Emulsion Solvent Evaporation Technique Research Articles

Comparison Study Between Encapsulation of Acalypha indica Linn Extracts with Chitosan-PCL and Chitosan-OA

Drug delivery is one of the major applications in the biodegradable polymer science. Chitosan is a non-toxic and naturally biodegradable polymer. It is soluble in acidic aqueous media and insoluble in higher pH media. Chitosan has been modified to improve its properties such as stability and the modified derivatives have been widely used in many applications especially for drug delivery. There are several kinds of chitosan modification. This study investigated the modification of chitosan with polyester-types of polymer and the fatty acidbased polymer. The aim of this study is to compare the formation encapsulation of chitosan-oleic acid conjugate (Ch-OA) and chitosan- polycaprolactone(PCL) copolymer for the encapsulation of Acalypha indica active compounds for drug delivery by using emulsion-solvent evaporation technique. The crude extracts have been extracted and the phytochemicals inside the crude extracts are less stable in nature. These active compounds need to be encapsulated to stabilize them and delivered well into the body system. As for conclusion, chitosan:PCL is able to form better encapsulation using this method.

Application of Plackett-Burman design for screening of factors affecting pitavastatin nanoparticle formulation development.

Nanoparticle formulation of pitavastatin calcium is a potential alternative to solve the solubility related problem. However, the formulation of nanoparticle involves various parameters that affect product quality. Plackett-Burman design could facilitate an economical experimental plan that focuses on determining the relative significance of many. The objective of this study was to screen the variables which could significantly affect the pitavastatin nanoparticle formulation. The pitavastatin nanoparticles were formulated by preparing nanosuspension using the emulsion solvent evaporation technique followed by freeze-drying. A Plackett-Burman screening design methodology was employed in which seven factors at two levels were tested at 12 runs to study the effect of formulation and process variables on particle size and polydispersity index of nanoparticles. The surface morphology and crystalline nature of nanoparticle were also evaluated. The particle size and polydispersity index of nanosuspension was found in the range of 113.1 to 768.5 nm and 0.068 to 0.508, respectively. Statistical analysis of various variables revealed that stabilizer concentration, injection flow rate, and stirring rate were the most influential factors affecting the particle size and polydispersity index of the formulation. X-ray diffraction (XRD) and scanning electron microscopy (SEM) study suggested the amorphous nature of nanoparticles. This study concluded that the Plackett-Burman design was an efficient tool for screening the process and formulation variables affecting the properties of pitavastatin nanoparticles and also for the identification of the most prominent factor.

A Novel Sustained Anti-Inflammatory Effect of Atorvastatin-Calcium PLGA Nanoparticles: In Vitro Optimization and In Vivo Evaluation.

Atorvastatin Calcium (At-Ca) has pleiotropic effect as anti-inflammatory drug beside its main antihyperlipidemic action. Our study was conducted to modulate the anti-inflammatory effect of At-Ca to be efficiently sustained for longer time. Single oil-water emulsion solvent evaporation technique was used to fabricate At-Ca into polymeric nanoparticles (NPs). In vitro optimization survey was performed on Poly(lactide-co-glycolide) (PLGA) loaded with At-Ca regrading to particle size, polydispersity index (PDI), zeta potential, percent entrapment efficiency (% EE), surface morphology and in vitro release pattern. In vitro drug-polymers interactions were fully scanned using Fourier-Transform Infrared Spectroscopy (FTIR) and Differential Scanning calorimetry (DSC) proving that the method of fabrication is an optimal strategy maintaining the drug structure with no interaction with polymeric matrix. The optimized formula with particle size (248.2 ± 15.13 nm), PDI (0.126 ± 0.048), zeta potential (−12.41 ± 4.80 mV), % EE (87.63 ± 3.21%), initial burst (39.78 ± 6.74%) and percent cumulative release (83.63 ± 3.71%) was orally administered in Male Sprague–Dawley rats to study the sustained anti-inflammatory effect of At-Ca PLGA NPs after carrageenan induced inflammation. In vivo results demonstrate that AT-Ca NPs has a sustained effect extending for approximately three days. Additionally, the histological examination revealed that the epidermal/dermal layers restore their typical normal cellular alignment with healthy architecture.

