scholarly journals A 23 FACTORIAL DESIGN FOR FORMULATION AND DEVELOPMENT OF DOXYCYCLINE HYDROCHLORIDE IN SITU GEL FORMING SOLUTION FOR WOUND HEALING APPLICATION

2021 ◽  
pp. 221-232
Author(s):  
N. VISHAL GUPTA ◽  
S. SHANMUGANATHAN ◽  
SANDEEP KANNA ◽  
K. TRIDEVA SASTRI
Keyword(s):  
Wound Healing ◽  
Antimicrobial Agents ◽  
Gelation Time ◽  
In Vitro Release ◽  
In Vivo Studies ◽  
Control Group ◽  
Gelation Temperature ◽  
Vitro Release

Objective: To develop and formulate doxycycline hydrochloride hydrogels employing various polymers for wound healing application. Methods: A thermo-reversible gel can transmute from a sol-gel in replication to environmental temperature vicissitudes made up of gallic acid (GA) and tamarind seed polysaccharide (TSP). An antimicrobial agent (doxycycline hydrochloride) integrated to provide the benefit and efficiently safeguard the wound from infection. A low temperature causes TSP to aggregate intermolecularly with GA to create a gel network. GA–TSP gel heat stability increased with increased concentration of GA. Prepared gel formulations were optimized by 23 factorial designs further evaluated for stability and compatibility, appearance, gelation temperature, gravitational flow simulation, in vitro release, in vivo excision wound model in rats. Results: A strong viscoelastic gel was formed at body temperature in the GA–TSP mixture containing 0.6% (w/v) GA. The prepared formulation exhibited absolute stability and compatibility. The formulations indicated a range of 23±1.47 to 50±1.40 °C. The viscosity values were in the range 6628 to 19146 cps. The optimized gel formulation (DT8) was prepared to analyze the checkpoints and further evaluated for gelation temperature ( °C), viscosity (cps), gelation time (s), and in vitro release of drugs (percent cumulative release of drugs) up to 12 h reflecting R1=36.5±0.61 °C, R2=12887±11 cps, R3=16.2±1.38 min and R4=94.65±0.59 percent. Formulation DT8 showed significant wound healing property and it is comparable to the control group. Formulation DT9 treated group showed faster epithelialization and greater rates of wound contraction in rats. Conclusion: The formulations comprising of TSP with antimicrobial agents demonstrated to be efficient in wound healing. Out of all formulations, DT8 showed better wound healing ability, which is evident from in vivo studies.

In vitro Controlled Release of two new Tuberculocidal Adamantane Aminoethers from Solid Pharmaceutical Formulations (II)

Drug Research ◽  
2017 ◽  
Vol 67 (11) ◽  
pp. 653-660 ◽  
Author(s):  
Marilena Vlachou ◽  
Angeliki Siamidi ◽  
Dimitrios Spaneas ◽  
Dimitrios Lentzos ◽  
Polixeni Ladia ◽  
...  
Keyword(s):  
Controlled Release ◽  
In Vitro Release ◽  
Pharmaceutical Formulations ◽  
Adamantane Derivative ◽  
In Vivo Studies ◽  
Matrix Tablet ◽  
The Us ◽  
Vitro Release

AbstractThe aim of the present investigation was to develop matrix tablet formulations for the in vitro controlled release of two new tuberculocidal adamantane aminoethers (compounds III and IV), congeneric to the adamantane derivative SQ109, which is in final clinical trials, and aminoethers (I) and (II), using carefully selected excipients, such as polyvinylpyrrolidone, sodium alginate and lactose. The tablets were prepared using the direct compression method and dissolution experiments were conducted using the US Pharmacopoeia type II apparatus (paddle method) in gastric and intestinal fluids. The results suggest that both analogues, albeit more lipophilic than SQ109, and aminoethers (I) and (II), have the requisite in vitro release characteristics for oral administration. In conclusion, these formulations merit further assessment by conducting in vivo studies, at a later stage.

