Nanoemulsifying Drug Delivery System Research Articles

Enhancement of Icariin Aphrodisiac Effect by Solid-SNEDDS Method Using Shark Liver Oil Phase

The Epimedium brevicornu Maxim plant contains icariin, a flavonoid compound known for its aphrodisiac effects. However, icariin has low solubility and bioavailability. This study aims to find the best formula for S-SNEDDS icariin, its physical properties, characteristics, and aphrodisiac activity. Using the S-SNEDDS (Solid-Self Nanoemulsifying Drug Delivery System) method with shark liver oil phase is expected to increase the solubility and bioavailability of icariin. The optimum formula used is tween 80 (72.5%): PEG 400 (13.75%) and shark liver oil (13.75%). The optimal formula of S-SNEDDS icariin with the adsorption method to solid carriers requires aerosol 200 as much as 783±28.86mg per 1mL. S-SNEDDS icariin has characteristics with an average emulsification time of 12.88±0.26 seconds, transmittance value of 98.08±0.94%, droplet size 171.8±8.9 nm, zeta potential -35.2±1.1 mV, flow speed less than 10 seconds, resting angle 35.159°. The dissolution test of S-SNEDDS icariin is better than icariin instead of S-SNEDDS. S-SNEDDS icariin dose 50 mg/KgBW has a better aphrodisiac effect than pure icariin 100 mg/kgBW.

Oral hydrogel nanoemulsion co-delivery system treats inflammatory bowel disease via anti-inflammatory and promoting intestinal mucosa repair

BackgroundDue to oral nano-delivery systems for the treatment of inflammatory bowel disease (IBD) are often failed to accumulated to the colonic site and could not achieve controlled drug release, it’s urgent to develop a microenvironment responsive drug delivery to improve therapy efficacy. Inflammation at the IBD site is mainly mediated by macrophages, which are the key effector cells. Excessive inflammation leads to oxidative stress and intestinal mucosal damage. The use of curcumin (CUR) and emodin (EMO) together for the treatment of IBD is promising due to their respective anti-inflammatory and intestinal mucosal repair effects. In view of the pH gradient environment of gastrointestinal tract, here we prepared pH-responsive sodium alginate (SA) hydrogel-coated nanoemulsions to co-deliver CUR and EMO (CUR/EMO NE@SA) to achieve controlled drug release and specifically target macrophages of the colon.ResultsIn this study, a pH-responsive CUR/EMO NE@SA was successfully developed, in which the CUR/EMO NE was loaded by chitosan and further crosslinked with sodium alginate. CUR/EMO NE@SA had a pH-responsive property and could achieve controlled drug release in the colon. The preparation could significantly alleviate and improve the colon inflammatory microenvironment by decreasing TNF-α and IL-6 expression, increasing IL-10 expression, scavenging reactive oxygen species in macrophages, and by ameliorating the restoration of intestinal mucosal tight junction protein expression. Furthermore, we revealed the molecular mechanism of the preparation for IBD treatment, which might due to the CUR and EMO synergic inhibition of NF-κB to improve the pro-inflammatory microenvironment. Our study provides a new IBD therapy strategy via synergically inhibiting inflammatory, repairing mucosal and clearing ROS by pH-sensitive hydrogel-encapsulated nanoemulsion drug delivery system, which might be developed for other chronic inflammatory disease treatment.ConclusionsIt’s suggested that pH-sensitive hydrogel-coated nanoemulsion-based codelivery systems are a promising combinatorial platform in IBD.Graphical

Review on Nano-Emulsion Drug Delivery System and Formulation, Evaluation and Their Pharmaceutical Applications

