This document presents a formulation and evaluation of aceclofenac proniosome-loaded orabase for the management of dental pain. Key points include:
- Aceclofenac-loaded proniosomes were prepared using the coacervation phase separation method and characterized. Span 60-containing formulations showed the highest drug entrapment.
- Optimized proniosomal gels were incorporated into an orabase base to develop an aceclofenac-loaded proniosomal orabase.
- In vitro and ex vivo studies showed the proniosomal orabase provided prolonged drug release over 14 hours and higher permeation across buccal mucosa compared to a plain drug-loaded orabase.
Design and Evaluation of Ion Induced in Situ Gel formulation For Levofloxacin...inventionjournals
International Journal of Pharmaceutical Science Invention (IJPSI) is an international journal intended for professionals and researchers in all fields of Pahrmaceutical Science. IJPSI publishes research articles and reviews within the whole field Pharmacy and Pharmaceutical Science, new teaching methods, assessment, validation and the impact of new technologies and it will continue to provide information on the latest trends and developments in this ever-expanding subject. The publications of papers are selected through double peer reviewed to ensure originality, relevance, and readability. The articles published in our journal can be accessed online.
Evaluation of cyclosporine A eye penetration after administration of liposoma...Nanomedicine Journal (NMJ)
Abstract
A lot of researches have investigated the effects of topical cyclosporine A on the eye surface layers’ diseases. By now the main limitation in cyclosporine application is the low permeation of the drug into the posterior segments of the eye. The aim of present study was to formulate high permeable dosage form can be beneficial in the topical treatment of the uveitis. To reach higher corneal drug absorption and drug concentration in the posterior segments of the eye, 3 nanoliposomal formulations containing 0.5 mg/ml cyclosporine A were prepared. Liposomal formulations and the commercial product (Restasis®) were instilled in the right and left eyes of the rabbits, respectively. The rabbits were killed in the 3, 7, 14 and 28 days of study and the aqueous humor and vitreous were extracted. Mean size of liposomal formulation number 1, number 2 and number 3 were 107.2 ± 0.7, 129.3±0.9 and 144.8±1.8 nm and their zeta potential were -5.0±1.7, -5.5±2.3 and 44.6±6.2 mV, respectively. Results of ocular analysis showed that the liposomal formulations could increase the concentration of the drug in the aqueous and vitreous like Restasis®. But, in contrast with what has been expected the findings of this study implicate nanoliposomal formulations prepared could not make a significant difference in concentration of the drug in aqueous and vitreous humor compared to Restasis® (anionic microemulsion). In conclusion, we can state that liposomes with the same composition as our formulations are not more efficient than microemulsion for cyclosporine as ophthalmic drug delivery.
Objective: To evaluate the results of the effect of nebivolol on tibial bone defect and graft application in new bone development in the rat.
Study Design: Thirty Wistar albino rats were divided into 3 groups. In the Control group, tibia bone defect was created without any treatment. In the Defect+ Graft group, allograft treatment was performed by forming a 6 mm tibial bone defect. In the Defect+Graft+ Nebivolol group, alloplastic bone graft was placed in the calvarial bone defect and then nebivolol (0.34 mg/mL solution/day) treatment was intraperitoneally applied for 28 days.
Results: Histopathological examination revealed inflammation in the defect area, congestion in the vessels, degeneration in collagen fibers, and an increase in osteoclast cells. There was an increase in inflammation and blood vessel structure in graft application, and osteoblastic activity matrix formation after reorganization nebivolol application in collagen fibers. Osteonectin expression was positive in the collagen fiber and matrix, starting in the Graft group, in osteoblasts, whereas in the Nebivolol group, osteoblasts increased in osteocytes and new bone formation.
Conclusion: Nebivolol is thought to have a positive effect on osteoinductive bone growth factors and contribute to the cell-matrix interaction, in addition to the supporting effect of the graft with its antioxidative effect.
Keywords: allograft; bone; bone regeneration; disease models, animal; nebivolol; orthopedic procedures; osteonectin; rats; tibia; tibial defect
Design and Evaluation of Ion Induced in Situ Gel formulation For Levofloxacin...inventionjournals
International Journal of Pharmaceutical Science Invention (IJPSI) is an international journal intended for professionals and researchers in all fields of Pahrmaceutical Science. IJPSI publishes research articles and reviews within the whole field Pharmacy and Pharmaceutical Science, new teaching methods, assessment, validation and the impact of new technologies and it will continue to provide information on the latest trends and developments in this ever-expanding subject. The publications of papers are selected through double peer reviewed to ensure originality, relevance, and readability. The articles published in our journal can be accessed online.