Formulation and clinical performance of nanosilver loaded poly-l-glycolic acid modified orthodontic adhesive for orthodontic bonding

This study aimed to synthesize and characterize nanosilver particles (NSPs)-loaded Poly-l-glycolic acid (PLGA) nanoparticles (NPs) and to examine their mechanical properties as well as antibacterial and cytotoxicity activity. Additionally, this study investigated the association of NSPs-loaded PLGA NPs with tooth-bracket interface after mixing with commercially available orthodontic bracket adhesive for orthodontic bonding. PLGA NPs were formulated utilizing the emulsification solvent evaporation technique. NSPs-loaded PLGA NPs in orthodontic adhesive with two varying concentrations (2.5 wt.% and 5 wt.%) were characterized using the scanning (SEM) and transmission (TEM) electron microscopy, Fourier transformed infrared spectroscopy (FTIR), degree of conversion (DC), antibacterial MTT assay, cytotoxicity, shear bond strength (SBS), and adhesive remnant index (ARI), were studies after bonding to the tooth structure. The formulated PLGA NPs were round to ovoid regular structures having an average size ranging between 50 nm and 80 nm. After loading NSPs inside PLGA NPs, the morphology of the PLGA NPs was altered significantly into irregular-shaped structures. Bracket specimens treated with 5 wt.% NSPs-loaded PLGA NPs-modified adhesive exhibited the minimum mean DC values (36.4 ± 8.2). A 5 wt.% NSPs-loaded PLGA NPs-modified adhesive samples exhibited more profound antimicrobial activity against Streptococcus mutans. The minimum mean SBS scores were shown by 5 wt.% NSPs-loaded PLGA NPs-modified adhesive specimens (8.6 ± 2.5 MPa). A statistically significant difference was noticed in the mean SBS and mean ARI scores among 5 wt.% and 2.5 wt.% NSPs-loaded PLGA NPs-modified adhesive samples (p<0.05). The incorporation of NSPs-loaded PLGA NPs in commercially available Transbond XT is efficacious and safe and improved the mechanical and antibacterial properties of orthodontic bracket adhesive.

Polysaccharides as Stabilizers for Polymeric Microcarriers Fabrication.

Biodegradable polymeric microparticles are widely used in drug delivery systems with prolonged-release profiles and/or cell microcarriers. Their fabrication via the oil/water emulsion solvent evaporation technique has normally required emulsifiers in the aqueous phase. The present work aims to evaluate the effectiveness of various polysaccharides, such as chitosan, hyaluronic acid, cellulose, arabinogalactan, guar and their derivatives, as an alternative to synthetic surfactants for polylactide microparticle stabilization during their fabrication. Targeted modification of the biopolymer’s chemical structure was also tested as a tool to enhance polysaccharides’ emulsifying ability. The transformation of biomacromolecules into a form of nanoparticle via bottom-up or top-down methods and their subsequent application for microparticle fabrication via the Pickering emulsion solvent evaporation technique was useful as a one-step approach towards the preparation of core/shell microparticles. The effect of polysaccharides’ chemical structure and the form of their application on the polylactide microparticles’ total yield, size distribution and morphology was evaluated. The application of polysaccharides has great potential in terms of the development of green chemistry and the biocompatibility of the formed microparticles, which is especially important in biomedicine application.

CENTRAL COMPOSITE DESIGN FOR FORMULATION AND OPTIMIZATION OF LONG-ACTING INJECTABLE (LAI) MICROSPHERES OF PALIPERIDONE PALMITATE