Development of Polymeric Nanocarriers for Brain Targeted Delivery of Atorvastatin: A Quality-By-Design Approach

2020 ◽  
Vol 10 (2) ◽  
pp. 149-158
Author(s):  
Guilherme A.G. Martins ◽  
Fabio S. Murakami ◽  
Mauro S. Oliveira ◽  
Ana F. Furian ◽  
Helen Treichel ◽  
...  
Keyword(s):  
Quality By Design ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
Physicochemical Characteristics ◽  
In Vivo Studies ◽  
Mean Size ◽  
Release Study ◽  
Vitro Release

Objective: Atorvastatin (ATV) is effective in reducing total cholesterol and low-density lipoprotein levels. Furthermore, it produces pleiotropic effects in neurodegenerative conditions such as Parkinson's, Alzheimer's, and epilepsy. However, due to the effective defense system of the central nervous system (CNS), the development of new medicines for clinical conditions has proven difficult. In this context, nanotechnology was applied as a promising solution to promote drug vectorization to the brain. Methods: The solvent emulsification-diffusion method was used to develop nanoparticles (NPs) based on polylactic acid and coated with polysorbate 80 containing ATV. Quality-by-Design (QbD) was used in the optimization of nanoparticles production through the application of the experimental design Box-Behnken Design. Results: After optimizing the independent factors including sonication time, surfactant concentration and surfactant volume, the NPs presented physicochemical characteristics such as entrapment efficiency of 86.4 ± 2.4%, mean size of 225.2 ± 4.8 nm, and zeta potential of -14.4 ± 0.36 mV. In the in vitro release study, approximately 20% of the encapsulated ATV was released. Conclusion: The application of QbD was very useful in demonstrating its applicability in the nanotechnological pharmaceutical area for controlling and predicting the influence of the variables in the production of NPs. The NPs developed in this study presented adequate physicochemical characteristics, which is promising for future in vivo studies. The physicochemical characteristics included entrapment efficiency of 86.4 ± 2.4%, mean size of 225.2 ± 4.8 nm, and zeta potential of -14.4 ± 0.36 mV. In the in vitro release study, approximately 20% of the encapsulated ATV was released. The application of QbD was very useful in demonstrating its applicability in the nanotechnological pharmaceutical area for controlling and predicting the influence of the variables in the production of NPs. The NPs developed in this study presented adequate physicochemical characteristics, which is promising for future in vivo studies.

Formulation and Evaluation of Pimozide Buccal Mucoadhesive Patches

1970 ◽  
Vol 2 (4) ◽  
pp. 739-747
Author(s):  
Biswajit Basu ◽  
Kevin Garala ◽  
Thimmasetty J
Keyword(s):  
Release Kinetics ◽  
In Vitro Release ◽  
In Vivo Studies ◽  
Poly Vinyl Alcohol ◽  
Content Uniformity ◽  
In Vivo Absorption ◽  
Systemic Drug Delivery ◽  
Vitro Release

Within the oral mucosal cavity, the buccal region offers an attractive route of administration for systemic drug delivery. Pimozide patches were prepared using HPMC (15 & 47 cPs), carbopol 934, poly vinyl alcohol, and poly vinyl pyrolidone. FTIR and UV spectroscopic methods revealed that there is no interaction between pimozide and polymers. The patches were evaluated for their thickness uniformity, folding endurance, weight uniformity, content uniformity, swelling behaviour, tensile strength, and surface pH. In vitro release studies of pimozide-loaded patches in phosphate buffer (pH, 6.6) exhibited drug release in the range of 55.32 % to 97.49 % in 60 min. Data of in vitro release from patches were fit in to different equations and kinetic models to explain release kinetics. The models used were zero and first-order equations, Hixon-Crowell, Higuchi and Korsmeyer-Peppas models. In vivo absorption of pimozide from all the patches ranged from 47.96 % to 83.42 % in 60 min in human volunteers. In vivo studies in rabbits showed 85.97% of drug absorption from HPMC-15 cPs patch in 60 min. Good correlation among in vitro release and in vivo absorption of pimozide was observed

Enhanced “In Vitro“ Release of Platelet α-Granules After Acute Myocardial Infarction (AMI)

1985 ◽  
Vol 54 (02) ◽  
pp. 544-546 ◽  
Author(s):  
V Pengo ◽  
M Boschello ◽  
P Prandoni ◽  
R Schiavon ◽  
F Bellotto ◽  
...  
Keyword(s):  
Coronary Care Unit ◽  
In Vitro Release ◽  
Control Group ◽  
Platelet Activity ◽  
Platelet Factor ◽  
Coronary Care ◽  
Vitro Release ◽  
Simultaneous Assessment

