thermodynamic stability study, transmittance studies, drug content, and in-vitro release study. Results: Fourier-transform infrared studies revealed negligible drug and polymer interaction. From the phase diagram, it was observed that self-emulsifying region was enhanced with increasing surfactant and co-surfactant concentrations with oil. F13 was selected as optimized formulation on the basis of physicochemical parameters, particle size, and in-vitro dissolution studies with the release of 98.39±5.10% drug in 1 hour. The optimized formulation size was found to be 156.7 nm as mean droplet size and Z-Average of 808.6 nm with -18.3 mV as zeta potential. Conclusion: The study demonstrated that SNEDDS was a promising strategy to enhance the dissolution rate of EFV by improving solubility.

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

Research Journal of Pharmacy and Technology ◽

10.52711/0974-360x.2021.01014 ◽

2021 ◽

pp. 5831-5837

Author(s):

Kiran C. Mahajan ◽

Smita S. Pimple ◽

Hemant A. Deokule

Keyword(s):

Drug Delivery ◽

Drug Delivery System ◽

Delivery System ◽

Ternary Phase ◽

In Vitro Dissolution ◽

Ternary Phase Diagrams ◽

Globule Size ◽

Capmul Mcm ◽

Negative Zeta Potential

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 & 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.

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Development of a self-microemulsifying drug delivery system of domperidone: In vitro and in vivo characterization

Acta Pharmaceutica ◽

10.2478/acph-2013-0013 ◽

2013 ◽

Vol 63 (2) ◽

pp. 241-251 ◽

Cited By ~ 9

Author(s):

Ramesh Jakki ◽

Muzammil Afzal Syed ◽

Prabhakar Kandadi ◽

Kishan Veerabrahma

Keyword(s):

Drug Delivery ◽

Drug Delivery System ◽

Delivery System ◽

Oral Bioavailability ◽

Ternary Phase Diagram ◽

Water Soluble ◽

In Vitro Dissolution ◽

Size Analysis

The main objective of this work was to prepare a self-micro emulsifying drug delivery system (SMEDDS) for enhancement of oral bioavailability of domperidone, a poorly water soluble drug. The solubility of the drug was determined in various vehicles. A pseudo ternary phase diagram was constructed to identify the self-micro emulsification region. The in vitro self-micro emulsification properties and droplet size analysis of SMEDDS were studied following their addition to water under mild agitation. Further, the resultant formulations were investigated for clarity, phase separation, globule size, effect of pH and dilutions (1:100, 1:500, 1:1000) and freeze-thaw stability. The optimized formulation, SMEDDS-B used for in vitro dissolution and bioavailability assessment, contained oil (Labrafac CC, 25 %, m/m), surfactant (Tween 80, 55 %, m/m), and co-surfactant (Transcutol®, 20 %, m/m). The preliminary oral bioavailability of domperidone from SMEDDS was 1.92-fold higher compared to that of domperidone suspension in rats. The AUC0-24 and cmax values were 3.38 ± 0.81 μg h mL-1 and 0.44 ± 0.03 μg mL-1 for SMEDDS-B formulation in comparison with 1.74 ± 0.18 μg h mL-1 and 0.24 ± 0.02 μg mL-1 for domperidone suspension, suggesting a significant increase (p < 0.05) in oral bioavailability of domperidone from SMEDDSS.

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Quality-By-Design-Based Development of a Voxelotor Self-Nanoemulsifying Drug-Delivery System with Improved Biopharmaceutical Attributes

Pharmaceutics ◽

10.3390/pharmaceutics13091388 ◽

2021 ◽

Vol 13 (9) ◽

pp. 1388

Author(s):

Aristote B. Buya ◽

Romano Terrasi ◽

Jérémie K. Mbinze ◽

Giulio G. Muccioli ◽

Ana Beloqui ◽

...

Keyword(s):

Drug Delivery ◽

Drug Delivery System ◽

Delivery System ◽

Oral Bioavailability ◽

Oral Delivery ◽

Ternary Phase Diagram ◽

Desirability Function ◽

Limiting Factors ◽

In Vitro Dissolution

Low aqueous solubility and poor oral bioavailability are limiting factors in the oral delivery of voxelotor, an antisickling agent. To overcome these limitations, a voxelotor self-nanoemulsifying drug delivery system was developed. Various oils, surfactants, and cosurfactants were screened for their solubilization potential for the drug. The area of nanoemulsification was identified using a ternary phase diagram. An experimental mixture design and a desirability function were applied to select SNEDDSs that contain a maximum amount of lipids and a minimum amount of surfactant, and that possess optimal emulsification properties (i.e., droplet sizes, polydispersity index (PDI), emulsification time, and transmittance percentage). The optimized SNEDDS formulation was evaluated for the self-emulsifying time (32 s), droplet size (35 nm), and zeta potential (−8 mV). In vitro dissolution studies indicated a 3.1-fold improvement in drug solubility from the optimized SNEDDS over pure drug powder. After 60 min of in vitro lipolysis, 88% of the voxelotor loaded in the SNEDDS remained in the aqueous phase. Cytotoxicity evaluation, using Caco-2 cells, indicated the safety of the formulation at 0.9 mg/mL. The transport of the voxelotor SNEDDS across Caco-2 monolayers was significantly enhanced compared to that of the free drug. Compared to the drug suspension, the developed SNEDDS enhanced the oral bioavailability (1.7-fold) of voxelotor in rats. The results suggest that further development of SNEDDSs for the oral delivery of voxelotor is needed.