Objective: The aim of the present study was to optimize long-acting injectable (LAI) microspheres of Paliperidone palmitate (PP) for treatment of schizophrenia using face-centered central composite design (FC-CCD). Methods: In this study, poly lactic-co-glycolic acid (PLGA) based LAI microspheres of paliperidone palmitate (PP) were formulated by using FC-CCD. LAI microspheres were developed by using oil in water (O/W) emulsion solvent evaporation technique. On the basis of preliminary trials, FC-CCD was employed to check effect of independent variables such as drug polymer ratio (X1), homogenization speed (X2) and rate of addition (X3). While mean particle size (Y1), drug loading (Y2), entrapment efficiency (Y3), burst release (Y4), and drug release on day 60 (Y5) were considered as dependent variables and statistically evaluation performed by using design expert 12 software. Morphology of prepared microspheres was studied by using the scanning electron microscopy (SEM) technique, while particle size was analyzed by laser diffraction technique. In vitro drug release studies were performed using a controlled temperature shaking water bath apparatus. Fourier transforms infrared spectroscopy (FTIR) and differential scanning calorimetric (DSC) study were performed to analyze any changes in crystal behavior or to detect any chemical bonding between ingredients. 13C NMR and 1H NMR techniques were used to analyze end-capping and monomer ratio in developed microspheres. Results: The factorial batches mean particle size was found to be 38 µm to 104 µm and drug loading were found between 27.2 % to 47.2%. Mathematical modelling of drug release kinetics revealed that near zero-order drug release of checkpoint formulations. Endcap analysis and molar ratio of formulated microspheres were found to be ester end cap and ~75:25, respectively. Morphologically all the prepared samples were found to be spherical in shape and smooth surface. FTIR data showed no significant interactions occurred between drug and excipients. The actual responses of checkpoint formulations were observed within 5% variation of predicted values. Conclusion: The prepared microspheres showed promising results of morphology, particle size, drug loading, entrapment efficiency, burst release and drug release on day 60. The successful predictive designs models were achieved from employed FC-CCD.

Formulation, Characterization and Cytotoxicity Effects of Novel Thymoquinone-PLGA-PF68 Nanoparticles.

Thymoquinone has anti-cancer properties. However, its application for clinical use is limited due to its volatile characteristics. The current study aims to develop a polymeric nanoformulation with PLGA-PEG and Pluronics F68 as encapsulants to conserve thymoquinone’s (TQ) biological activity before reaching the target sites. Synthesis of nanoparticles was successfully completed by encapsulating TQ with polymeric poly (D, L-lactide-co-glycolide)-block-poly (ethylene glycol) and Pluronics F68 (TQ-PLGA-PF68) using an emulsion–solvent evaporation technique. The size and encapsulation efficiency of TQ-PLGA-PF68 nanoparticles were 76.92 ± 27.38 nm and 94%, respectively. TQ released from these encapsulants showed a biphasic released pattern. Cytotoxicity activity showed that tamoxifen-resistant (TamR) MCF-7 breast cancer cells required a higher concentration of TQ-PLGA-PF68 nanoparticles than the parental MCF-7 cells to achieve IC50 (p < 0.05). The other two resistant subtypes (TamR UACC732 inflammatory breast carcinoma and paclitaxel-resistant (PacR) MDA-MB 231 triple-negative breast cell line) required a lower concentration of TQ-PLGA-PF68 nanoparticles compared to their respective parental cell lines (p < 0.05). These findings suggest that TQ encapsulation with PLGA-PEG and Pluronics F68 is a promising anti-cancer agent in mitigating breast cancer resistance to chemotherapeutics. In future studies, the anti-cancer activity of TQ-PLGA-PF68 with the standard chemotherapeutic drugs used for breast cancer treatment is recommended.