Evaluation of cyclosporine A eye penetration after administration of liposoma...Nanomedicine Journal (NMJ)
Abstract
A lot of researches have investigated the effects of topical cyclosporine A on the eye surface layers’ diseases. By now the main limitation in cyclosporine application is the low permeation of the drug into the posterior segments of the eye. The aim of present study was to formulate high permeable dosage form can be beneficial in the topical treatment of the uveitis. To reach higher corneal drug absorption and drug concentration in the posterior segments of the eye, 3 nanoliposomal formulations containing 0.5 mg/ml cyclosporine A were prepared. Liposomal formulations and the commercial product (Restasis®) were instilled in the right and left eyes of the rabbits, respectively. The rabbits were killed in the 3, 7, 14 and 28 days of study and the aqueous humor and vitreous were extracted. Mean size of liposomal formulation number 1, number 2 and number 3 were 107.2 ± 0.7, 129.3±0.9 and 144.8±1.8 nm and their zeta potential were -5.0±1.7, -5.5±2.3 and 44.6±6.2 mV, respectively. Results of ocular analysis showed that the liposomal formulations could increase the concentration of the drug in the aqueous and vitreous like Restasis®. But, in contrast with what has been expected the findings of this study implicate nanoliposomal formulations prepared could not make a significant difference in concentration of the drug in aqueous and vitreous humor compared to Restasis® (anionic microemulsion). In conclusion, we can state that liposomes with the same composition as our formulations are not more efficient than microemulsion for cyclosporine as ophthalmic drug delivery.
Objective: To evaluate the results of the effect of nebivolol on tibial bone defect and graft application in new bone development in the rat.
Study Design: Thirty Wistar albino rats were divided into 3 groups. In the Control group, tibia bone defect was created without any treatment. In the Defect+ Graft group, allograft treatment was performed by forming a 6 mm tibial bone defect. In the Defect+Graft+ Nebivolol group, alloplastic bone graft was placed in the calvarial bone defect and then nebivolol (0.34 mg/mL solution/day) treatment was intraperitoneally applied for 28 days.
Results: Histopathological examination revealed inflammation in the defect area, congestion in the vessels, degeneration in collagen fibers, and an increase in osteoclast cells. There was an increase in inflammation and blood vessel structure in graft application, and osteoblastic activity matrix formation after reorganization nebivolol application in collagen fibers. Osteonectin expression was positive in the collagen fiber and matrix, starting in the Graft group, in osteoblasts, whereas in the Nebivolol group, osteoblasts increased in osteocytes and new bone formation.
Conclusion: Nebivolol is thought to have a positive effect on osteoinductive bone growth factors and contribute to the cell-matrix interaction, in addition to the supporting effect of the graft with its antioxidative effect.
Keywords: allograft; bone; bone regeneration; disease models, animal; nebivolol; orthopedic procedures; osteonectin; rats; tibia; tibial defect
Vesicular systems have been realized as extremely useful carrier systems in various scientific domains. Over the years, vesicular systems have been investigated as a major drug delivery system, due to their flexibility to be tailored for varied desirable purposes. In spite of certain drawbacks, the vesicular delivery systems still play an important role in the selective targeting, and the controlled delivery of various drugs. Researchers all over the world continue to put in their efforts in improving the vesicular system by making them steady in nature, in order to prevent leaching of contents, oxidation, and their uptake by natural defense mechanisms.
Nanosuspensions accelerate drug substance dissolution rates by increasing surface area and reducing particle size. The key to nanosuspension development is the identification of a suitable delivery system, such that nano-technology.
Almost Exact Procedure is provided in each & every slide ..
Thanks & Best Regards
Anurag Pandey (B.Pharm)
Contact :- anurag.dmk05@gmail.com (Facebook & Gmail)
DESIGN, PREPARATION, EVALUATION, COMPATIBILITY AND INVITRO STUDIES OF NAPROXE...Maksud Al- Hasan (Mahim)
ABSTRACT
The rationale of the present study was to design and prepare a combination product of naproxen and esomeprazole tablet by layer by layer tableting method. In this method shellac, cellulose acetate phthalate, methacrylic acid (copolymers), polyvinyl acetate phthalate and hypromellose phthalate were used as an enteric coating agent, to provide delayed action of naproxen, and esomeprazole was combined as an immediate release part which was added as a drug layer around the enteric coated naproxen core through a coating suspension.