SummaryIn vivo platelet activity was studied in 58 patients with AMI on admittance to the Coronary Care Unit, in 48 of these patients after 1 week, in 30 after 1 month and in 24 patients after 6 months. Patients were carefully selected and excluded if they had associated diseases known to increase platelet activity. In vivo activation was studied by evaluating the plasma concentration of beta-thromboglobulin (β-TG) and platelet factor 4 (PF4) in the same blood sample. On admittance (x = 58.5) and on day 7 (x = 52.9) β-TG values were significantly higher than those obtained in the control group (x = 29). β-TG values were moderately elevated after 1 month (x = 37.7) and then returned to values similar to those of the control group after 6 months (x = 27.9). The simultaneous assessment of PF4 shows a β-TG/PF4 ratio indicative for in vitro release (≤2.5) in many patients on days 1 and 7. Moreover, the β-TG/PF4 ratio in patients with AMI tends towards 2 when β-TG values are high. These results may indicate a greater tendency to an in vitro platelet release in the acute phase of AMI.

scholarly journals Influence of Porous Dressings Based on Butyric-Acetic Chitin Co-Polymer on Biological Processes In Vitro and In Vivo

Materials ◽  
2019 ◽  
Vol 12 (6) ◽  
pp. 970 ◽  
Author(s):  
Witold Sujka ◽  
Zbigniew Draczynski ◽  
Beata Kolesinska ◽  
Ilona Latanska ◽  
Zenon Jastrzebski ◽  
...  
Keyword(s):  
Wound Healing ◽  
Subcutaneous Tissue ◽  
Biological Effects ◽  
Skin Irritation ◽  
Early Period ◽  
In Vivo Studies ◽  
Control Group ◽  
Dressing Materials

In spite of intensively conducted research allowing for the development of more and more advanced wound dressing materials, there is still a need for dressings that stimulate not only reparative and regenerative processes, but also have a positive effect on infected and/or difficult-to-heal wounds. Porous dressing materials based on butyric-acetic chitin co-polyester containing 90% of butyryl and 10% of acetyl groups (BAC 90/10) can also be included in the group mentioned above. Two types of dressings were obtained by the salt leaching method, i.e. a porous sponge Medisorb R and Medisorb Ag with an antibacterial additive. The aim of the study was to evaluate biological effects of porous Medisorb R and Medisorb Ag dressings under in vitro and in vivo conditions. In an in vitro biodegradation test, no mass loss of Medisorb R dressing was observed within 14 days of incubation in physiological fluids at 37 °C. However, on the basis of the FTIR (Fourier Transform Infrared Spectroscopy) tests, surface degradation of Medisorb R dressing was observed. Additionally, the antibacterial activity of the porous Medisorb Ag dressing containing microsilver as an antibacterial additive was confirmed. The in vivo studies included inflammatory activity, skin irritation and sensitisation tests, as well an assessment of local effect after contact with subcutaneous tissue up to 6 months and skin wounds up to 21 days. In the in vivo tests, the dressings exhibited neither effects of skin irritation nor sensitisation. Under macroscopic examination, in full thickness defects of subcutaneous tissue and skin, the dressings caused wound healing with no inflammation, undergoing the most gradual biodegradation between weeks 4 and 8, and the observed differences were statistically significant. In the histological assessment, a weakened, limited inflammatory process associated with degradation of the material has been observed. The process of skin wound healing under Medisorb R dressing in the early period was accelerated compared to that observed in the control group with a gauze dressing.

Bosentan Monohydrate Vesicles Loaded Transdermal Drug Delivery System: In Vitro In Vivo Evaluation

2017 ◽  
Vol 7 (1) ◽  
Author(s):  
Revathi M. ◽  
Indira Y.
Keyword(s):  
Controlled Release ◽  
Delivery System ◽  
Ex Vivo ◽  
In Vitro Release ◽  
In Vivo Studies ◽  
In Vivo Evaluation ◽  
Vitro Release ◽  
Transdermal Route