Formulation and Evaluation of Ethyl Cellulose Based Fluconazole Nanosponges

Background and Objective: Fluconazole (FLZ) is a novel triazole antifungistatic drug; topical administration of FLZ resulted in systemic absorption and skin inflammation, and thereby failed to achieve mycological eradication, resulting in low patient compliance and undermining therapy effectiveness. The aim of this study was to use the emulsion solvent evaporation technique to create FLZ-loaded nanosponges (NSs) using ethylcellulose (EC) and polyvinyl alcohol (PVA) as a stabiliser. Materials and Method: By varying the drug concentration (FLZ), EC, and PVA, four formulations were developed, each of which was then optimized through particle characterization (polydispersity index (PDI), scanning electron microscopy (SEM), zeta potential (ZP), drug entrapment, and loading efficiency). Results: SEM (Scanning Electron Microscope) analysis showed that the particle sizes of FLZ inclusion complexes ranged from 150 2 to 250 5 nm. The ZP was strong enough to produce stable formulations. FLZ was released from the nano sponges in a regulated manner for 24 hours in both in vitro and in vivo experiments. FTIR and DSC were used to validate the association of the FLZ with the nanosponges. The crystalline nature of FLZ was modified to an amorphous state due to the complexation with the nanosponges, according to an XRPD analysis. The FLZ nanosponges were found to be stable in a stability analysis. Conclusion: Therefore, ethyl cellulose-based nanosponges provide a novel method for controlling the release of FLZ for antifungal effects.

Optimized Taste-Masked Microparticles for Orally Disintegrating Tablets as a Promising Dosage Form for Alzheimer's Disease Patients.

The objective of this research was to optimize the tasted-masked microparticles for orally disintegrating tablets containing donepezil hydrochloride using quality risk assessment and design of experiment approaches. The double emulsion solvent evaporation technique using aminoalkyl methacrylate copolymer (AMC) was used to prepare taste-masked microparticles. Factors affecting the quality of the taste-masked microparticles were analyzed using an Ishikawa diagram. A risk-ranking approach was used to rank the formulation and process risks. Furthermore, the effect of AMC quantity, stirring time, and volume of outer water phase on various responses, such as particle size, the amount of drug dissolved at 5 min (Q5) in simulated saliva fluid, and mean dissolution time (MDT) in simulated gastric fluid, was investigated using the Box-Behnken design. The optimized microparticles were then used to prepare orally disintegrating tablets (ODTs) and evaluated by in vitro and in vivo testing. The results demonstrated that particle size was influenced by the AMC amount and stirring time. Q5 was significantly affected by the amount of AMC and the volume of the outer water phase. On the other hand, these two factors had a positive effect on MDT. The optimized microparticles had a particle size of 174.45 ± 18.19 µm, Q5 of 5.04%, and MDT of 5.97 min. The ODTs with taste-masked microparticles showed acceptable in vitro dissolution with an MDT of 5 min. According to the results of a panel of six human volunteers, they greatly improved palatability.

Preparation and Characterization of 5-Fluorouracil Loaded Nanogels for Skin Cancer Treatments: In Vitro Drug Release, Cytotoxicity and Cellular Uptake Analysis

Objective: The present study aimed to explore the in-vitro anticancer potential of 5-fluorouracil (5-FU) loaded PLGA nanogels coated with nerolidol sesquiterpene. Methods: The emulsification-solvent evaporation technique was used for the preparation of plain PLGA nanogels (PNGs) and 5-FU loaded PLGA nanogels (FPNGs). A surface coating of Nerolidol (2%) sesquiterpene was employed to improve the penetration efficacy of the nanogels into the stratum corneum. Results: The nanogels formulation FPNGs have the size range 220±0.25% nm obtained by dynamic light scattering. The entrapment efficiency of approx ~ 42% with a sustained-release pattern for 24 h was estimated at different pH ranges. The cell uptake and localization profile were revealed by confocal microscopy analysis using the HaCaT cell line. MTT assay demonstrated the cell compatibility of nanogels, confirmed by apoptosis assay depicting the apoptotic index of 0.87. Conclusion: This study concludes that FPNGs are a promising nanogels system against skin cancer that can be used to boost the chemo-therapeutic efficiency of bioactives with sustained and controlled release at the desired site.