(May 29th, 2024) Advancements in Intravital Microscopy- Insights for Preclini...Scintica Instrumentation
Intravital microscopy (IVM) is a powerful tool utilized to study cellular behavior over time and space in vivo. Much of our understanding of cell biology has been accomplished using various in vitro and ex vivo methods; however, these studies do not necessarily reflect the natural dynamics of biological processes. Unlike traditional cell culture or fixed tissue imaging, IVM allows for the ultra-fast high-resolution imaging of cellular processes over time and space and were studied in its natural environment. Real-time visualization of biological processes in the context of an intact organism helps maintain physiological relevance and provide insights into the progression of disease, response to treatments or developmental processes.
In this webinar we give an overview of advanced applications of the IVM system in preclinical research. IVIM technology is a provider of all-in-one intravital microscopy systems and solutions optimized for in vivo imaging of live animal models at sub-micron resolution. The system’s unique features and user-friendly software enables researchers to probe fast dynamic biological processes such as immune cell tracking, cell-cell interaction as well as vascularization and tumor metastasis with exceptional detail. This webinar will also give an overview of IVM being utilized in drug development, offering a view into the intricate interaction between drugs/nanoparticles and tissues in vivo and allows for the evaluation of therapeutic intervention in a variety of tissues and organs. This interdisciplinary collaboration continues to drive the advancements of novel therapeutic strategies.
Vesicular systems have been realized as extremely useful carrier systems in various scientific domains. Over the years, vesicular systems have been investigated as a major drug delivery system, due to their flexibility to be tailored for varied desirable purposes. In spite of certain drawbacks, the vesicular delivery systems still play an important role in the selective targeting, and the controlled delivery of various drugs. Researchers all over the world continue to put in their efforts in improving the vesicular system by making them steady in nature, in order to prevent leaching of contents, oxidation, and their uptake by natural defense mechanisms.
Nanosuspensions accelerate drug substance dissolution rates by increasing surface area and reducing particle size. The key to nanosuspension development is the identification of a suitable delivery system, such that nano-technology.
Almost Exact Procedure is provided in each & every slide ..
Thanks & Best Regards
Anurag Pandey (B.Pharm)
Contact :- anurag.dmk05@gmail.com (Facebook & Gmail)
DESIGN, PREPARATION, EVALUATION, COMPATIBILITY AND INVITRO STUDIES OF NAPROXE...Maksud Al- Hasan (Mahim)
ABSTRACT
The rationale of the present study was to design and prepare a combination product of naproxen and esomeprazole tablet by layer by layer tableting method. In this method shellac, cellulose acetate phthalate, methacrylic acid (copolymers), polyvinyl acetate phthalate and hypromellose phthalate were used as an enteric coating agent, to provide delayed action of naproxen, and esomeprazole was combined as an immediate release part which was added as a drug layer around the enteric coated naproxen core through a coating suspension.
(May 29th, 2024) Advancements in Intravital Microscopy- Insights for Preclini...Scintica Instrumentation
Intravital microscopy (IVM) is a powerful tool utilized to study cellular behavior over time and space in vivo. Much of our understanding of cell biology has been accomplished using various in vitro and ex vivo methods; however, these studies do not necessarily reflect the natural dynamics of biological processes. Unlike traditional cell culture or fixed tissue imaging, IVM allows for the ultra-fast high-resolution imaging of cellular processes over time and space and were studied in its natural environment. Real-time visualization of biological processes in the context of an intact organism helps maintain physiological relevance and provide insights into the progression of disease, response to treatments or developmental processes.
In this webinar we give an overview of advanced applications of the IVM system in preclinical research. IVIM technology is a provider of all-in-one intravital microscopy systems and solutions optimized for in vivo imaging of live animal models at sub-micron resolution. The system’s unique features and user-friendly software enables researchers to probe fast dynamic biological processes such as immune cell tracking, cell-cell interaction as well as vascularization and tumor metastasis with exceptional detail. This webinar will also give an overview of IVM being utilized in drug development, offering a view into the intricate interaction between drugs/nanoparticles and tissues in vivo and allows for the evaluation of therapeutic intervention in a variety of tissues and organs. This interdisciplinary collaboration continues to drive the advancements of novel therapeutic strategies.
Slide 1: Title Slide
Extrachromosomal Inheritance
Slide 2: Introduction to Extrachromosomal Inheritance
Definition: Extrachromosomal inheritance refers to the transmission of genetic material that is not found within the nucleus.
Key Components: Involves genes located in mitochondria, chloroplasts, and plasmids.
Slide 3: Mitochondrial Inheritance
Mitochondria: Organelles responsible for energy production.
Mitochondrial DNA (mtDNA): Circular DNA molecule found in mitochondria.