Nano-emulsion drug delivery system such as develop to eliminate the limitations with traditional drug administration system. This review provided a good overview of the recent advances in the Nano-emulsion drug delivery system. These are nano-sized submicron emulsions developed to enhanced the circulates of active pharmaceutical ingredients to targeted site. Nano-emulsion is a homogeneous mixture of lipid and aqueous phase and stabilization is obtained through the use of an effective substance such as emulsifying agents. The droplet size has been range between the 50-500 nm. The size and shape of the substance distributed throughout the usual process differentiates of emulsion, micro-emulsion, and nano-emulsion. Nano-emulsion gives a novel dosage form for less water solubility drugs and increases pharmacological activity of drugs. Nano-emulsion is used in the future cosmetic industry, diagnostic testing, drug treatment, and biotechnology. This analysis aims to include brief information on the nano-emulsion, advantages, disadvantages, limitations of nano-emulsion, types of nano-emulsion, components of formulations, surface active agents (Surfactant), preparation methods, characterization methods with strong attention of different pharmaceutical applications of nano-emulsion in a different area such as cancer and tumors therapy, targeted drug delivery, mucosal vaccine, trans-dermal drug delivery system.

NANOTECHNOLOGY APPROACH-SELF NANOEMULSIFYING DRUG DELIVERY SYSTEM (SNEDDS)

This review article aims to develop nanotechnology in novel drug delivery systems using self-nano emulsifying drug delivery systems (SNEDDS). This Article was selected using a database with Prism Guideline diagrams. A total of 18 articles obtained from 2010-2020 were used as the primary reference to be analyzed using a systematic review method in the form of meta-synthesis. This review describes the mechanism of SNEDDS in increasing absorption, the components of the SNEDDS formula, the characterization of self-nano emulsifying drug delivery systems (SNEDDS), the effect of the physicochemical properties of SNEDDS on in vivo activity, and the basis for selecting compounds in the SNEDDS formulation. Self-Nanoemulsifying Drug Delivery System (SNEDDS) is a novel drug delivery system from nanoemulsion used to increase the solubility of lipophilic drugs. SNEDDS is an isotropic mixture consisting of oil, surfactant, and co-surfactant. SNEDDS is considered pre-concentrated nanoemulsions or anhydrous forms of nanoemulsions. In SNEDDS, the formation of nanoemulsions occurs when self-nanoemulsions come into contact with gastrointestinal fluids in the presence of light stirring in the peristaltic motion of the gastrointestinal tract. In general, SNEDDS have small particle sizes in the range of 10-200 nm. The application of the self nanoemulsion development system can be used for BCS Class II lipophilic drug compounds and BCS Class IV drugs. SNEDDS is a novel drug delivery system that can be used for oral drug delivery. In occlusion, a self-nanoemulsifying drug delivery system (SNEDDS) is a new approach for the formulation of drug molecules with poor water solubility. Self Nanoemulsifying drug delivery system (SNEDDS) is an isotropic mixture of oil, surfactant, and co-surfactant.

Therapeutic Importance and Pharmacological Activities of Norisoboldine in Medicine for the Treatment of Human Disorders.

Natural products constitute a unique source of chemical compounds with multi-target potential for the treatment of complex human disorders. Phytochemicals are pure phytoconstituents of plants, mainly responsible for their therapeutic potential and pharmacological activities. Natural products isolated from medicinal plants have been used as a lead source of drug. Norisoboldine is an important isoquinoline alkaloid found to be present in the dry root of Lindera aggregate. In the present paper, scientific data of norisoboldine have been collected from Google, Google Scholar, PubMed, Science Direct and Scopus and analyzed in order to know the biological potential and therapeutic effectiveness of norisoboldine in medicine. Scientific data of medicinal importance and therapeutic potential of norisoboldine has been collected and analyzed in the present work. Moreover, all the collected scientific data have been separated into different sub-section i.e. Medicinal importance, pharmacological activities and analytical aspects. Detailed pharmacological activity data of norisoboldine have been analyzed in the present work to know the therapeutic effectiveness of norisoboldine in medicine. Analytical data of norisoboldine have also been collected and analyzed in the present work. Scientific data analysis revealed the biological importance of isoquinoline alkaloids in medicine. Isoquinoline alkaloids are pure, active phytochemical present in several natural edible products including vegetables, plants, and fruits. Norisoboldine has a biological effect on arthritis, colitis, apoptosis, osteoclast differentiation, inflammatory pain, renal ischemia-reperfusion injury, acute lung injury, pro-inflammatory cytokines, tumor, regulatory T cells, and endothelial cell migration. However nanoemulsifying drug delivery system of norisoboldine has also been prepared in order to get better therapeutic value. Further analytical parameters of norisoboldine were also discussed in the present work in order to get the scientific information of separation, isolation and identification parameter of norisoboldine. Present work revealed the therapeutic potential of norisoboldine in medicine.