Optimization of pearl millet-derived bioactive peptide microspheres with double emulsion solvent evaporation technique and its release characterization

• Bioactive peptide-loaded microspheres were successfully prepared via double emulsion solvent evaporation technique. • Central composite experimental design was used to optimized the best formulation. • Optimized formulation possessed highest entrapment efficiency with 88.23 %. • Eudrgit S100 prevented the degradation of peptide into stomach environment at low pH. • Maximum in vitro peptide release was found after in intestinal phase at pH > 6. Past decade has noticed significant scientific progress in the area of food-derived bioactive peptides. However, selection of optimum carrier system, to improve release, absorption efficiency and bioavailability of these peptides is essential. Thus, aim of the current study was to develop bioactive peptide-loaded-eudragit S100 microspheres using double emulsion solvent evaporation technique. A central composite experimental design, with two independent variables (peptide and polymer), was used to study the dependent variables (yield, particle size, and entrapment efficiency). Based on response surface methodology, thirteen formulations were developed. Regression model interpretation revealed the significant relationship between considered dependent and independent variables. Optimum formulation with peptide and polymer concentration of 9.00 mg and 58.58 mg, respectively, showed good yield (88.07 %) with particle size (150.21 μm) and promising entrapment efficiency (88.22 %). In vitro release profile of optimized formulation showed maximum peptide release (89 %) during intestinal phase at pH > 6, and followed Zero order and Hixson crowel models of release due to higher regression coefficient (R2) value which indicate the occurrence of diffusion controlled release of peptide. FT-IR study confirmed the presence of peptide in polymer without any interaction. Thus, eudragit S100 microspheres containing bioactive peptide may be an efficient way to protect peptide degradation and control release during GI environment.

Inhibition of cow's milk allergy development in mice by oral delivery of β-lactoglobulin-derived peptides loaded PLGA nanoparticles is associated with systemic whey-specific immune silencing.

BackgroundTwo to four percentage of infants are affected by cow's milk allergy (CMA), which persists in 20% of cases. Intervention approaches using early oral exposure to cow's milk protein or hydrolysed cow's milk formula are being studied for CMA prevention. Yet, concerns regarding safety and/or efficacy remain to be tackled in particular for high‐risk non‐exclusively breastfed infants. Therefore, safe and effective strategies to improve early life oral tolerance induction may be considered.ObjectiveWe aim to investigate the efficacy of CMA prevention using oral pre‐exposure of two selected 18‐AA β‐lactoglobulin‐derived peptides loaded poly (lactic‐co‐glycolic acid) (PLGA) nanoparticles (NPs) in a whey‐protein induced CMA murine model.MethodsThe peptides were loaded in PLGA NPs via a double emulsion solvent evaporation technique. In vivo, 3‐week‐old female C3H/HeOuJ mice received 6 daily gavages with PBS, whey, Peptide‐mix, a high‐ or low‐dose Peptide‐NPs or empty‐NP plus Peptide‐mix, prior to 5 weekly oral sensitizations with cholera toxin plus whey or PBS (sham). One week after the last sensitization, the challenge induced acute allergic skin response, anaphylactic shock score, allergen‐specific serum immunoglobulins and ex vivo whey‐stimulated cytokine release by splenocytes was measured.ResultsMice pre‐treated with high‐dose Peptide‐NPs but not low‐dose or empty‐NP plus Peptide‐mix, were protected from anaphylaxis and showed a significantly lower acute allergic skin response upon intradermal whey challenge compared to whey‐sensitized mice. Compared with the Peptide‐mix or empty‐NP plus Peptide‐mix pre‐treatment, the high‐dose Peptide‐NPs‐pre‐treatment inhibited ex vivo whey‐stimulated pro‐inflammatory cytokine TNF‐α release by splenocytes.Conclusion & Clinical relevanceOral pre‐exposure of mice to two β‐lactoglobulin‐derived peptides loaded PLGA NPs induced a dose‐related partial prevention of CMA symptoms upon challenge to whole whey protein and silenced whey‐specific systemic immune response. These findings encourage further development of the concept of peptide‐loaded PLGA NPs for CMA prevention towards clinical application.

Preparation and Drug Release Behavior of Nifedipine-Loaded Poly(lactic acid)/Polyethylene Glycol Microcapsules.