This study elucidates the enhancement of the permeation of bosentan monohydrate through skin by encapsulating it in vesicles loaded transdermal delivery system. Niosomal vesicles were formulated by ether injection method. Formulation FN7 (span 60: cholesterol: poloxamer 401, 1.25:1:0.25) showed maximum entrapment efficiency of 96.7±0.037% and was optimized for loading in to transdermal system. Transdermal systems were formulated using both hydrophilic and hydrophobic polymers like HPMC, HEC and EC. Formulation F1 with HPMC was optimized based on in vitro release (99.21±1.45 %) and was further evaluated for ex-vivo permeation. The results indicate that the ex vivo release (98.13±1.65%) was as par with in vitro release and followed zero order super case- II transport mechanism. The in vivo studies were done on New Zealand male rabbits for oral and transdermal route. The results inferred no significant change in half-life of drug but a substantial difference in Tmax, AUC and MRT was observed in transdermal systems. A two fold increase in AUC was observed in transdermal route (18.609±7.251µg/ml/h) when compared to oral route (9.644±5.621µg/ml/h). A controlled release was attained up to 35h and reservoir effect was observed and this may be due to the barrier properties of skin. Drug encapsulated niosomes were released in to the skin by loosening the lipid layers and the surfactant acted as penetration enhancer. The study infers that niosomes loaded transdermal patches of bosentan monohydrate can enhance the bioavailability and provided controlled release for better therapeutic efficacy and safety of drug.

scholarly journals Effect of Sodium Lauryl Sulfate (SLS) on Primary Human Gingival Fibroblasts in an In Vitro Wound Healing Model

2019 ◽  
Vol 184 (Supplement_1) ◽  
pp. 97-101 ◽  
Author(s):  
Augustine H Chuang ◽  
Justin Bordlemay ◽  
Jeremy L Goodin ◽  
James C McPherson
Keyword(s):  
Wound Healing ◽  
Sodium Lauryl Sulfate ◽  
Potential Effect ◽  
Human Gingival Fibroblasts ◽  
In Vivo Studies ◽  
Control Group ◽  
Lauryl Sulfate ◽  
Gingival Fibroblasts

Abstract Objectives Sodium lauryl sulfate (SLS) is a surfactant used to decrease the surface tension of water. Most commercially available dentifrices contain 0.5–2.0% SLS. This study investigated the potential effect of SLS on oral wound healing using primary human gingival fibroblasts (HGFs). Methods HGFs cells were grown in12-well culture plates in DMEM medium. A 3 mm wound was created on confluent HGFs. The cells were challenged with 0 (the control group), 0.01, 0.02, 0.03, 0.04, or 0.05% SLS-containing media once daily for 2 minutes. The cells were stained on day 0, 2, 4, 6 and 8. The percent of wound fill area was measured. Results On day 2, 4, 6, and 8, the wound fill of the control group (0% SLS) was 15, 35, 67 and 98%, respectively; at 0.01% SLS, it was 10, 20, 65 and 84%; at 0.02%, it was 7, 10, 15 and 25%; at 0.03% SLS, it was only 5% and 8% on day 2 and 4. Conclusion Our results showed a dose- and time-dependent inhibition on HGFs wound fill by SLS; however, future in vivo studies are needed to validate if our in vitro findings using SLS-free dentifrices to avoid the potential delay of wound healing.

Reliability of a Single β-Thromboglobulin Measurement in a Diabetic Population : Importance of PGE1 in Anticoagulant Mixture

1987 ◽  
Vol 57 (02) ◽  
pp. 201-204 ◽  
Author(s):  
P Y Scarabin ◽  
L Strain ◽  
C A Ludlam ◽  
J Jones ◽  
E M Kohner
Keyword(s):  
In Vitro Release ◽  
Mean Value ◽  
Reliable Estimate ◽  
Diabetic Patients ◽  
Single Measurement ◽  
Diabetic Population ◽  
The Difference ◽  
Vitro Release

SummaryDuring the collection of samples for plasma β-thromboglobulin (β-TG) determination, it is well established that artificially high values can be observed due to in-vitro release. To estimate the reliability of a single β-TG measurement, blood samples were collected simultaneously from both arms on two separate occasions in 56 diabetic patients selected for a clinical trial. From each arm, blood was taken into two tubes containing an anticoagulant mixture with (tube A) and without (tube B) PGE!. The overall mean value of B-TG in tube B was 1.14 times higher than in tube A (p <0.01). The markedly large between-arms variation accounted for the most part of within-subject variation in both tubes and was significantly greater in tube B than in tube A. Based on the difference between B-TG values from both arms, the number of subjects with artifically high B-TG values was significantly higher in tube B than in tube A on each occasion (overall rate: 28% and 14% respectively). Estimate of between-occasions variation showed that B-TG levels were relatively stable for each subject between two occasions in each tube. It is concluded that the use of PGEi decreases falsely high B-TG levels, but a single measurement of B-TG does not provide a reliable estimate of the true B-TG value in vivo.