Development of a Novel Pomegranate Polysaccharide Nanoemulsion Formulation with Anti-Inflammatory, Antioxidant, and Antitumor Properties.

Colorectal cancer is one of the most serious gastrointestinal cancers in Africa and its prevention is a pronounced challenge in contemporary medicine worldwide. The present study aimed to develop nanoemulsion drug delivery system using pomegranate polysaccharides (PGPs) as an alternative cancer remedy, and then the evaluated its biological activities. The PGPs yield and chemical composition were evaluated, and then a PGPs nanoemulsion (PGPs-NE) was prepared using the self-emulsification technique with an oil phase. The physicochemical characterization of PGPs-NE was then analyzed. The in vitro antioxidant, anti-inflammatory activities, and antitumor potency of PGPs and PGPs-NE were also evaluated. The PGPs yield was 10%. The total sugar and protein content of PGPs was 44.66 mg/dl and 19.83μg/ml, respectively. PGPs were mainly composed of five monosaccharides including fructose, glucose, galactose, rhamnose, and arabinose. Concerning physiochemical characterization, the formulated PGPs-NE had three optical absorption bands at 202, 204, and 207nm and a transmittance of 80%. Its average hydrodynamic particle size was 9.5nm, with a PDI of less than 0.2 and a negative zeta potential (-30.6 mV). The spherical shape of PGPs-NE was confirmed by a transmission electron microscope study, with an average size of less than 50 nm. Additionally, the method used to prepare the PGPs-NE formulation provided high entrapment efficiency (92.82%). The current study disclosed that PGPs-NE exhibited strong antioxidant, anti-inflammatory, and antitumor agent potency compared to that of free PGPs. These promising current findings provide evidence for the possible efficacy of novel PGPs-NE as an alternative treatment for CRC.

Formulation and Statistical Evaluation of Tablets Containing Pitavastatin- Self Nano Emulsifying Drug Delivery Systems.

To formulate and characterize tablets containing Pitavastatin that have been loaded with a self-nano emulsifying drug delivery system (SNEDDS). Pitavastatin SNEDDS were prepared with a variety of oils, surfactants, co-surfactants, and solvents to improve the dissolution rate and bioavailability of the HMG-CoA reductase inhibitor. The SNEDDS components were preliminarily investigated for drug solubility in various vehicles, excipient miscibility, emulsification rate, and ternary phase diagrams. The tablets were made using a porous carrier made of Aerosil 200 and then loaded with SNEDDS using a simple absorption method. Physical parameters such as tablet hardness, weight variation, disintegration, drug content, and in-vitro drug release were then measured on the tablets. Labrafac Lipophilewl1349 (Oil), Tween 80 (Surfactant) and Egg lecithin (Co-surfactant) were selected for the preparation of SNEDDS. Tablets with high porosity suitable for loading with SNEDDS and containing the super-disintegrants, achieved complete dissolution of Pitavastatin from the tablets. In vitro release of Pitavastatin from SNEDDS and the tablets was similar (p < 0.05). SNEDDS of Pitavastatin is a promising approach to achieving a solid dosage form of the liquid-loaded drug delivery systems for enhancing the solubility and dissolution rate of the drug, and hence also its bioavailability.