Inheritance Pattern: Maternally inherited, meaning it is passed from mothers to all their offspring.
Diseases: Examples include Leber’s hereditary optic neuropathy (LHON) and mitochondrial myopathy.
Slide 4: Chloroplast Inheritance
Chloroplasts: Organelles responsible for photosynthesis in plants.
Chloroplast DNA (cpDNA): Circular DNA molecule found in chloroplasts.
Inheritance Pattern: Often maternally inherited in most plants, but can vary in some species.
Examples: Variegation in plants, where leaf color patterns are determined by chloroplast DNA.
Slide 5: Plasmid Inheritance
Plasmids: Small, circular DNA molecules found in bacteria and some eukaryotes.
Features: Can carry antibiotic resistance genes and can be transferred between cells through processes like conjugation.
Significance: Important in biotechnology for gene cloning and genetic engineering.
Slide 6: Mechanisms of Extrachromosomal Inheritance
Non-Mendelian Patterns: Do not follow Mendel’s laws of inheritance.
Cytoplasmic Segregation: During cell division, organelles like mitochondria and chloroplasts are randomly distributed to daughter cells.
Heteroplasmy: Presence of more than one type of organellar genome within a cell, leading to variation in expression.
Slide 7: Examples of Extrachromosomal Inheritance
Four O’clock Plant (Mirabilis jalapa): Shows variegated leaves due to different cpDNA in leaf cells.
Petite Mutants in Yeast: Result from mutations in mitochondrial DNA affecting respiration.
Slide 8: Importance of Extrachromosomal Inheritance
Evolution: Provides insight into the evolution of eukaryotic cells.
Medicine: Understanding mitochondrial inheritance helps in diagnosing and treating mitochondrial diseases.
Agriculture: Chloroplast inheritance can be used in plant breeding and genetic modification.
Slide 9: Recent Research and Advances
Gene Editing: Techniques like CRISPR-Cas9 are being used to edit mitochondrial and chloroplast DNA.
Therapies: Development of mitochondrial replacement therapy (MRT) for preventing mitochondrial diseases.
Slide 10: Conclusion
Summary: Extrachromosomal inheritance involves the transmission of genetic material outside the nucleus and plays a crucial role in genetics, medicine, and biotechnology.
Future Directions: Continued research and technological advancements hold promise for new treatments and applications.
Slide 11: Questions and Discussion
Invite Audience: Open the floor for any questions or further discussion on the topic.
Observation of Io’s Resurfacing via Plume Deposition Using Ground-based Adapt...Sérgio Sacani
Since volcanic activity was first discovered on Io from Voyager images in 1979, changes
on Io’s surface have been monitored from both spacecraft and ground-based telescopes.
Here, we present the highest spatial resolution images of Io ever obtained from a groundbased telescope. These images, acquired by the SHARK-VIS instrument on the Large
Binocular Telescope, show evidence of a major resurfacing event on Io’s trailing hemisphere. When compared to the most recent spacecraft images, the SHARK-VIS images
show that a plume deposit from a powerful eruption at Pillan Patera has covered part
of the long-lived Pele plume deposit. Although this type of resurfacing event may be common on Io, few have been detected due to the rarity of spacecraft visits and the previously low spatial resolution available from Earth-based telescopes. The SHARK-VIS instrument ushers in a new era of high resolution imaging of Io’s surface using adaptive
optics at visible wavelengths.
Introduction:
RNA interference (RNAi) or Post-Transcriptional Gene Silencing (PTGS) is an important biological process for modulating eukaryotic gene expression.
It is highly conserved process of posttranscriptional gene silencing by which double stranded RNA (dsRNA) causes sequence-specific degradation of mRNA sequences.
dsRNA-induced gene silencing (RNAi) is reported in a wide range of eukaryotes ranging from worms, insects, mammals and plants.
This process mediates resistance to both endogenous parasitic and exogenous pathogenic nucleic acids, and regulates the expression of protein-coding genes.
What are small ncRNAs?
micro RNA (miRNA)
short interfering RNA (siRNA)
Properties of small non-coding RNA:
Involved in silencing mRNA transcripts.
Called “small” because they are usually only about 21-24 nucleotides long.
Synthesized by first cutting up longer precursor sequences (like the 61nt one that Lee discovered).
Silence an mRNA by base pairing with some sequence on the mRNA.
Discovery of siRNA?
The first small RNA:
In 1993 Rosalind Lee (Victor Ambros lab) was studying a non- coding gene in C. elegans, lin-4, that was involved in silencing of another gene, lin-14, at the appropriate time in the
development of the worm C. elegans.