Development, in vitro and in vivo Evaluations of Solid-Lipid Microparticles based on Solidified Micellar Carrier System for Oral Delivery of Cefepime

2017 ◽  
Vol 10 (1) ◽  
pp. 3582-3593
Author(s):  
Chukwuebuka Umeyor ◽  
Uchechukwu Nnadozie ◽  
Anthony Attama
Keyword(s):  
Oral Delivery ◽  
In Vitro Release ◽  
Carrier System ◽  
Solid Lipid ◽  
Solid Lipid Microparticles ◽  
Release Study ◽  
Lipid Microparticles ◽  
Vitro Release

This study seeks to formulate and evaluate a solid lipid nanoparticle-based, solidified micellar carrier system for oral delivery of cefepime. Cefepime has enjoyed a lot of therapeutic usage in the treatment of susceptible bacterial infections; however, its use is limited due to its administration as an injection only with poor patient compliance. Since oral drug administration encourage high patient compliance with resultant effect in improved therapy, cefepime was formulated as solid lipid microparticles for oral delivery using the concept of solidified micellar carrier system. The carrier system was evaluated based on particle yield, particle size and morphology, encapsulation efficiency (EE %), and thermal analysis using differential scanning calorimeter (DSC). Preliminary microbiological studies were done using gram positive and negative bacteria. In vitro release study was performed using biorelevant media, while in vivo release study was performed in white albino rats. The yield of solid lipid microparticles (SLM) ranged from 84.2 – 98.0 %. The SLM were spherical with size ranges of 3.8 ± 1.2 to 42.0 ± 1.4 µm. The EE % calculated ranged from 83.6 – 94.8 %. Thermal analysis showed that SLM was less crystalline with high potential for drug entrapment. Microbial studies showed that cefepime retained its broad spectrum anti-bacterial activity. In vitro release showed sustained release of cefepime from SLM, and in vivo release study showed high concentration of cefepime released in the plasma of study rats. The study showed that smart engineering of solidified micellar carrier system could be used to improve oral delivery of cefepime.

Formulation and Evaluation of Itopride Hydrochloride Floating Beads for Gastroretentive Delivery

2013 ◽  
Vol 6 (4) ◽  
pp. 2269-2280
Author(s):  
Nagratna Dhople ◽  
P N Dandag ◽  
A P Gadad ◽  
C K Pandey ◽  
Masthiholimath V S
Keyword(s):  
Sustained Release ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
Sustained Release Formulation ◽  
Prokinetic Drug ◽  
Drug Entrapment Efficiency ◽  
Itopride Hydrochloride ◽  
Vitro Release

A gastroretentive sustained release system of itopride hydrochloride was formulated to increase the gastric residence time and modulate its release behavior. Itopride hydrochloride is a prokinetic drug used in the treatment of gastroeosophageal reflux disease, Non-ulcer dyspepsia and as an antiemetic. Hence, itopride hydrochloride beads were prepared by emulsion gelation method by employing low methoxy pectin and sodium alginate as sustained release polymers in three different ratios alone and in combination and sunflower oil was used to enable floating property to the beads. The effect of variation in polymer and their concentration was investigated. The beads were evaluated for production yield, particle size, swelling index, density measurement, buoyancy, drug content, drug entrapment efficiency, in vitro release characteristics and release kinetic study. Based on drug entrapment efficiency, buoyancy, swelling and in vitro release, F9 was selected as the optimized formulation. F9 was further subjected to surface morphology by SEM, in vitro release comparison with marketed formulation, in vivo floating study in rabbits and stability study for 90 days. In vitro release follows zero order and fitted in Korsmeyer peppas model (Non-Fickian release). Therefore, the rate of drug release is due to the combined effect of drug diffusion and polymer swelling. The in vivo X-ray studies revealed that the beads were floating in the rabbit stomach up to 10 hours. Thus, it was concluded that the sustained release formulation containing itopride hydrochloride was found to improve patient compliance, minimize the side effects and decrease the frequency of administration.

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