Formulation and evaluation of self-nanoemulsifying drug delivery system for improved oral delivery of exemestane hydrochloride

Exemestane HCl (EXM) is a new irreversible steroidal aromatase inhibitor for adjuvant therapy of hormonally sensitive breast cancer in post-menopausal women. EXM's low water solubility hinders solid oral dosage form development. The current work aims to increase EXM solubility by formulating the self nanoemulsifying drug delivery (SNEDDs) system. The water titration approach was employed in the development of SNEDDs. Based on solubility tests, SNEDDs components Caprol Microexpress and Labrafac were selected as oil phase, Tween 80 as surfactant, and Triacetin as co-surfactant. Phase investigations were carried out with various surfactant:co-surfactant ratios (1:1, 1:2, 1:3, 2:1, 3:1). Tween 80: triacetin (1:2) and (1:3) with Caprol Microexpress and Labrafac alone had the greatest nanoemulsion area. Visual evaluation, optical clarity, particle size, medication concentration, and viscosity were used to optimise 10 formulations. F3, F7, and F8 batches had the lowest size at 7.313 ± 1.44 nm, 6.379 ± 0.45 nm, and 14.67 ± 0.37 nm, respectively, with self-emulsification times under 1 min.But optical clarity data was suggested that F7 was not showing any precipitation up to 24 H. Overall, the developed SNEDDS formulation could be a promising approach for the improved oral delivery of EXE with enhanced dissolution and bioavailability.

Novel Self Nanoemulsifying Drug Delivery System and its Future Perspectives

One-third of newly discovered drug molecules are water-insoluble, resulting in poor oral bioavailability in BCS (Biopharmaceutical Classification System). The Self Nanoemulsifying Drug Delivery System (SNEDDS) is a novel drug delivery system designed to improve the water solubility of medications that are ineffectively water soluble. It consists of an isotropic blend of oil, surfactant, and cosurfactant particles, as well as a codissolvable atom. Encapsulating a drug in SNEDDSs can lead to increased solubilization, stability in the gastro-intestinal tract, and absorption, resulting in enhanced bio-availability. The use of solid SNEDDS in the form of dry, solid powders would help to overcome the limitations of liquid SNEDDS by increasing the stability and patient compliance. Solid dosage forms are more stable and easier to handle than liquid systems, so efforts are being made to convert liquid systems to solid SNEDDS. Self-emulsification approach has been successful in oral drug delivery Spray drying, freeze drying, Micro fluidization, High Pressure Homogenizer, Sonication, and adsorption on carriers are some of the techniques that can be used to convert liquid SNEDDS into solid SNEDDS compressed into tablets. The composition of the SNEDDS can be optimized with the help of phase diagrams, whereas statistical experimental design can be used to further optimize SNEDDS. It is a novel drug delivery system that can be used for parenteral, ophthalmic, intranasal, and cosmetic drug delivery.

Formulation and Evaluation of O/W Nanoemultion of Ketoconazole

Abstract: Ketoconazole is a broad spectrum imidazole antifungal agent marketed as creams and tablets. It interacts with 14- demethylase, a cytochrome P-450 enzyme and inhibits ergo sterol synthesis and increased fungal cellular permeability and is used against a wide variety of fungi and yeast .Nano technology scales up to one billionth of a meter Generally, they are considered to be in range of 100nm to 1000nm. Ketoconazole Nano emulsion drug delivery system is known to improve dissolution characteristics of a poorly water soluble drug since they maintain the drug in a dissolution characteristics of a poorly water soluble drug since they maintain the drug in solubilized state. Using the optimized Nano emulsion of ketoconazole loaded were prepared. The prepared liquid Nano emulsion are subjected to thermodynamic stability testing and zeta potential due to their characteristics size and properties which included kinetic stability; they are effective L solubilizing the drug and transferring them to words the target areas. It is characterized for droplet size, ze potential, viscosity, in vitro drug release study we performed.