Two small transcripts of lin-4 (22nt and 61nt) were found to be complementary to a sequence in the 3' UTR of lin-14.
Because lin-4 encoded no protein, she deduced that it must be these transcripts that are causing the silencing by RNA-RNA interactions.
Types of RNAi ( non coding RNA)
MiRNA
Length (23-25 nt)
Trans acting
Binds with target MRNA in mismatch
Translation inhibition
Si RNA
Length 21 nt.
Cis acting
Bind with target Mrna in perfect complementary sequence
Piwi-RNA
Length ; 25 to 36 nt.
Expressed in Germ Cells
Regulates trnasposomes activity
MECHANISM OF RNAI:
First the double-stranded RNA teams up with a protein complex named Dicer, which cuts the long RNA into short pieces.
Then another protein complex called RISC (RNA-induced silencing complex) discards one of the two RNA strands.
The RISC-docked, single-stranded RNA then pairs with the homologous mRNA and destroys it.
THE RISC COMPLEX:
RISC is large(>500kD) RNA multi- protein Binding complex which triggers MRNA degradation in response to MRNA
Unwinding of double stranded Si RNA by ATP independent Helicase
Active component of RISC is Ago proteins( ENDONUCLEASE) which cleave target MRNA.
DICER: endonuclease (RNase Family III)
Argonaute: Central Component of the RNA-Induced Silencing Complex (RISC)
One strand of the dsRNA produced by Dicer is retained in the RISC complex in association with Argonaute
ARGONAUTE PROTEIN :
1.PAZ(PIWI/Argonaute/ Zwille)- Recognition of target MRNA
2.PIWI (p-element induced wimpy Testis)- breaks Phosphodiester bond of mRNA.)RNAse H activity.
MiRNA:
The Double-stranded RNAs are naturally produced in eukaryotic cells during development, and they have a key role in regulating gene expression .
Seminar of U.V. Spectroscopy by SAMIR PANDASAMIR PANDA
Spectroscopy is a branch of science dealing the study of interaction of electromagnetic radiation with matter.
Ultraviolet-visible spectroscopy refers to absorption spectroscopy or reflect spectroscopy in the UV-VIS spectral region.
Ultraviolet-visible spectroscopy is an analytical method that can measure the amount of light received by the analyte.
What is greenhouse gasses and how many gasses are there to affect the Earth.moosaasad1975
What are greenhouse gasses how they affect the earth and its environment what is the future of the environment and earth how the weather and the climate effects.
Richard's entangled aventures in wonderlandRichard Gill
Since the loophole-free Bell experiments of 2020 and the Nobel prizes in physics of 2022, critics of Bell's work have retreated to the fortress of super-determinism. Now, super-determinism is a derogatory word - it just means "determinism". Palmer, Hance and Hossenfelder argue that quantum mechanics and determinism are not incompatible, using a sophisticated mathematical construction based on a subtle thinning of allowed states and measurements in quantum mechanics, such that what is left appears to make Bell's argument fail, without altering the empirical predictions of quantum mechanics. I think however that it is a smoke screen, and the slogan "lost in math" comes to my mind. I will discuss some other recent disproofs of Bell's theorem using the language of causality based on causal graphs. Causal thinking is also central to law and justice. I will mention surprising connections to my work on serial killer nurse cases, in particular the Dutch case of Lucia de Berk and the current UK case of Lucy Letby.
1. FORMULATION AND EVALUATION OF ACECLOFENAC
PRONIOSOME LOADED ORABASE FOR MANAGEMENT
OF DENTAL PAIN
Presented By
K. TRIDEVA SASTRI
Pharmaceutics (M.Pharm)
GITAM (DEEMED TO BE UNIVERSITY)
VISAKHAPATNAM 530045
16TH March 2019
ORAL PRESENTATION
NATIONAL CONFERENCE- Novel drug delivery systems
RAGHU College of Pharmacy
VISAKHAPATNAM
2. Oral cavities are the chief complaint about a toothache, nonsteroidal anti-
inflammatory drugs (NSAIDs) effectively mitigate acute and chronic dental,
tissues and other adjacent structures.
ACL (aceclofenac) is an NSAID and exhibits potent analgesic activity,
effective in the treatment of painful inflammatory conditions, mostly
administered orally.
Gastrointestinal disturbances raise concerns to post oral ACL administration.
Designing the delivery system with localized action at the site of ailment,
improves the efficiency of the drug by potentiating drug concentration at the
site of inflammation with low dose relative to conventional oral administration
22-08-2023
K. Trideva Sastri
2 Introduction
3. Development of new drug delivery, while improving the safety of the existing
drugs is quite challenging, expensive affair and also tedious.