Nifedipine (NF)-loaded poly(lactic acid) (PLA) and PLA/polyethylene glycol (PLA/PEG) microcapsules are synthesized using a high-speed agitator and a syringe pump with an oil-in-water emulsion-solvent evaporation technique to evaluate the effect of PLA/PEG ratio on morphology and drug release behavior of the capsules. Fourier transform infrared spectroscopy (FT-IR), differential scanning calorimeter (DSC), and X-ray diffraction (XRD) results indicate that PEG reacts successfully with PLA due to the ether bond between PEG and PLA. The drug release rate of PLA and PLA/PEG capsules increases dramatically from 0 to 5 min and then reaches a plateau within 15 to 20 min. Due to the high specific surface area, the amount of NF released is raised by reducing the PLA concentration from 5 wt% to 2 wt%. Unlike PLA capsules, the drug release rate of PLA/PEG capsules increases due to the size effect by varying the PLA/PEG ratio from 10/0 to 6/4. Larger PLA/PEG capsules are attributed to higher amounts of encapsulated NF. The capsules show no evidence of cytotoxicity, suggesting that the PLA and PLA/PEG drug carriers are clinically safe.

A new combination strategy to enhance apoptosis in cancer cells by using nanoparticles as biocompatible drug delivery carriers

Some experimental and clinical studies have been conducted for the usage of chemotherapeutic drugs encapsulated into nanoparticles (NPs). However, no study has been conducted so far on the co-encapsulation of doxorubicin (Dox) and epoxomicin (Epo) into NPs as biocompatible drug delivery carriers. Therefore, we investigated if co-encapsulation of doxorubicin (Dox) and/or epoxomicin (Epo) into NPs enhance their anticancer efficiency and prevent drug resistance and toxicity to normal cells. We synthesized Dox and/or Epo loaded poly (lactic-co-glycolic acid) (PLGA) NPs using a multiple emulsion solvent evaporation technique and characterized them in terms of their particle size and stability, surface, molecular, thermal, encapsulation efficiency and in vitro release properties. We studied the effects of drug encapsulated NPs on cellular accumulation, intracellular drug levels, oxidative stress status, cellular viability, drug resistance, 20S proteasome activity, cytosolic Nuclear Factor Kappa B (NF-κB-p65), and apoptosis in breast cancer and normal cells. Our results proved that the nanoparticles we synthesized were thermally stable possessing higher encapsulation efficiency and particle stability. Thermal, morphological and molecular analyses demonstrated the presence of Dox and/or Epo within NPs, indicating that they were successfully loaded. Cell line assays proved that Dox and Epo loaded NPs were less cytotoxic to single-layer normal HUVECs than free Dox and Epo, suggesting that the NPs would be biocompatible drug delivery carriers. The apoptotic index of free Dox and Epo increased 50% through their encapsulation into NPs, proving combination strategy to enhance apoptosis in breast cancer cells. Our results demonstrated that the co-encapsulation of Dox and Epo within NPs would be a promising treatment strategy to overcome multidrug resistance and toxicity to normal tissues that can be studied in further in vivo and clinical studies in breast cancer.

Quality by Design Approach for Formulation and Optimization of Microparticles Based Inhalable Phytopharmaceuticals of Trigonella Foenum-Graecum and Alpinia Galanga

Chronic obstructive pulmonary disease has been the most widespread worldwide health problem that has influenced millions of people worldwide. The freeze-dried inhalable microparticles (FDIMs) of Trigonella foenum-graecum and Alpinia galanga extracts were synthesized by simple emulsification solvent evaporation technique using polyvinyl pyrrolidone K30 (PVP K30) and polyethylene glycol 6000 (PEG 6000) and were optimized using Box-Behnken design (BBD). Mannitol was utilized for surface modification of FDIM for enhancing their aerodynamic characteristics. The independent parameters which were utilized in the optimization strategy were herbal extract: polymer (w/w, X1), mannitol (% w/v, X2), and surfactant (% v/v, X3). The studied response variables were mean diameter (µm) (Y1) and bulk density (g/cc) (Y2). The present study concluded that optimized FDIMs could be successfully manufactured using herbal extract: polymer (1:2 w/w), mannitol (4.616 % w/v) and surfactant (1.5 % v/v), which had 0.977 desirability functions. The predicted values of response parameters of optimized FDIMs were found at 1.326 µm mean diameter and 0.244 g/cc bulk density. The percentage relative error between actual and model-predicted values of mean diameter and bulk density for optimized FDIM was found 4.09 and 2.45%, respectively (&lt; 5%), which authenticated the articulacy of the optimization approach.