Self-Solidifying and Self-Nanoemulsifying Drug Delivery System of Itraconazole

Objective: To improve solubility, dissolution, and permeability of BCS class II drug Itraconazole (ITZ) using a self solidifying self nano emulsifying drug delivery system (SNEDDS). Method: The solubility of ITZ was assessed in oils, surfactants, co-surfactants, and buffers. Surfactants, co-surfactants, and combination of surfactants (S-comb) were selected on the basis of emulsification efficacy test. The ability to solidify self emulsifying mixture was assessed and solid SNEDDSS was developed and optimised. Finding: Solubility of ITZ was found maximum in 0.1N HCl (0.120  0.07mg/mL) followed by SGF (0.089  0.01mg/mL). Out of 20 oils screened, Peceol showed highest solubility. Among all surfactants and co-surfactants studied, Labrafil M 1944 CS (LM 1944) showed highest potential to solubilize ITZ (14.91 mg/g). The globule size of the optimised formulation was found to be 40.11 nm with PDI of 0.144. Zeta potential study revealed the stability of the SNEDDS. Drug content of solid SNEDDS of ITZ was found within the range of 98.11% to 102.51%, which was found in the acceptable limit. It was observed that ITZ solid SNEDDS (SSNEDDS) showed a promising improvement in the in vitro dissolution profile compared to the plain ITZ and marketed product in all three-dissolution media. Nearly 3-fold enhancement of permeability of ITZ was attributed by uniformly dispersed globules with nano size. Analytical characterization demonstrated that the drug and excipients are compatible with amorphous characteristics of the ITZ. Novelty: The developed self solidifying SNEDDS of ITZ showed enhanced solubility, dissolution, and permeability in comparison to the pure drugs (ITZ). Self solidifying SNEDDS would be a novel approach to overcome the limitations associated with liquid dosage forms. Keywords: Itraconazole; Solubility; Bioavailability; Self Nano Emulsifying Drug Delivery System (SNEDDS); Permeability

Development and Characterization of Non-Aqueous based Self Emulsifying Nano Emulsion of Curcumin

This research presented a novel as well as an easy method for a non-aqueous based self-emulsifying nanoemulsion of hydrophobic drug. In this Non Aqueous based self nanoemulsifying drug delivery system (SNEDDS) of curcumin was prepared, and in vitro Analysis was done. Oleic acid serves as the oil phase in Curcumin SENE formulations, which also contain Tween 20. PEG 400 as co-surfactants was selected. The preliminary confirmation was done by FTIR spectra and 1603.80cm -1 [C=C], 3420.87 cm -1 [polymeric OH stretching], 1377.22 cm -1 [C=O stretching] was observed. The preformulation study was also done with excellentflow property. Melting point of curcumin was shown at the range of 180-183°C. The λ max of Curcumin was found to be at 424 nm in methanol. Highest solubility of curcumin was found in oleic acid. The primarily confirmation of nano emulsion was done by conductivity test, fluorescence test and Viscosity. Characterization of formulation was done by FT-IR, Droplet size, viscosity, drug content, % Transmittance and robustness study. The spectrum FT-IR of pure drug and self emulsifying nanoemulsion (SENE) was showing the changes.

A Review on Different Solubility Enhancement Techniques of Ticagrelor

Ticagrelor is a BCS class IV drug that inhibits platelet action by reversibly binding to the P2Y12 receptor. One of the major challenges faced by the class IV (low solubility, low permeability) drug is the lower dissolution rate leading to low bioavailability. The bioavailability of the marketed formulation of ticagrelor is approximately 36%. Researchers have come up with various techniques to improve the BCS class II and IV drug formulations as an integral part of the development of the pharmaceutical sciences. An increase in solubility can be achieved by various methods such as Salt formation, Complexation, Micronization, Solid Dispersion, altering the pH, Co-solvency, co-crystals, polymeric micelles, etc. A highly efficacious technique is converting a crystalline drug to its amorphous form. An extensive literature search was conducted using various databases like science direct, Taylor and Francis, Springer to extract relevant articles. Keywords like “Ticagrelor”, “low permeability”, “P2Y12 receptor inhibitor” were used for the literature search. Relevant articles were screened and referred for further study. This article discusses the techniques employed to increase the solubility of ticagrelor, thus highlighting the research conducted and reported. The increase in bioavailability of ticagrelor could be seen when formulated as nanoparticles, co-crystals, ticagrelor loaded self-micro emulsifying and nano emulsifying drug delivery system, solid dispersion, etc. the conversion of the crystalline drug into amorphous drug is a highly recommended approach to increase the solubility of ticagrelor which can be seen in cases of co-crystals and solid dispersion formulation.