Drug encapsulation in vesicular structures is one promising delivery system.
like liposomes, niosomes, ethosomes, etc
These deliver to the specific site when targeted, resulting in reduced toxicity
and with lesser adverse affects.
22-08-2023
K. Trideva Sastri
3
4. Niosomes are synthetic microscopic vesicles consisting of an aqueous core
enclosed in a bi-layer consisting of cholesterol and one or more non-ionic
surfactants.
Vesicles are prepared from self assembly of hydrated non-ionic surfactant
molecules.
22-08-2023
K. Trideva Sastri
4
Pro vesicular systems
The concept of pro-vesicular has evolved to resolve issues regarding
conventional vesicular system.
The systems consist of hydrophilic porous powders as carriers upon
which one can load phospholipid/ non-ionic surfactants and drug dissolved
in organic solvent.
E.g. Pro-liposomes, pro-niosomes etc
6. Ora base is an effective mucoadhesive base effectively employed as a drug
carrier.
It is considered as hydrophobic gel, dental paste or sometimes is referred to as
an ointment due to the presence of high portion of liquid paraffin in its
constituents.
The base consists of gelatin, pectin, mineral oil and sodium
carboxymethlycellulose in a hydrocarbon gel
22-08-2023
K. Trideva Sastri
6
7. Objective:
Prepare proniosomal gels of ACL by using various non-ionic surfactants.
To characterize proniosome gels, entrapment, microscopy, in vitro
diffusion
To incorporate optimized proniosomal gel into the mucoadhesive
orabase.
To characterize proniosomal orabase in vitro release, mucoadhesive
strength, ex vivo permeation, microscopy, FTIR- studies, and SEM.
22-08-2023
K. Trideva Sastri
7
Aim
The present investigation was to achieve the prolonged release of ACL
by loading in proniosome vesicles
To improve its retention time at the particular site of action by
incorporating drug loaded proniosomes into orabase
Mitigate analgesia and dental pain conditions
8. Literature Review
Narayan Dutt Shukla et al. described the approaches to stabilize niosomal
drug delivery system without affecting its properties of merits have resulted
in the development of the promising drug carrier, proniosomes. Proniosomes
is dry formulation using suitable carrier coated with nonionic surfactants and
can be converted into niosomes immediately before use by hydration. These
proniosome-derived niosomes are as good as or even better than conventional
niosomes. The focus of this review is to bring out different aspects related to
proniosomes preparation, clinical application and merit of Proliposomes.
22-08-2023
K. Trideva Sastri
8
9. Arora Sonia et al. described that Niosomes are one of the best carriers for
drug targeting. Niosomes are self–assembled vesicles composed primarily of
synthetic surfactants and cholesterol. They are analogous in structure to the
more widely studied liposomes formed from biologically derived
phospholipids. Niosomes are biodegradable, relatively nontoxic, more stable
and inexpensive, an alternative to liposomes. The method of preparation of
niosome is based on liposome technology. The basic process of preparation is
the same i.e. hydration by aqueous phase of the lipid phase which may be
either a pure surfactant or a mixture of surfactant with cholesterol. After
preparing niosomal dispersion, unentrapped drug is separated by dialysis
centrifugation or gel filtration. Niosomes can be SUV (Small Unilamellar
Vesicles), MLV (Multilamellar Vesicles) or LUV (Large Unilamellar Vesicles).
Niosomal drug delivery is potentially applicable to many pharmacological
agents for their action against various diseases.
22-08-2023
K. Trideva Sastri
9
10. M. Intakhab Alam et al. investigated that a low dose proniosomal gel
containing celecoxib was developed for the treatment of osteoarthritis. All the
prepared formulations were subjected to physicochemical evaluations and anti-
inflammatory studies. The entrapment was> 90%. The vesicle shape was
determined with the help of transmission electron microscopy. The vesicle
size, size distribution and poly dispersity studies were performed using photon
correlation spectroscopy. Anti-inflammatory studies were performed using the
rat hind-paw oedema induced by carrageenan (1% w/v). The selected
proniosomal gel (N1LE3) produced 100% inhibition of paw oedema in rats up
to 8 h after carrageenan injection. It produced 95% and 92% inhibition after 12
h and 24 h, respectively. These results indicate that proniosomes are a
promising carrier for the transdermal delivery of celecoxib.