Performance of simvastatin microsponges as a local treatment for chronic periodontitis – Randomized clinical trial

Simvastatin (SV) is a lipid lowering drug exhibits anti-inflammatory and anabolic effects on the bone, so it could be utilized for the local treatment of periodontitis. However, the poor solubility of SV limits its penetration through the gingival sulcus. Encapsulating SV into microsponges may have the potential to enhance the dissolution and subsequently its local penetration. In this study, SV microsponges had been prepared using the emulsion-solvent evaporation technique where, Eudragit RS-100 was employed as the polymer. The % encapsulation efficiency(%EE) of drug approached 77.32 ± 2.03. The prepared microsponges were free flowing, spherical in shape having narrow size distribution range. The particle size of the prepared microsponges was 93.79 ± 7.21 μm in diameter with a small polydispersity index (PDI) of 0.0059 ± 0.0008. In-vitro dissolution studies of SV microsponges showed that the solubility of SV had significantly enhanced upon inclusion inside the microsponges. Fourier transform infrared (FT-IR) spectroscopy indicated hydrogen bond formation between SV and Eudragit RS-100. The prepared microsponges were incorporated in chitosan 2% gels. A clinical study was conducted on 24 selected patients having bony periodontal defects to compare the efficacy of chitosan 2% gel containing free (SV) with that containing SV microsponge in treatment of chronic periodontitis. Results showed that the chitosan gels containing SV microsponges exhibited significant reduction in both pocket depth and clinical attachment loss compared to those prepared with free SV. This might be attributed to hydrogen bond formation between microsponges entrapped SV and chitosan, thus microsponges are auspicious as a carrier for SV for local treatment of periodontitis.

Statistically optimized pentazocine loaded microsphere for the sustained delivery application: Formulation and characterization.

Pentazocine (PTZ) is a narcotic analgesic used to manage moderate to severe, acute and chronic pains. In this study, PTZ loaded Ethyl cellulose microsphere has been formulated for sustained release and improved bioavailability of PTZ. These microspheres were fabricated by oil in water emulsion solvent evaporation technique. A three factorial, three levels Box-Behnken design was applied to investigate the influence of different formulation components and process variables on the formulation response using the numeric approach through the design expert® software. All the formulations were characterized for the morphology, different physicochemical properties and the results were supported with the ANOVA analysis, three dimensional contour graphs and regression equations. The maximum percentage yield was 98.67% with 98% entrapment of PTZ. The mean particle size of the formulations ranges from 50–148μm, which directly relates to the concentration of polymer and inversely proportional to the stirring speed. SEM revealed the spherical shape of PTZ microspheres with porous structures. These are physically, chemically and thermally stable as confirmed through Fourier transform infrared spectroscopy (FTIR), powder X-ray diffraction (PXRD) and thermal gravimetric (TG) analysis respectively. The microspheres provided a sustained release of the PTZ for more than 12 hours, following zero order with fickian and non fickian diffusion. The results indicate that prepared microspheres can be a potential drug delivery system (DDS) for the delivery of PTZ in the management of pains.

Nanoparticle Delivered Anti-miR-141-3p for Stroke Therapy.