Beneficial effects of topical 6-gingerol loaded nanoemulsion gel for wound and inflammation management with their comparative dermatokinetic

PurposeTo develop, formulate and evaluate a 6-Gingerol (GL) loaded self nano emulsifying drug delivery system and its conversion to nanoemulgel to achieve better topical application via their solubility improvement as well as permeation of skin for the management of wound healing and anti-inflammatory mechanism. MethodsWe used the aqueous microtitration method for the preparation of GL-NE with the help of Oleic Acid (oil phase), Tween 20 (surfactant), and PEG-400 (co-surfactant). To improve contact time for topical delivery, it was loaded into Carbopol 934 gel to form nanoemulgel. Nanoemulsion and nanoemulgel were evaluated for globule size, thermodynamic stability, physical appearance, ZP, PDI, pH, drug content, rheological behavior, drug release (in-vitro) with skin permeation, spreadability, DSC, swelling index and bioadhesive strength. ResultsGL-SN7 showed a clear, stable, and transparent nanoemulsion containing mean droplet size (91.36 ± 4.61 nm), zeta potential (−9.12 ± 0.79 mV), and PDI (0.119 ± 0.005). Nanoemulgel (NEG) showed that showed the mean droplet size (103.24 ± 6.31 nm) and PDI (0.126 ± 0.123), and ZP (−10.8 ± 0.95 mV), pH (6.69 ± 0.06), viscosity (5552 cP) at 100 rpm and spreadability 234.10 ± 0.75 g cm/sec with better mucoadhesive strength with their smooth and spherical shape by SEM. Finally, optimized-6-GL-SNEDDS-Gel was used to enhance skin permeation and their dermatokinetic results showed a significant (p˂0.001) enhancement in the CSkin max and AUC0–8h in the treated skin with optimized-6-GL-SNEDDS-Gel as compared to 6-GL-conventional-gel treated with skin. However, optimized-6-GL-SNEDDS-Gel found significant wound healing as compared to GL-S on topical application. We didn't observe any signs of inflammatory cells after the treatment from the GL-SNEDDS-Gel as well as suggested the safety and non-toxicity of optimized-GL-SNEDDS-Gel. ConclusionWe have successfully developed a novel GL-SNEDDS-Gel. It improved the solubility and skin permeation of GL. GL-SNEDDS-Gel showed a better treatment of wound healing as well as anti-inflammatory treatment of GL given topically.

Antithrombotic and Antioxidant Activities of Binahong [Anredera cordifolia (Ten.) Steenis] Leaf Ethanol Extract and Its Nanoemulsion Preparation in Swiss Webster Mice

Platelet aggregation has the potential to form thrombi and result in cardiovascular system diseases such as myocardial infarction and ischemic stroke - one of the leading causes of death globally. Traditionally, people use binahong leaves as blood thinners. Therefore, this study aims to obtain scientific data on the efficacy of binahong leaf as antithrombotic. The efficacy test was carried out on male Swiss-Webster mice. The results showed that the ethanol extract of binahong leaves at doses of 50 (BLEE50) and 100 mg/kg bw (BLEE100) could increase bleeding time on H7 (7.61±1.79% and 3.72±1.76% vs 1.08±0.90%) and H14 (13.81±4.42% and 5.06±2.30% vs 1.66±1.09%) and coagulation time at H7 (5.01±1.36% and 4.18±1.67% vs 1.38±1.08%) and at H14 (7.92±1.97% and 7.19±1.96% vs 1.70±1.10%) significantly (p&lt;0.05). The two doses of BLEE were formulated in the form of nanoemulsions with the Self Nano Emulsifying Drug Delivery System (NBLEE50 and NBLEE100) were also able to prolong bleeding time and coagulation time significantly (p&lt;0.01) but only NBLEE50 prolonged bleeding time (p&lt;0.05) significantly against BLEE50. In the test of the anti-platelet aggregation effect with ADP as an inducer, both doses of BLEE and the nanoemulsion preparation (NBLEE) could significantly (p&lt;0.01) inhibit platelet aggregation with a percentage of inhibition &gt;70% which was not different from the standard (acetylsalicylic acid). In the antioxidant effect test using the DPPH method, BLEE has an IC50 = 66.08?g/mL which is classified as a strong antioxidant. Both doses of BLEE and its NBLEE could significantly (p&lt;0.01) inhibit lipid peroxidation in plasma and liver and NO radicals formation. BLEE50 can significantly (p&lt;0.05) reduce mean platelet volume (6.05±0.24fL vs 6.55±0.34fL) and platelet distribution width (8.52±0.36% vs 9.25±0.42%). Based on those results, BLEE has the potential to be used as an antiplatelet aggregation and antioxidant.