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K. Trideva Sastri
10
11. Drug profile
22-08-2023
K. Trideva Sastri
11
IUPAC Name
2-[(2-{2-[(2,6
dichlorophenyl)amino]phenyl}acetyl)oxy]acetic acid
Molecular
formula
C16H13Cl2NO4
Molecular Weight 353.0216 g/mol
Category NSAID
CAS 89796-99-6
Solubility In water, 0.00199 mg/mL
Melting point 149-153°C
Therapeutic Use
Analgesic activity and is widely prescribe for the
treatment of osteoarthritis, rheumatoid arthritis, acute
lumbago, and dental pain condition
Mechanism of
action
Through COX-2 inhibition, aceclofenac
downregulates the production of various
inflammatory mediators including prostaglandin E2
(PGE2), IL-1β, and TNF from the arachidonic acid
(AA) pathway..
O
OH
O
O
NH
Cl
Cl
12. Preparation of aceclofenac proniosomal gel
ACL loaded proniosomal gel was formulated employing coacervation phase
separation method.
The required measures of surfactant, lecithin and cholesterol were dissolved in
alcohol in a beaker.
Contents were stirred uniformly using glass rod, further introduced into water
bath shaker (REMI) to warm the ingredients (60-70 ℃) for about five minutes
for complete solubilization.
Consequently, aqueous buffer pH 7.4 was added to the preparation, with gentle
warming yielded proniosomal gel on cooling.
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K. Trideva Sastri
12
13. Composition of the proniosomal formulation of Aceclofenac
22-08-2023
K. Trideva Sastri
13
Sno. Formulation Surfactant
Drug
(mg)
Soya lecithin
(mg)
Surfactant
concentration
(mg)
Cholesterol
(mg)
pH 7.4 Buffer
(ml)
1 F (ACL) 1 Span 60 10 468 468 52 1.6
2 F (ACL) 2 Span 40 10 468 468 52 1.6
3 F (ACL) 3 Span 20 10 468 468 52 1.6
4 F (ACL) 4 Span 80 10 468 468 52 1.6
14. Entrapment efficiency
Proniosomal formulations (0.2g) after reconstitution with sufficient aqueous
buffer (pH 7.4) were executed for centrifugation using a cooling centrifuge at
3500 rpm for about 1 h at 4℃.
The clear and distinct supernatant was collected carefully to separate
unentrapped ACL, and the sediment was then treated with ethanol (1 ml) to
lyse the vesicles and diluted with ethanol respectively, and absorbances were
determined spectrophotometrically at 275 nm.
% 𝐄. 𝐄 = 𝟏 −
𝐔𝐧𝐞𝐧𝐭𝐫𝐚𝐩𝐩𝐞𝐝 𝐝𝐫𝐮𝐠
𝐓𝐨𝐭𝐚𝐥 𝐝𝐫𝐮𝐠
× 𝟏𝟎𝟎
22-08-2023
K. Trideva Sastri
14
15. The Formulation comprising span 60 exhibited highest entrapment efficiency
over other spans, span 80 showed minimal entrapment efficiency.
Observed variation with entrapment efficiencies of different surfactants is the
consequence of diverse structure and length of alkyl chain used as
surfactants
22-08-2023
K. Trideva Sastri
15
0
20
40
60
80
100
120
F(AC) 1 F(AC) 2 F(AC) 3 F(AC) 4
%Drug
entraped
Formulation
16. Optical microscopy
The preparation yielded niosomal suspension upon hydration; the same was
mounted on a glass slide and examined for vesicles using a compound
microscope under 100X magnification, magnified images were captured.
22-08-2023
K. Trideva Sastri
16
17. The size of the formed vesicles has a major contribution towards in vivo fate
It is observed that the shape of proniosomal (F(ACL)1-F(ACL)4) formulations
exhibited, following hydration yields niosomes with spherical morphology on
100X magnification.
22-08-2023
K. Trideva Sastri
17
18. In vitro diffusion
In vitro release studies were performed for the preparations using Franz
diffusion cell.
An equivalent dose of ACL preparation was introduced on the membrane.
Receptor compartment was charged with pH 7.4 buffer (15 ml). Cells were
conditioned at 37±5℃ with stirring at 500 rpm.
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19. F(ACL)1 exhibited higher diffusion as compared to F(ACL)2-F(ACL)4
respectively. Commonly the release profiles of the proniosomal systems
predominantly depended on hydrophobic lipophilic balance (HLB) value
besides the alkyl chain length.
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20. Preparation of aceclofenac proniosomal and pure
aceclofenac orabase
Required equivalent quantities of gelatin, pectin, sodium
carboxymethylcellulose, polyethylene glycol, and liquid paraffin were blended
and triturated in optimum ratios for obtaining a smooth orabase in a mortar and
pestle.