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FORMULATION DEVELOPMENT AND IN VITRO EVALUATION OF CURCUMIN-LOADED SOLID SELF-NANOEMULSIFYING DRUG DELIVERY SYSTEM FOR COLON CARCINOMA

Asian Journal of Pharmaceutical and Clinical Research ◽

10.22159/ajpcr.2019.v12i7.33231 ◽

2019 ◽

pp. 243-247

Author(s):

CHENMALA KARTHIKA ◽

RAMAN SURESHKUMAR ◽

AMEER SUHAIL

Keyword(s):

Drug Delivery ◽

Colon Cancer ◽

Drug Delivery System ◽

Delivery System ◽

Dosage Form ◽

In Vitro Dissolution ◽

Formulation Development ◽

The World ◽

Tablet Dosage

Objective: Cancer is the deadliest disease affecting the life of the people all around the world. Colon cancer is the cancer which is affecting the colon region it is the last part of the gastrointestinal tract which is mainly responsible for the absorption of water and minerals from the food debris. Colon cancer is the second most cancer creating death in the world. It affects both male and female equally. Curcumin is a flavonoid used from decades for the treatment of various ailments including cancer. This present work is to formulate Self-nanoemulsifying drug delivery (SNEDDS) system with the help of curcumin for colon delivery. Materials and Methods: Nanoemulsion was prepared using the curcumin pre-concentrated self-nanoemulsifying drug delivery system, with which tablets were prepared and coated with pectin followed by the evaluation test such as in vitro dissolution and cell line studies. Results: Solubility profile of curcumin was found with a greater impact using Capmul MCM and Labrafac PG which is then added with the surfactants and co-surfactants and were converted into Nano-droplets. F1 formulation was selected after carrying out the characterisation studies and converted into a tablet dosage form and then coated with pectin, in vitro studies depicted a release of 80% in pH 6.8. Conclusions: Formulation of a solid self-Nano emulsifying drug delivery system using curcumin was successfully carried out. From the results obtained, the formulation (F1) was selected for the formation of the tablets and the further experimental part is carried out. The tablet dosage form is then coated with pectin and used for targeting the colon cancer cells for its treatment.

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DEVELOPMENT OF SOLID SELF-MICROEMULSIFYING DRUG DELIVERY SYSTEM OF DIACEREIN FOR ENHANCED DISSOLUTION RATE

Asian Journal of Pharmaceutical and Clinical Research ◽

10.22159/ajpcr.2019.v12i2.29500 ◽

2019 ◽

pp. 315-319

Author(s):

JAMEER A TAMBOLI ◽

SHRINIVAS K MOHITE

Keyword(s):

Drug Delivery ◽

Zeta Potential ◽

Dissolution Rate ◽

Drug Delivery System ◽

Delivery System ◽

Water Soluble ◽

In Vitro Dissolution ◽

Dissolution Study ◽

Globule Size

Objective: The objective of the present study was to develop solid self-microemulsifying drug delivery system (S-SMEDDS) of diacerein (DCN) for enhancement of dissolution rate. Methods: Three batches of liquid SMEDDS were prepared using oleic acid, Tween 80, and polyethylene glycol 200 as oil, surfactant, and cosurfactant, respectively. Microemulsion region was recognized by constructing a pseudoternary phase diagram containing a different proportion of oil, surfactant, and cosurfactant. Prepared liquid SMEDDS was evaluated for thermodynamic stability study, dispersibility tests, globule size, zeta potential, and viscosity. Liquid SMEDDS was then converted to S-SMEDDS by adsorption technique using Neusilin US2 as a solid carrier. Prepared S-SMEDDS was evaluated for different micromeritic properties, drug content, reconstitution properties, in vitro dissolution study, Fourier transform infrared, and scanning electron microscopy. Results: The results showed that all batches of liquid SMEDDS were found to be thermodynamically stable. Reconstitution properties of S-SMEDDS showed spontaneous microemulsification with globule size 0.271 μm and −16.18 mV zeta potential. From the results of in vitro dissolution study, it was found that the release of DCN was significantly increased as compared with plain DCN. Conclusion: The study concluded that dissolution rate of poorly water-soluble drug like DCN can be increased by developing S-SMEDDS formulation.

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