Precision engineering designed phospholipid-tagged pamidronate complex functionalized SNEDDS for the treatment of postmenopausal osteoporosis.

Disodium pamidronate, a second-generation bisphosphonate is a potent drug for the treatment of osteoporosis, which has been very well established by previous literature. It has very low oral permeability, leading to its low oral bioavailability, which restrict this drug to being administered orally. Therefore, the present research work includes the development of an orally effective nanoformulation of pamidronate. In this work, disodium pamidronate was complexed with phospholipon 90G for the enhancement of permeability and to investigate the phospholipon 90G-tagged pamidronate complex-loaded SNEDDS for oral delivery with promises of enhanced bioavailability and anti-osteoporotic activity. The rational design and optimization was employed using Central Composite Design (Design Expert® 12, software) to optimize nanoformulation parameters. In this work, a commercially potential self nano-emulsifying drug delivery system (SNEDDS) has been developed and evaluated for improved oral bioavailability and better clinical acceptance. The hot micro-emulsification and ultracentrifugation method with vortex mixing was utilized for effective tagging of phospholipon 90G with pamidronate and then loading into the SNEDDS nanocarrier. The optimized Pam-PLc SNEDDS formulation was characterized for particle size, PDI, and zeta potential and found to be 56.38 ± 1.37nm, 0.218 ± 0.113, and 22.41 ± 1.14 respectively. Also, a 37.9% improved bioavailability of pamidronate compared to marketed tablet was observed. Similarly, in vivo pharmacokinetic studies suggest a 31.77% increased bone density and significant enhanced bone biomarkers compared to marketed tablets. The developed formulation is safe and effectively overcomes anti-osteoporosis promises with improved therapeutic potential. This work provides very significant achievements in postmenopausal osteoporosis treatment and may lead to possible use of nanotherapeutic-driven emerging biodegradable carriers-based drug delivery.

Formulation Development, Optimization by Box-Behnken Design, and In Vitro Characterization of Gefitinib Phospholipid Complex Based Nanoemulsion Drug Delivery System

Formulation Development, Optimization by Box-Behnken Design, and In Vitro Characterization of Gefitinib Phospholipid Complex Based Nanoemulsion Drug Delivery System

Oral self-emulsifying nanoemulsion systems for enhancing dissolution, bioavailability and anticancer effects of camptothecin