Further desired amount of aceclofenac loaded proniosomal gel and aceclofenac
pure was incorporated with uniform stirring until homogeneity was achieved.
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21. In vitro release studies
The preparation equivalent aceclofenac was diluted with 1 ml of the buffer,
introduced to the lower end of the glass cylinder on preconditioned dialysis
membrane.
The cylinder was maintained at 30 rpm with the membrane end being
submerged in the dissolution jars. The dissolution medium phosphate buffer
pH 7.4 was maintained at 37±5℃.
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22. Release profiles comprehend the efficiency in the delivery of the drug by
the proposed system. This specifies that the lipid bilayer of niosomes
limits drug release.
The release from proniosomal orabase was slow and spread over
more than 14 h, compared to ACL orabase with a complete release
within a few hours.
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-20
0
20
40
60
80
100
120
0 2 4 6 8 10 12 14 16
%
drug
release
time (h)
Proniosomal Orabase Drug Orabase
23. Mucoadhesive strength of the proniosomal orabase
formulation
The mucoadhesive strength of aceclofenac loaded proniosomal orabase formulation was
determined by measuring the potency necessary for detaching the preparation from oral goat
mucosa using dispensing balance.
Equal pieces (2.5×2.5 cm), cut from the goat oral mucosal membranes, were horizontally fixed to
the upper stage of the dispensing balance keeping the mucosal side out.
Proniosomal preparation (0.5 g) was positioned on the lower steel stage enabling the sample
surface to adjoin mucosal membrane attached to the upper stage.
The sample was placed adjacent to the mucosal membrane for 5 min. Into the other pan of
dispensing balance water was added in dropwise manner until the mucosal membrane extricates
from the gel sample.
The minimum amount of water required to detach the formulation from the oral mucosa
surface was determined by using the following equation
Detachment stress = (m/g)A
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24. The weight applied to detach the mucous from the proniosomal gel
mucoadhesive strength was found to be 6370 dynes/cm2
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25. Ex vivo permeation studies
Proniosomal orabase permeation against buccal mucosa was determined
employing altered Franz diffusion cell.
The buccal mucosal membrane of goat pre-conditioned was placed in
between donor and receptor compartments with the mucosal side facing the gel
sample in the donor compartment.
An equivalent amount of proniosomal orabase was introduced to the donor
compartment, and subsequently, 50 ml of phosphate buffer filled in the
receptor compartment maintained at 37±5℃ and stirred at 50 rpm.
𝐊𝐩 = 𝐉𝐬𝐬 𝐂𝐝𝐨𝐧𝐚𝐫
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26. Percentage drug released for proniosomal orabase and ACL loaded orabase
were determined to be 36.6% and 21.6% respectively with permeation
coefficient of 10.397 cm2/h and 3.270 cm2/h. exhibited flux of 230 µg/cm2/h
and 110µg/cm2/h for proniosomal orabase and aceclofenac loaded orabase
respectively.
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0
5
10
15
20
25
30
35
40
45
0 5 10 15 20 25 30
%
drug
permeated
time (h)
Proniosomal Orabase Drug Orabase
27. Drug deposited in oral mucosa
Selected proniosomal orabase formulation exhibited 68.26% retention in the
oral mucosa.
The formulation showed significant deposition within the oral mucosal layer
when compared to control preparation.
This reveals potential aspects of these intact niosomes to overcome the
epithelial barrier of the oral mucosa and enhance concentrate within mucosal
layers.
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28. Optical microscopy
It is observed that the shape of proniosomal orabase formulation exhibited
spherical morphology at 100X magnification.
The proniosomal orabase formulation system exhibited abundant vesicle
formation in contrast to drug orabase.
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30. Scanning electron microscopy (SEM)
SEM images revealed the well identified spherical morphology of
proniosomal orabase, post hydration prepared employing span 60
Formulation exhibited particle size ranges from 136 μm to 236 μm
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31. CONCLUSION
Proniosomal gel formulation F(ACL)1, considered optimal formulation with
EE% (97.60±1.85 %) post reconstitution.
The optimal formula was further incorporated into orabase with desirable
mucoadhesive behavior essential to achieve increased retention for effective
pain management.
The formula exhibited significant permeation with two-fold increased flux
and sustained for longer periods compared to the aceclofenac control at the
same dose level.
Hence, orabase loaded with proniosomal gels may be a promising carrier for
NSAIDs in dental pain management with their intact vesicles and safety
aspects for local action for longer periods with simple preparation technique.
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