Ischemic stroke and factors modifying ischemic stroke responses, such as social isolation, contribute to long-term disability worldwide. Several studies demonstrated that the aberrant levels of microRNAs contribute to ischemic stroke injury. In prior studies, we established that miR-141-3p increases after ischemic stroke and post-stroke isolation. Herein, we explored two different anti-miR oligonucleotides; peptide nucleic acid (PNAs) and phosphorothioates (PS) for ischemic stroke therapy. We used US FDA approved biocompatible poly (lactic-co-glycolic acid) (PLGA)-based nanoparticle formulations for delivery. The PNA and PS anti-miRs were encapsulated in PLGA nanoparticles by double emulsion solvent evaporation technique. All the formulated nanoparticles showed uniform morphology, size, distribution, and surface charge density. Nanoparticles also exhibited a controlled nucleic acid release profile for 48 h. Further, we performed in vivo studies in the mouse model of ischemic stroke. Ischemic stroke was induced by transient (60 min) occlusion of middle cerebral artery occlusion followed by a reperfusion for 48 or 72 h. We assessed the blood-brain barrier permeability of PLGA NPs containing fluorophore (TAMRA) anti-miR probe after systemic delivery. Confocal imaging shows uptake of fluorophore tagged anti-miR in the brain parenchyma. Next, we evaluated the therapeutic efficacy after systemic delivery of nanoparticles containing PNA and PS anti-miR-141-3p in mice after stroke. Post-treatment differentially reduced both miR-141-3p levels in brain tissue and infarct injury. We noted PNA-based anti-miR showed superior efficacy compared to PS-based anti-miR. Herein, we successfully established that nanoparticles encapsulating PNA or PS-based anti-miRs-141-3p probes could be used as a potential treatment for ischemic stroke.

Application of Central Composite Design for Development and Optimization of Eflornithine Hydrochloride-loaded Sustained Release Solid Lipid Microparticles

Topical application of eflornithine hydrochloride (EFH) is the only available non-hormonal and non-systemic choice available for hirsutism treatment. EFH has low permeability (log P is -2.9). The current investigation's objective is the development of solid lipid microparticles-based sustained topical release delivery with enhanced permeability of eflornithine hydrochloride. EFH-loaded solid lipid microparticles (EFH-SLM) composed of Monecol PC and Softemul 165 using emulsion solvent evaporation technique. The central composite design has been applied to explore an optimized EFH-SLM, which was incorporated into cream (EFH-SLM-C) and evaluated for in-vitro drug release and permeation analysis. Design expert software illustrated that an optimized EFH-SLM having desirability function (0.806) could be achieved using 1:3.74 drug: lipid (w/w) (X1), 1.84% surfactant concentration (X2), and 3.5 h stirring time (X3), which would illustrate entrapment efficiency (74.97%), drug loading (15.84%), mean diameter (102.8 µm) and process yield (78.07%). EFH-SLM-C revealed biphasic fickian diffusion release of 16.95% within 0.5 h, 52.31% in the next 4 h followed by sustained release of 88.75% over 24 h. This was confirmed by release exponent 0.411 (n &lt; 0.45) for Korsmeyer-Peppas. In-vitro steady-state flux (Jss) (µgcm-2h-1) from EFH-C and EFH-SLM-C were 17.27 and 36.65 while apparent permeability coefficient (Papp) (cmh-1) was 0.046 and 0.0977, respectively. EFH-SLM-C could be a promising strategy for augmented permeation and sustained release with minimization of dose, frequency of application, and local adverse effects.

Development and In-Vitro Evaluation of Budesonide Mucoadhesive Microspherefor Pulmonary Drug Delivery

Thepurpose of the study was to develop and evaluatemucoadhesive microspheres of Budesonide for pulmonary drug delivery systemhaving prolonged residence time and sustained drug release. Microspheres were prepared by emulsificationsolvent evaporation technique using HPMC, carbopol as polymers in varying ratios. The microspheres were evaluated for its percentage yield, drug entrapment efficiency, particle size and shape, in vitro mucoadhesion study and in vitro drug release studies.The FTIR studies revealed no chemical interaction between the drug molecule and polymers and found that drug was compatible with used polymer. The mucoadhesive microspheres showed particle size, drug entrapment efficiency and yield in the ranges of148 - 164 μm, 68.0 - 85.0%and67.52 - 87.25% respectively. In vitro drug release and mucoadhesion study confirms thatformulationF5 was the best formulation as it releases 81.8 % at the end of 12 hr. in controlled manner and percentage mucoadhesion of 75.2 % after 10 hr. This confirms the developed budesonidemucoadhesive microspheres are promising for pulmonary drug delivery system.&#x0D; &#x0D; Keywords: Budesonide, Mucoadhesion, Microspheres, Drug entrapment efficiency.