This research aimed to prepare a camptothecin (CPT) loaded self nano emulsifying drug delivery system (SNEDDS) that would improve the oral therapeutic efficacy of CPT. 32 full factorial design was employed, and the effect of the amount of oil (X1) and surfactant mixture (X2) was systematically investigated on percentage transmittance (Y1), self-emulsification time (Y2), and percentage cumulative drug release (Y1). Pseudo-ternary phase diagrams were constructed at different km values (1, 2, and 3). In total, 13 experimental runs (LF–1 to LF–13) were prepared at km = 3, evaluated, and converted to solid free-flowing granules (S–SNEDDS) using neusilin® US2. LF–10 comprising 12.5% omega oil and 40% cremophor-RH40 and labrafil-M2125 had nanosizing (<200 nm), high % transmittance (98.42 ± 1.82%), and lower self-emulsification time (21 ± 0.38 Sec). Nano-sized droplets were spherical, as revealed by the TEM study. FT-IR spectra showed no incompatibilities, whereas DSC and XRD results confirmed CPT's amorphous state and molecular dispersion in SNEDDS. In-vitro dissolution studies demonstrated significant (P < 0.05) improvement in CPT release characteristics from S–SNEDDS (SF–10). in-silico studies confirmed hydrogen bond interaction between an amino group of CPT and neusilin oxygen. S-CPT-10 significantly (P < 0.05) inhibited the proliferation of BEWO placental cancer cells more than CPT. It induced apoptosis in cancerous cells, revealed by DAPI, Annexin-V/PI staining, and mitochondrial potential measurement. Remarkably, oral administration of CPT–SNEDDS resulted in a 17-fold increase in bioavailability compared to plain CPT. Thus, SNEDDS could be utilized as a potential carrier for CPT delivery.

Physical characterization of clove oil based self Nano-emulsifying formulations of cefpodoxime proxetil: Assessment of dissolution rate, antioxidant & antibacterial activity

Cefpodoxime proxetil (CPD) is a broad-spectrum cephalosporin widely indicated in respiratory tract infections like pneumonia. CPD is a BCS class IV drug with the constraint of low bioavailability attributable to its poor aqueous solubility (10µg/ml) and impaired permeability. Clove oil (CO) acts as a lipophilic additive for lipid-based delivery systems designed to facilitate dissolution characteristics of poorly soluble drugs, modulating drug permeability as well as stability against oxidation. The present work aims to improve CPD solubilization by developing CO-based fully dilutable self nano emulsifying formulation (SNF), and assessment of its antibacterial and antioxidant potential. The existence of nanoemulsion domains was tracked from ternary phase diagrams plotted between CO, Tween 20/PEG400 to act as oil phase, surfactant/co-surfactant (Smix) respectively at weight ratios 1:1, 1:2, and 2:1 whereas aqueous phase acted its tertiary component. Two subsets of SNF formulations coded as (DAO1-DAO5) and (DAM1-DAM3) were prepared and assessed for antioxidant and antibacterial activities respectively, along with their naive CO-counterparts (AO1-AO5) and (AM1- AM5) respectively. Physical characterization revealed SNFs were droplet size range 35-170nm, conductivities in the range 200-500uS/cm, and RI values in 1.361-1.429. The dilution-induced microstructure transition effect was observed in SNF with the addition of an aqueous phase as its oil-continuous domain transformed into water-continuous via bi-continuous structure formation as interpreted from conductivity and refractive index data. In-vitro dissolution characterization of SNF formulation exhibits a quick CPD release pattern in comparison to control in phosphate buffer at pH 6.8 and HCl buffer at pH3.0. SNF produced significant differences in the CPD release characteristics measured at different pH conditions in comparison to controls. These observations are plausible in terms of drug solubilization effect since SNFs possess a high proportion of surfactant and produce interfacial action on CO and CPD. Antioxidant activities in DAO and AO at CO 20, 40 & 100µg/ml levels were significantly different from controls as measured using the DPPH method. Comparison of antibacterial activity of DAMs against E. coli, B. subtilis, Enterobacter species, and S. aureus (scheme-II) vs CPD suspension or its coarse emulsion or even naive CO counterpart were statistically different and minimum inhibitory concentration of CPD was reduced in SNF formulations. These differences were well corroborated in the data exhibited in zones of inhibition studies. CO-based SNFs produced significantly improved dissolution characteristics of poorly soluble drugs like CPD and potentiated the antibacterial and antioxidant activities. Developed SNFs could be employed as Self nano emulsifying drug delivery systems (SNEDDS) for BCS class IV drugs.

Formulation & In vivo Evaluation of Self Nano Emulsifying Drug Delivery System of Doravirine

Formulation & In vivo Evaluation of Self Nano Emulsifying Drug Delivery System of Doravirine